Patents by Inventor Christian Hubschwerlen
Christian Hubschwerlen has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
-
Publication number: 20110059946Abstract: The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria:Type: ApplicationFiled: September 10, 2010Publication date: March 10, 2011Applicant: Morphochem Aktiengesellschaft fuer Kombinatorische ChemieInventors: Christian Hubschwerlen, Jean-Luc Specklin
-
Publication number: 20110039836Abstract: The invention relates to antibacterial compounds of formula (I) wherein U represents CH or N; W represents CH or N; R1 represents alkoxy, halogen or CN; ring A represents a pyrrolidin-1,3-diyl-, a piperidin-1,3-diyl or a morpholin-2,4-diyl group and B represents CH2; or ring A is selected from the groups drawn below: wherein R2 represents H, F or hydroxymethyl, and B is absent; G represents a group selected from the group consisting of —CH?CH-E, wherein Y1, Y2, Y3 and Z independently represent CH or N; Q represents O or S; and E represents phenyl which is mono- or di-substituted wherein the substituents are each independently halogen; and to pharmaceutically acceptable salts of such compounds.Type: ApplicationFiled: April 14, 2009Publication date: February 17, 2011Applicant: ACTELION PHARMACEUTICALS LTD.Inventors: Christian Hubschwerlen, Georg Rueedi, John-Philippe Surivet, Cornelia Zumbrunn-Acklin
-
Publication number: 20110039823Abstract: The invention relates to compounds of formula (I) wherein U, V, W, X, R1, R2, R3, R4, R5, R6, A, B, D, E, G, m, and n are as defined in the description, to pharmaceutically acceptable salts of such compounds for use in the manufacture of a medicament for the prevention or treatment of a bacterial infection. Certain compounds of formula (I) are new and are also part of this invention.Type: ApplicationFiled: April 11, 2008Publication date: February 17, 2011Applicant: Actelion Pharmaceuticals LtdInventors: Daniel Bur, Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
-
Patent number: 7888359Abstract: The invention relates to antibiotic cyclohexyl or piperidinyl carboximide derivatives of formula (I) wherein R1 represents hydrogen, halogen, (C1-C4)alkyl, (C1-C4)alkoxy, cyano or COOR2, R2 being (C1-C4)alkyl; one or two of U, V, W and X represent(s) N and the remaining represent each CH, or, in the case of X, may also represent CRX, RX being a halogen atom; either B represents N and A represents CH2CH2 or CH(OR3)CH2, or B represents CH or C(OR4) and A represents OCH2, CH2CH(OR5), CH(OR6)CH2, CH(OR7)CH(OR8), CH?CH or CH2CH2; each of R3, R4, R5, R6, R7, and R8 represents independently hydrogen, SO3H, PO3H2, CH2OPO3H2 or COR9, R9 being either CH2CH2COOH or such that R9—COOH is naturally occurring amino acid or dimethylaminoglycine; and to salts of such compounds of formula (I).Type: GrantFiled: March 22, 2007Date of Patent: February 15, 2011Assignee: Actelion Pharmaceutical Ltd.Inventors: Christian Hubschwerlen, Rueedi Georg, Jean-Philippe Surivet, Cornelia Zumbrunn Acklin
-
Publication number: 20110003789Abstract: The invention relates to antibacterial compounds of formula I wherein one or two of U, V, W, and X represent N, the rest represent CH or, in the case of X, may also represent CRa wherein Ra is fluorine; R1 represents alkoxy, halogen or cyano; R2 represents H, CH2OH, CH2N3, CH2NH2, alkylcarbonylaminomethyl or triazol-1-ylmethyl; R3 represents H, or, when n is 1, R3 may also represent OH, NH2, NHCOR6 or triazol-1-yl; A represents CR4; K represents O, NH, OCH2, NHCO, NHCH2, CH2NH, CH2CH2, CH?CH, CHOHCHOH or CHR5; R4 represents H or together with R5 forms a bond, or also R4 can represent OH when K is not O, NH, OCH2 or NHCO; R5 represents OH or together with R4 forms a bond; R6 represents alkyl; m is 0 or 1 and n is 0 or 1; and G is as defined in the description; and to salts of such compounds.Type: ApplicationFiled: December 17, 2008Publication date: January 6, 2011Inventors: Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn Acklin
-
