Patents Assigned to Leo Pharmaceutical Products Ltd.
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Patent number: 7071178Abstract: Compounds of the formula I wherein X represents hydrogen or hydroxy; Y represents oxygen or sulphur or oxidized sulphur selected from the groups S(O) and S(O2); R1 and R2, which may be the same or different, represent hydrogen or a residue after removal of 1 hydrogen atom from a straight, branched or cyclic, saturated or unsaturated, C1–C6-hydrocarbon; or R1 and R2, together with the carbon atom to which they are attached (marked with an asterisk in formula I), bearing the group X, form a C3–C8 carbocyclic ring; Q represents a diradical residue after removal of 2 hydrogen atoms from a straight, branched or cyclic, saturated or unsaturated C1–C8-hydrocarbon; and R3 represents hydrogen or a residue after removal of 1 hydrogen atom from a straight, branched or cyclic, saturated or unsaturated C1–C6-hydrocarbon; may be used for the preparation of a medicament for the treatment and/or prophylaxis of osteoporosis and related bone disorders.Type: GrantFiled: January 31, 2001Date of Patent: July 4, 2006Assignee: Leo Pharmaceutical Products, Ltd.Inventors: Gunnar Grue-Sørensen, Henrik Pedersen, Ernst Torndal Binderup, Mikael Tranholm
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Patent number: 6897236Abstract: The present invention relates to compounds of formula (I) wherein R1, R2 and R3 independently represent one or more, same or different substituents selected from the group consisting of hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, carbamoyl, or phenyl; R1 and R2 further represented by nitro and R3 by carboxy; R4 represents hydrogen, (C1-C3)alkyl, or allyl; Q represents a bond, or —C(R6)(R7)(—O—C?O)—, in which formula R6 and R7 independently represent hydrogen, trifluoromethyl, or (C1-C4)alkyl; Y represents either (C5-C15)alkyl, (C2-C15)olefinic group, (C3-C10)monocyclic hydrocarbon, or phenyl, any of which may be optionally substituted with one or more, same or different substituents represented by the formula R5; or (C1-C4)alkyl substituted with at least one or more substituents with the formula R5; or Y represents a group of formula —CH2—(Z—O)n—Z where Z is a (C1-C3)alkyl,Type: GrantFiled: July 11, 2000Date of Patent: May 24, 2005Assignee: Leo Pharmaceutical Products, Ltd.Inventors: Erik Rytter Ottosen, Heinz Wilhelm Dannacher
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Patent number: 6787529Abstract: The present invention relates to a pharmaceutical gel composition for application on skin, said composition comprising at least one vitamin D or vitamin D analogue and at least one corticosteroid as well as a viscosity-increasing excipient.Type: GrantFiled: October 26, 2001Date of Patent: September 7, 2004Assignee: Leo Pharmaceutical Products Ltd. A/SInventors: Gert Høy, Erik Johannes Didriksen
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Patent number: 6753013Abstract: A pharmaceutical composition for dermal use, wherein the composition has a first pharmacologically active component A consisting of at least one vitamin D or vitamin D analogue, and a second pharmacologically active component B consisting of at least one corticosteroid, wherein the difference between the maximum stability pH of said first component A and the maximum stability pH of said second component B is at least 1.Type: GrantFiled: October 22, 2001Date of Patent: June 22, 2004Assignee: Leo Pharmaceutical Products, Ltd. A/SInventors: Erik Didriksen, Gert Høy
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Patent number: 6750253Abstract: The present invention relates to compounds of the formula wherein R1 independently represents one or more, same or different substituents selected from the group consisting of halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, carbamoyl, phenyl and nitro, provided that when R1 represents one substituent, it is in the ortho position, and when R1 represents more than one substituent, at least one R1 substituent is in the ortho position; R2 is one substituent in the ortho position, said substituent being selected from the group consisting of hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, carbamoyl, phenyl and nitro; R3 represents hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1Type: GrantFiled: February 22, 2002Date of Patent: June 15, 2004Assignee: Leo Pharmaceutical Products Ltd. A/SInventor: Erik Rytter Ottosen
