Patents Assigned to Leo Pharma A/S
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Publication number: 20100279936Abstract: The invention relates to novel compounds according to formula Ia and Ib; (Formula Ia and Ib) wherein A represents substituted or unsubstituted C1-10heteroaryl, C6-14aryl or C6-10heterocycloalkylaryl; R1 is C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6hydroxyalkyl, C1-6haloalkyl, C1-6amino, C3-6 cycloalkyl, or C1-6heterocycloalkyl, each of which are optionally substituted; X represents —CR3R4—(CR5R6)n—(CR7?CR8)m—(C6-14aryl)r-(C1-10heteroaryl)s-(CR9R10)p—(CR11?CR12)q, R2 represents C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6hydroxyalkyl, C1-6haloalkyl, C1-6amino, C1-12alkylsilyl, C6-30alkylarylsilyl, C1-10heteroaryl, C6-14aryl, C1-10heterocycloalkyl, C1-10heterocycloalkenyl, C1-8cycloalkyl, C1-18cycloalkenyl, each of which is optionally substituted, or R2 represents hydrogen, carboxy, or hydroxy; or a pharmaceutically acceptable salt, solvate, or ester thereof; to processes for the preparation thereof, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, wherein said compounType: ApplicationFiled: August 16, 2007Publication date: November 4, 2010Applicant: LEO PHARMA A/SInventors: Xifu Liang, Thomas Høyer, Jef Fensholdt, Sophie Elisabeth Havez, Bjarne Nørremark
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Patent number: 7807682Abstract: Compounds according to formula I wherein R1 represents hydrogen, halogen or one or more straight or branched, saturated or unsaturated C1-6 hydrocarbon radical, optionally substituted with halogen, hydroxy, cyano, nitro, carboxy, alkoxy, alkoxycarbonyl, alkylcarbonyl, formyl, amino, aminoalkyl, aminocarbonyl, alkylcarbonylamino, sulfo, aminosulfonyl, alkylsulfonylamino, hydroxysulfonyloxy, dihydroxyphosphinoyloxy or phosphono; X represents a straight or branched, saturated or unsaturated C1-12 hydrocarbon diradical, optionaly substituted with halogen, hydroxy, cyano, nitro, carboxy, alkoxy, alkoxycarbonyl, alkylcarbonyl, formyl, amino, aminoalkyl, aminocarbonyl, alkylcarbonylamino, sulfo, aminosulfonyl, alkylsulfonylamino, hydroxysulfonyloxy, dihydroxyphosphinoyloxy or phosphono; Y represents a bond, 0, C(O), S, S(O), S(0)2, C(O)O, NH, C(O)NH, OC(O) or NHC(O); Z represents an aromatic or non-aromatic heterocyclic radical with 5-12 ring atoms, optionally substituted with halogen, hydroxy, cyano, nitro, alkType: GrantFiled: November 30, 2007Date of Patent: October 5, 2010Assignee: Leo Pharma A/SInventor: Fredrik Bjorkling
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Publication number: 20100122356Abstract: The present invention relates to a genetically modified pig as a model for studying psoriasis. The modified pig model displays one or more phenotypes associated with psoriasis. Disclosed is also a modified pig comprising a mutation in the endogenous ILK-I Ra, JunB/cJun, CD18, IKK2, and/or LIG1 gene, and/or a human, porcine and/or murine PPARs, PPAR-?, l?B-?, STAT3c, Integrin beta 1, Integrin alpha 2, MEK1, Amphiregulin, BMP-6, VEGF, JunB?ec-Jun?ep, IL-I a, TGF.beta 1, CD18 hypo, Cre/lkk2FL/FL, Dsg1, SCCE, TGF-a, TNF-a, IL-20, IFN-g, LIG1 KO, KGF, IL-6, PAFR1 Cre/lkk2FL/FL, IL1 R, Dsg3, IFN-gamma, p40, ILI Ra, IKK2, JunB/c-Jun, and/or LIG1 gene, transcriptional and/or translational product or part thereof. The invention further relates to methods for producing the modified pig; and methods for evaluating the effect of a therapeutical treatment of psoriasis, for screening the efficacy of a pharmaceutical composition, and a method for treatment of human being suffering from psoriasis are disclosed.Type: ApplicationFiled: March 7, 2008Publication date: May 13, 2010Applicants: AARHUS UNIVERSITET, LEO PHARMA A/S, SYDDANSK UNIVERSITETInventors: Peter Michael Kragh, Lars Axel Bolund, Karsten Kristiansen, Charlotte Brandt Sørensen, Jacob Giehm Mikkelsen, Nicklas Heine Staunstrup, Thomas Kongstad Petersen, Lars Svensson
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Publication number: 20100099688Abstract: The present invention relates to a compound according to formula I, wherein X, A, G, E, R1, R2, R3 are as shown herein; and pharmaceutically acceptable salts, hydrates, N-oxides or solvates hereof. The invention further relates to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases, e.g. dermal diseases, with said compounds, and to the use of said compounds in the manufacture of medicaments.Type: ApplicationFiled: February 26, 2008Publication date: April 22, 2010Applicant: Leo Pharma A/SInventors: Jakob Felding, Simon Feldbaek Nielsen, Jens Christian Højland Larsen, Bollu Ravindra Babu