Publication number: 20100331318Abstract: The invention relates to antibacterial compounds of formula I wherein n is 0 or 1; R1 represents H or F; U represents CH2 or, provided n is 1, O or NH; “-----” is a bond or is absent; V represents CH or N when “-----” is a bond, or CH2 or NH when “-----” is absent; W represents CH or N; A represents —(CH—)p—NH—(CH2)q— wherein p is 1 and q is 1 or 2 or, provided U represents CH2 and n is 1, p may also be 0 and q is then 2; G represents one of the groups wherein Z represents N or CH and Q represents O or S; and Z0, Z1 and Z2 each represent CH, or Z0 and Z1 each represent CH and Z2 represents N, or Z0 represents CH, Z1 represents N and Z2 represents CH or N, or Z0 represents N and Z1 and Z2 each represent CH; and to salts of such compounds.Type: ApplicationFiled: February 19, 2009Publication date: December 30, 2010Applicant: Actelion Pharmaceuticals Ltd.Inventors: Christian Hubschwerlen, Georg Rueedi, John-Philippe Surivet, Cornelia Zumbrunn-Acklin
-
Publication number: 20100331308Abstract: The invention relates to compounds of Formula (I) wherein U, V, W, R1, R1b, A and G are as defined in the description, to pharmaceutically acceptable salts of such compounds and to the use of these compounds in the manufacture of a medicament for the prevention or treatment of a bacterial infection.Type: ApplicationFiled: February 20, 2009Publication date: December 30, 2010Applicant: Actelion Pharmaceuticals Ltd.Inventors: Christian Hubschwerlen, Georg Rueedi, John-Philippe Surivet, Cornelia Zumbrunn-Acklin
-
Publication number: 20100324030Abstract: The present invention describes novel anti-bacterial compounds of the formula (I). These compounds are, amongst others, of interest as inhibitors of DNA gyrase and topoisomerases, for example of topoisomerase II and IV.Type: ApplicationFiled: April 11, 2008Publication date: December 23, 2010Applicant: Morphochem Aktiengesellschaft Fur Kombinatorische ChemieInventors: Glenn Dale, Sabine Pierau, Michael W. Cappi, Christopher Gray, Christian Hubschwerlen, Jean P. Surivet, Cornelia Zumbrunn
-
Patent number: 7820655Abstract: The invention relates to antibiotic ethanol or 1,2-ethanediol cyclohexyl derivatives of formula (I) wherein R1 represents (C1-C4)alkoxy; one or two of U, V, W and X represents) N and the remaining represent each independently CH or, in the case of V or X, may also represent CRa; Ra represents halogen; R2 represents H or OH; A represents CH2, CO, CH2CH?CH or COCH?CH; D represents a phenyl group optionally substituted one or two times by halogen atoms, or D represents a group of the formula (II) in which Q is oxygen or sulphur; and to salts of these derivatives of formula (I).Type: GrantFiled: February 14, 2007Date of Patent: October 26, 2010Assignee: Actelion Pharmaceuticals Ltd.Inventors: Christian Hubschwerlen, Jean-Philippe Surivet, Cornelia Zumbrunn Acklin
-
Patent number: 7820823Abstract: The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria.Type: GrantFiled: October 4, 2002Date of Patent: October 26, 2010Assignee: Morphochem Aktiengesellschaft Fur Kominatorische ChemiInventors: Christian Hubschwerlen, Jean-Luc Specklin
-
Publication number: 20100222302Abstract: The invention relates to novel chimeric antibiotics of formula I wherein R1 is CH2NHCOR5, heteroarylmethyl, heteroaryloxymethyl or heteroarylaminomethyl; R2 is H, OH, OSO3H, OPO3H2, OCH2OPO3H2, OCOCH2CH2COOH, OCOR6; R3 is H or halogen; R4 is (C1-C3)alkyl, (C1-C3)haloalkyl or cycloalkyl; R5 is alkyl or haloalkyl; and R6 is the residue of a naturally occurring amino acid or of dimethylaminoglycine. These chimeric compounds are useful in the manufacture of medicaments for the treatment of infections (e.g. bacterial infections).Type: ApplicationFiled: August 7, 2006Publication date: September 2, 2010Inventors: Christian Hubschwerlen, Philippe Panchaud, Christine Sigwalt, Jean-Luc Specklin
-
Publication number: 20100179135Abstract: Antibacterial compounds including 3-amino-6-(1-amino-ethyl)-tetrahydropyran derivatives are provided, and methods of treatment or prevention of bacterial infection with such compounds are provided.Type: ApplicationFiled: June 13, 2008Publication date: July 15, 2010Applicant: ACTELION PHARMACEUTICALS LTD.Inventors: Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
-
