Solna, Sweden
Solna, Sweden

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Pelcman B.,Uppsala University | Sanin A.,Biolipox AB | Nilsson P.,Uppsala University | Nilsson P.,Biolipox AB | And 14 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2015

Investigation of 1N-substituted pyrazole-3-carboxanilides as 15-lipoxygenase-1 (15-LOX-1) inhibitors demonstrated that the 1N-substituent was not essential for activity or selectivity. Additional halogen substituents on the pyrazole ring, however, increased activity. Further development led to triazole-4-carboxanilides and 2-(3-pyrazolyl) benzoxazoles, which are potent and selective 15-LOX-1 inhibitors. © 2015 Elsevier Ltd. All rights reserved.


Pelcman B.,Uppsala University | Sanin A.,Biolipox AB | Nilsson P.,Uppsala University | Nilsson P.,Biolipox AB | And 11 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2015

High-throughput screening was used to find selective inhibitors of human 15-lipoxygenase-1 (15-LOX-1). One hit, a 1-benzoyl substituted pyrazole-3-carboxanilide (1a), was used as a starting point in a program to develop potent and selective 15-LOX-1 inhibitors. © 2015 Elsevier Ltd. All rights reserved.


PubMed | Uppsala University, MedChem ApS, Biolipox AB and Karolinska University Hospital
Type: Journal Article | Journal: Bioorganic & medicinal chemistry letters | Year: 2015

High-throughput screening was used to find selective inhibitors of human 15-lipoxygenase-1 (15-LOX-1). One hit, a 1-benzoyl substituted pyrazole-3-carboxanilide (1a), was used as a starting point in a program to develop potent and selective 15-LOX-1 inhibitors.


PubMed | Uppsala University, MedChem ApS, Biolipox AB and Karolinska University Hospital
Type: Journal Article | Journal: Bioorganic & medicinal chemistry letters | Year: 2015

Investigation of 1N-substituted pyrazole-3-carboxanilides as 15-lipoxygenase-1 (15-LOX-1) inhibitors demonstrated that the 1N-substituent was not essential for activity or selectivity. Additional halogen substituents on the pyrazole ring, however, increased activity. Further development led to triazole-4-carboxanilides and 2-(3-pyrazolyl) benzoxazoles, which are potent and selective 15-LOX-1 inhibitors.


Patent
Biolipox AB | Date: 2010-12-08

The present invention is directed to a method for reducing the emetogenic effects of PDE inhibitors, and more particularly is directed to compounds having PDE4 inhibition activity with little or no emetogenic side-effects, and chemical methods including benzylation for preparing such compounds. A benzyl group may be attached to either a carbon or nitrogen atom of a PDE4 inhibitor. Suitable benzylation chemistry is to extract a hydrogen from a PDE4 inhibitor, preferably with a base, and then react the resulting nucleophilic PDE4 inhibitor with a benzylating agent, e.g., benzyl bromide or a derivative thereof.


There is provided homogeneous pharmaceutical compositions for the treatment of, for example, rhinitis, asthma and/or chronic obstructive pulmonary disease comprising a corticosteroid and an antihistamine, a polar lipid liposome and a pharmaceutical-acceptable aqueous carrier.


Patent
Biolipox AB | Date: 2012-04-11

There is provided pharmaceutical compositions for the treatment of rhinitis by, for example, nasal or ocular administration comprising zwitterionic cetirizine, a polar lipid liposome and a pharmaceutical acceptable aqueous carrier. The compositions are preferably homogeneous in their nature.

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