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Publication number: 20090131389Abstract: The present invention relates to processes for the crystallisation and for the preparation and isolation of a novel crystalline form of fusidic acid, to the use of said processes in the manufacture of pharmaceutical formulation or medicament, and to the use of said crystalline fusidic acid form for the treatment of bacterial infections.Type: ApplicationFiled: October 30, 2006Publication date: May 21, 2009Applicant: LEO PHARMA A/SInventors: Jan Jensen, Niels Rastrup Andersen
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Publication number: 20090054389Abstract: A pharmaceutical composition for topical application comprises a fusidic acid derivative of general formula I as disclosed herein and one or more monoglycerides of a fatty acid. The composition may be used in the treatment of a disease or condition of the skin or mucosa, in particular skin infections.Type: ApplicationFiled: February 1, 2007Publication date: February 26, 2009Applicant: Leo Pharma A/SInventor: Mette Rydahl Sonne
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Publication number: 20080312275Abstract: Novel pyridyl cyanoguanidine compounds of general formula I (I) wherein R1, X, R2 and R3 are as defined herein, exhibit a high antiproliferative activity and may be used in the treatment of hyperproliferative and neo-plastic diseases.Type: ApplicationFiled: December 20, 2005Publication date: December 18, 2008Applicant: LEO Pharma A/SInventors: Fredrik Bjørkling, Heinz Wilhelm Dannacher
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Publication number: 20080118930Abstract: A screening method for agents which are capable of reversing resistance to the antibiotic fusidic acid in bacteria that contain the fusB resistance gene or a homologue thereof and that express the FusB fusidic acid resistance protein or a homologue thereof based on the interaction between the fusB resistance protein or a homologue thereof with elongation factor-G (EF-G) protein.Type: ApplicationFiled: October 14, 2005Publication date: May 22, 2008Applicant: LEO PHARMA A/SInventors: Ian Chopra, O'Neil Alexander
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Publication number: 20080090842Abstract: Compounds according to formula I wherein R1 represents hydrogen, halogen or one or more straight or branched, saturated or unsaturated C1-6 hydrocarbon radical, optionally substituted with halogen, hydroxy, cyano, nitro, carboxy, alkoxy, alkoxycarbonyl, alkylcarbonyl, formyl, amino, aminoalkyl, aminocarbonyl, alkylcarbonylamino, sulfo, aminosulfonyl, alkylsulfonylamino, hydroxysulfonyloxy, dihydroxyphosphinoyloxy or phosphono; X represents a straight or branched, saturated or unsaturated C1-12 hydrocarbon diradical, optionaly substituted with halogen, hydroxy, cyano, nitro, carboxy, alkoxy, alkoxycarbonyl, alkylcarbonyl, formyl, amino, aminoalkyl, aminocarbonyl, alkylcarbonylamino, sulfo, aminosulfonyl, alkylsulfonylamino, hydroxysulfonyloxy, dihydroxyphosphinoyloxy or phosphono; Y represents a bond, 0, C(O), S, S(O), S(0)2, C(O)O, NH, C(O)NH, OC(O) or NHC(O); Z represents an aromatic or non-aromatic heterocyclic radical with 5-12 ring atoms, optionally substituted with halogen, hydroxy, cyano, nitro, alType: ApplicationFiled: November 30, 2007Publication date: April 17, 2008Applicant: LEO Pharma A/SInventor: Fredrik Bjorkling
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Publication number: 20070255066Abstract: The present invention relates to processes for epimerising alcohols of compounds having a hydroxyl substituent on an asymmetric allylic carbon, such as compounds useful for the synthesis of vitamin D analogues where the epimeric hydroxyl substituent is at the 24 position. The Invention further relates to methods of producing intermediates useful for the synthesis of calcipotriol by said epimerisation processes.Type: ApplicationFiled: August 22, 2005Publication date: November 1, 2007Applicant: Leo Pharma A/SInventors: Hendrik Pedersen, Claus Age Bretting, Ernst Binderup
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Publication number: 20070249676Abstract: Pyridyl cyanoguanidine compounds of the general formula I wherein A, X1, X2, X3, Y1, Y2, Y3, R1, R2, R5, R6 and n are as indicated in the description are suitable as prodrugs in human and veterinary therapy of proliferative diseases such as cancers.Type: ApplicationFiled: June 28, 2007Publication date: October 25, 2007Applicant: LEO Pharma A/SInventors: Ernst Binderup, Tore Duvold
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Publication number: 20070244117Abstract: The invention relates to compounds of general formula I wherein D, E, F, G, W, Y, R1, A, R9, X, B, R8 are as defined herein, and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, for treating diseases associated with deregulated angiogenesis, such as cancer.Type: ApplicationFiled: December 2, 2004Publication date: October 18, 2007Applicant: Leo Pharma A/SInventors: Jef Fensholdt, Jacob Thorhauge, Bjarne Norremark