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Publication number: 20040014144Abstract: In a method of identifying substances acting as inhibitors of NF-&kgr;B activation by MSK1 or MSK2, MSK1 or MSK2 are contacted with a predetermined amount of one or more test substances in the presence of an NF-&kgr;B subunit or a complex of NF-&kgr;B subunits, and a test substance is identified as an inhibitor of NF-&kgr;B activation by determining a decrease in NF-&kgr;B activation by MSK1 or MSK2 in the presence of said test substance compared to the level of NF-&kgr;B activation in the absence of said test substance.Type: ApplicationFiled: June 3, 2003Publication date: January 22, 2004Applicant: Leo Pharmaceutical Products Ltd. A/SInventors: Mogens Winkel Madsen, Lone Stengelshoj Olsen, Manianne Scheel Fjording
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Patent number: 6673783Abstract: Novel 17,20-methanofusidic acid derivatives are used in pharmaceutical compositions for the treatment of infections, in particular in topical compositions for the treatment of skin or eye infections.Type: GrantFiled: March 7, 2002Date of Patent: January 6, 2004Assignee: Leo Pharmaceutical Products Ltd. A/SInventor: Tore Duvold
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Patent number: 6646143Abstract: Compounds of the formula I wherein X represents hydrogen or hydroxy; R1 and R2, which may be the same or different, represent hydrogen, (C1-C4)alkyl optionally substituted with one hydroxyl group or one or more fluorine atoms, or, together with the carbon atom to which they are attached, R1 and R2 form a (C3-C5)carbocyclic ring; R3 represents (C1-C4)alkyl, (C1-C4)alkoxy or a halogen atom, such as fluorine, chlorine, bromine, or iodine, and in-vivo hydrolyzable esters thereof with pharmaceutically acceptable acids, may be used in the prophylaxis and/or treatment of dieases characterized by abnormal cell differentiation and/or cell proliferation.Type: GrantFiled: March 20, 2001Date of Patent: November 11, 2003Assignee: Leo Pharmaceutical Products Ltd. A/SInventor: Kai Holst Hansen
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Patent number: 6646129Abstract: The present invention relates to hitherto unknown compounds of formula (I) or their tautomeric forms, the attachment to the pyridine ring being in the 3- or 4-position, in which formula R stands for one or more substituents which can be the same or different and are selected from the group consisting of: hydrogen, halogen, trifluoromethyl, carboxy, C1-C4 alkyl, alkoxy or alkoxycarbonyl, nitro, amino or cyano and Q stands for C5-C14 divalent hydrocarbon radical which can be straight, branched, cyclic, saturated or unsaturated and X stands for carboxy, C1-C4 alkoxycarbonyl, di(C1-C4 alkoxy)-phosphinoyloxy, amino, C1-C4 alkoxycarbonylamino or tetrahydropyranyloxy; and pharmaceutically acceptable, non-toxic salts and N-oxides thereof. The present compounds are of value in the human and veterinary practice.Type: GrantFiled: February 4, 2002Date of Patent: November 11, 2003Assignee: Leo Pharmaceutical Products Ltd. A/SInventors: Charlotte Schou Hunneche, Erik Rytter Ottosen
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Patent number: 6624199Abstract: The present invention relates to compounds of formula I wherein R1 represents one or more, similar or different substituents; R2 represents hydrogen, hydroxy, halogen, alkyl, alkoxy, alkylthio, or cyano; R3 represents one or more, similar or different substituents; and R6 represents hydrogen or methyl; and salts thereof with pharmaceutically acceptable acids, hydrates, and solvates, and to the use of compounds of the general formula II in which formula R1 and R2 independently represent one or more, similar or different substituents; R3 represents hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, amino, alkyl, alkoxy, alkylthio, alkylamino, or alkoxycarbonyl, phenyl, cyano, carboxy, or carbamoyl; R4, R5 and R6 represent independently hydrogen, trifluoromethyl, alkyl, carbamoyl, alkoxycarbonyl, or alkaloyl; x represents oxygen, N—OH, and N—O-alkyl, dialkoxy, cyclic dialkoxy, dialkylthio, or cyclic dialkylthio, and salts thereof with pharmaceutically acceptablType: GrantFiled: February 22, 2002Date of Patent: September 23, 2003Assignee: Leo Pharmaceuticals Products Ltd. A/SInventors: Erik Rytter Ottosen, Fredrik Björkling
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Patent number: 6593319Abstract: Novel 17,20-dihydrofusidic acid derivatives are used in pharmaceutical compositions for the treatment of infections, in particular in topical compositions for the treatment of skin or eye infections.Type: GrantFiled: August 14, 2001Date of Patent: July 15, 2003Assignee: Leo Pharmaceutical Products, Ltd. A/SInventors: Tore Duvold, Welf von Daehne
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Patent number: 6573255Abstract: Vitamin D compounds formula I wherein R represents hydrogen, or R represents (C1-C6)alkyl, phenyl, or (C7-C9)aralkyl, optionally substituted with one or more groups selected from (C1-C3)alkyl, F, phenyl; n is an integer having the value 0, 1, or 2; and X represents hydroxy or halogen.Type: GrantFiled: February 1, 2002Date of Patent: June 3, 2003Assignee: Leo Pharmaceutical Products Ltd., A/SInventor: Claus Aage Svensgaard Bretting
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Patent number: 6566554Abstract: The present invention relates to a compound of general formula (I) wherein R1, R2, and R3 represents one or more, same or different substituents selected from the group consisting of halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)akylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, —CONH2, phenyl, or nitro; further R2 can be hydrogen, and R3 can be carboxy and carbamoyl; R4 represents hydrogen, (C1-C3)alkyl, or allyl; X represents oxygen or sulphur; Q represents —(CO)—, —(CS)—, or a bond; Y represents (C5-C15)alkyl; (C2-C15)olefinic group; (C3-C10)monocyclic hydrocarbon group; or phenyl; any of which may be optionally substituted by one or more, same or different substituents selected from the group consisting of the formula R5 defined below; (C1-C4)alkyl substituted by one or more substituents selected for the group R5; or a group of the formula —(Z—O)n—Z, wherein Z is a (C1-C3)alkyl, n is anType: GrantFiled: February 22, 2002Date of Patent: May 20, 2003Assignee: Leo Pharmaceutical Products Ltd. a/s (Lovens Kemiske Fabrik Produktionsaktieselskab)Inventor: Erik Rytter Ottosen
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Patent number: 6555710Abstract: The present invention relates to compounds of formula (I) wherein R1 and R2 independently represent one or more, same or different substituents selected from the group consisting of halogen, hydroxy, mercapto, trifluoromethyl, amino (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, carbamoyl, phenyl, or nitro; R2 further being represented by hydrogen; R3 represents hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, phenyl, cyano, carboxy or carbomoyl; R4 represents hydrogen, (C1-C3)alkyl, or allyl; X represents oxygen or sulpher; with the proviso that formula (I) does not comprise the compound 2,2,2-trifluoro-N-[2-[3-chloro-4-(2-methylbenzoyl)-phenylamino]-phenyl]acetamide wherein R1 is a 2-methyl, R2 is 2-chloro, R3 and R4 is hydrogen, and X is oxygen; and a salt thereof with a pharmaceutically accepType: GrantFiled: March 15, 2002Date of Patent: April 29, 2003Assignee: Leo Pharmaceutical Products Ltd a/s Lovens Kemiske Fabrik ProduktionsaktieselskabInventor: Erik Rytter Ottosen
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Patent number: 6541670Abstract: A compound of the general formula I wherein R1 represents a substituent selected from the group consisting of halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, —CONH2, phenyl, and nitro; R2 represents one or more, same or different substituents selected from the group consisting of hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, —CONH2, phenyl, and nitro; R3 represents one or more, same or different substituents selected from the group consisting of hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, cyano, carboxy, carbamoyl, (C1-C10)alkyl, (C2-C10)olefinic group, (C3-C8)monocyclic hydrocarbon group, (C1-C10)alkoxy, (C1-C10)alkylthio, (C1-C10)alkoxycarbonyl, and phenyl; R4 represents hydrogen, (C1-C6)alkyl, (C2-C6)olefinicType: GrantFiled: March 20, 2001Date of Patent: April 1, 2003Assignee: Leo Pharmaceutical Products Ltd. A/SInventor: Erik Rytter Ottosen