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Publication number: 20070215455Abstract: The present invention relates to an isomerisation method of vitamin D analogues, such as compounds useful for the synthesis of calcipotriol, and to and to the use of a flow-through photoreactor or continuous flow photoreactor reactor for making said vitamin D analogues. The present invention relates further to the use of intermediates produced with said method for making calcipotriol or calcipotriol monohydrate, or pharmaceutical formulations thereof.Type: ApplicationFiled: May 11, 2006Publication date: September 20, 2007Applicant: Leo Pharma A/SInventors: Michael Folkmann, Erik Hansen
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Patent number: 7253193Abstract: Pyridyl cyanoguanidine compounds of the general formula I wherein A, X1, X2, X3, Y1, Y2, Y3, R1, R2, R5, R6 and n are as indicated in the description are suitable as prodrugs in human and veterinary therapy of proliferative diseases such as cancers.Type: GrantFiled: May 15, 2003Date of Patent: August 7, 2007Assignee: LEO Pharma A/SInventors: Ernst Torndal Binderup, Tore Duvold
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Publication number: 20070167488Abstract: Certain oxindole compounds have been found to be effective in experimentally induced autoimmune encephalitis and are therefore suggested for the preparation of a medicament for the prevention, treatment or amelioration of multiple sclerosis, or to delay the onset of or reduce the relapse rate in multiple sclerosis.Type: ApplicationFiled: December 16, 2004Publication date: July 19, 2007Applicant: Leo Pharma A/SInventors: Laetitia Bouerat Duvold, Jef Fensholdt, Simon Nielsen, Xifu Liang, Sophie Havez, Ellen Anderson, Lene Jensen, Jens Hansen
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Publication number: 20070135395Abstract: The present invention relates to novel methods for the preparation of intermediates which are useful in the synthesis of cacipotriol. The present invention relates further to the use of intermediates produced with said methods for making calcipotriol or calcipotriol monohydrate.Type: ApplicationFiled: March 23, 2005Publication date: June 14, 2007Applicant: Leo Pharma A/SInventors: Erik Hansen, Thomas Sabroe, Martin Calverley, Henrik Pedersen, Heinz-Josef Deussen
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Publication number: 20070105826Abstract: Fusidic acid derivatives substituted at C-24 may be used in therapy for the treatment of infections.Type: ApplicationFiled: July 9, 2004Publication date: May 10, 2007Applicant: LEO PHARMA A/SInventors: Tore Duvold, Claus Svensgaard Bretting, Poul Rasmussen, Laetitia Duvold, Jacob Thorhauge
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Publication number: 20070027333Abstract: The present invention relates to intermediates useful for the synthesis of calcipotriol or calcipotriol monohydrate, to methods of producing said intermediates, and to methods of stereoselectively reducing said intermediates.Type: ApplicationFiled: March 10, 2005Publication date: February 1, 2007Applicant: Leo Pharma A/SInventors: Thomas Sabroe, Martin Calverley
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Publication number: 20060166949Abstract: Compounds according to formula I in which formula R1 and R2, which may be the same or different, represent halogen, (C1-C6)hydrocarbyl, optionally substituted with one or two hydroxyl group or one or more fluorine atoms, or, together with the carbon atom to which they are both attached, R1 and R2 form a (C3-C6)carbocyclic ring, or one of R1 and R2 taken together with R3 forms a direct bond, such that a triple bond is constituted, or R1 and R2 represent both hydrogen; R3 when not forming a direct bond with one of R1 and R2 represents hydrogen or (C1-C3)hydrocarbyl; X represents (E)-ethylene, (Z)-ethylene, ethynylene, or a bond; Y and Z independently represent hydrogen or methyl; the bond between C#16 and C#17 is depicted with a dotted line to illustrate that said bond may be either a single bond, in which case the projection of the ring substituent is beta, or a double bond; A represents hydroxyl, fluorine or hydrogen; B represents CH2 or H2; the configuration in the 3-position corresponds to the same cType: ApplicationFiled: October 23, 2003Publication date: July 27, 2006Applicant: Leo Pharma A/SInventors: Ernst Binderup, Holst Kai, Aage Svensgaard Claus, John Martin
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Patent number: RE39706Abstract: The present invention relates to calcipotriol hydrate—a new crystalline form of calcipotriol—with superior technical properties and with superior stability.Type: GrantFiled: January 15, 1993Date of Patent: June 26, 2007Assignee: Leo Pharma A/SInventors: Erik Torngaard Hansen, Niels Smidt Rastrup Andersen, Lene Hoffmeyer Ringborg