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Patent number: 6537980Abstract: The present invention relates to compounds of general formula (I) wherein R1 and R2, which may be the same or different, represent (C1-C4)alkyl, and R3 represents hydrogen, halogen, (C1-C4)alkyl, or O—(C1-C4)alkyl, and in-vivo hydrolysable esters there with pharmaceutically acceptable acids. The present compounds are of value in the human and veterinary practice.Type: GrantFiled: October 23, 2001Date of Patent: March 25, 2003Assignee: Leo Pharmaceutical Products Ltd.Inventor: Kai Holst Hansen
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Patent number: 6525077Abstract: A compound of the formula is disclosed, the compound being suited for therapeutical uses. The invention also discloses compositions comprising said compound, methods of treatment involving administering said compound to a patient, and the use of said compound in the manufacture of medicaments.Type: GrantFiled: November 20, 2001Date of Patent: February 25, 2003Assignee: Leo Pharmaceutical Products Ltd. A/SInventors: Ernst Binderup, Pernille-Julia Vig Hjarnaa
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Patent number: 6521606Abstract: A compound of the general formula I wherein Y is O or S; n is 1, 2, 3 or 4; X represents hydroxamic acid, carboxylic acid, phosphonic acid, acetylthiomethyl group or a mercaptomethyl group; R1 is wherein E, when present represents, a bond or optionally substituted methylene or ethylene; s and t are independently 0, 1, 2 or 3; A and A′ independently represent a bond, or a saturated or unsaturated, optionally substituted cyclic or heterocyclic hydrocarbon di- or triradical; Z represents a bond, O, S, C(O), C(O)NR7, NR7C(O) or NR7, wherein R7 is hydrogen, hydroxy, branched or straight, saturated or unsaturated, optionally substituted hydrocarbon radical; R5 represents a bond, alkane or alkene diradical, one or more ether diradicals (R—O—R′) or amine diradicals (R—N—R′), wherein R and R′ independently represent alkane or alkene diradicals with a C-content from 0 to 3; R6 represents hydrogen, hydroxy, halogen, cyano, nitro,Type: GrantFiled: July 6, 2001Date of Patent: February 18, 2003Assignee: Leo Pharmaceutical Products, Ltd. A/SInventors: Morten Dahl Sørensen, Lars Kristian Albert Blæhr, Mette Knak Christensen
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Patent number: 6486137Abstract: A mixture of linear oligosaccharides containing different numbers of repeating sulphated disaccharide units derived from L-iduronic acid (IdoA) and N-acetyl-D-galactosamine (Gal-NAc) and having the following characteristics (a) a molecular weight in the range of 1600-20000 for 90% or more of the mixture, (b) a sulphur content of 6.0-8.0% by weight, (c) a sulphate/carboxylate ratio of 1.2-1.6, (d) a disulphated disaccharide content of 20-60% by weight of the mono-sulphated disaccharide content, and (e) an antithrombin activity of 20-60 IU/mg. The mixture may be used as an antithrombotic agent and is prepared by depolymerisation of dermatan sulphate by periodate oxidation, followed by borohydride reduction and acid hydrolysis and then ion exchange fractionation.Type: GrantFiled: December 3, 1999Date of Patent: November 26, 2002Assignee: Leo Pharmaceutical Products Ltd. A/SInventors: Mons Lundqvist, Kristian Betton Johansen
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Patent number: 6432962Abstract: Heteroaryl aminobenzophenones of general formula I inhibit interleukin-1&bgr; and TNF-&agr; and may therefore be useful in the therapy of inflammatory diseases and conditions.Type: GrantFiled: May 21, 2001Date of Patent: August 13, 2002Assignee: Leo Pharmaceutical Products Ltd. A/SInventor: Anne Marie Horneman