Publication number: 20100137290Abstract: The invention relates to antibacterial compounds of formula I wherein R1 is hydrogen, halogen, hydroxy, alkoxy or cyano; Y1 and Y2 each represent CH, one or two of U, V, W and X represent(s) N and the remaining each represent CH or, in the case of X, may also represent CRa, Ra being halogen, and, in the case of W, may also represent CRb, or each of U, V, W, X, Y1 and Y2 represents CH, or each of U, V, W, X and Y1 represents CH and Y2 represents N, or also one or, provided R1 is hydrogen, two of U, V, W, X, Y1 and Y2 represent(s) CRC and the remaining each represent CH, Rb being alkoxy, alkoxycarbonyl or alkoxyalkoxy and Rc being, each time it occurs, independently represents hydroxy or alkoxy; A-B-D represents a chain of 4 to 6 atoms, which 4 to 6 atoms are seleted from carbon, oxygen and nitrogen and may be substituted; E is one of the following groups: in which Z is CH or N and Q is O or S, or E is a phenyl group which is substituted once or twice in the meta and/or para position(s); and to salts ofType: ApplicationFiled: April 10, 2008Publication date: June 3, 2010Applicant: Actelion Pharmaceuticals Ltd.Inventors: Markus Gude, Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
-
Publication number: 20100069376Abstract: The invention relates to novel chimeric antibiotics of formula I wherein R1 represents OH, OPO3H2 or OCOR5; R2 represents H, OH or OPO3H2; R3 represents H or halogen; R4 is H, (C1-C3)alkyl, or cycloalkyl; R5 represents piperidin-4-yl or R5 is the residue of a naturally occurring amino acid, of the enantiomer of a naturally occurring amino acid or of dimethylaminoglycine; n is 0 or 1; and to salts (in particular pharmaceutically acceptable salts) of compounds of formula I. These chimeric compounds are useful in the manufacture of medicaments for the treatment of infections (e.g. bacterial infections).Type: ApplicationFiled: November 23, 2007Publication date: March 18, 2010Applicant: Actelion Pharmaceuticals, Ltd.Inventors: Christian Hubschwerlen, Philippe Panchaud, Jean-Luc Specklin
-
Publication number: 20100029623Abstract: The invention relates to compounds of formula (I) wherein R0 represents H or OH; R1 represents alkoxy; U and W represent N, V represents CH and R2 represents H or F, or U and V represent CH, W represents N and R2 represents H or F, or U and V represent N, W represents CH and R2 represents H, or U represents N. V represents CH, W represents CRa and R2 represents H; Ra represents CH2OH or alkoxycarbonyl; A represents the group CH?CH—B or a binuclear heterocyclic system D, B representing a mono- or di-substituted phenyl group wherein the substituents are halogen atoms and D representing one of the following groups wherein Z represents CH or N, and Q represents O or S; and to salts of such compounds. These compounds are useful as antibacterial agents.Type: ApplicationFiled: December 21, 2007Publication date: February 4, 2010Applicant: Actelion Pharmaceuticals Ltd.Inventors: Christian Hubschwerlen, Georg Rueedi, Jean-Phillippe Surivet, Cornelia Zumbrunn
-
Publication number: 20090306389Abstract: The present invention describes intermediates (ZP) for a novel and efficient synthesis of compounds in which the pharmacophores of quinolone and oxazolidinone are linked to one another by way of a chemically stable linker.Type: ApplicationFiled: June 5, 2009Publication date: December 10, 2009Applicant: Morphochem Aktiengesellschaft fur Kombinatorische ChemieInventors: Christian Hubschwerlen, Jean-Luc Specklin, Jean Phillippe Surivet, Daniel Baeschlin
-
Publication number: 20090270375Abstract: The invention relates to compounds of formula (I) wherein R1 represents H, alkyl, alkoxy, cyano or halogen; one of U and X represents CH or N and the other represents CH, or, in the case of U, may also represent CRa and, in the case of X, may also represent CRb; Ra represents halogen; Rb represents halogen or alkoxy; B represents N, D represents CH2 and A represents CH(OH)CH2 or CH2CH2, or B represents CH, D represents CH2 or O and A represents OCH2, CH2CH(OH), CH(OH)CH2, CH(OH)CH(OH), CH?CH, CH2CH2 Or NHCO, or also B represents C(OH), D represents CH2 and A represents OCH2, CH2CH(OH), CH(OH)CH2, CH(OH)CH(OH), CH?CH, CH2CH2 Or NHCO; R2 represents H, alkyl, alkenyl, hydroxyalkyl or alkoxycarbonylalkyl; and E represents naphthyl or a binuclear heterocyclic group; and to salts of such compounds. These compounds are useful as antimicrobial agents.Type: ApplicationFiled: August 29, 2007Publication date: October 29, 2009Applicant: Actelion Pharmaceuticals Ltd.Inventors: Christian Hubschwerlen, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
-
Publication number: 20090247578Abstract: The invention relates to novel chimeric antibiotics of formula I wherein R1 represents OH, OPO3H2 or OCOR5; R2 represents H, OH or OPO3H2; A represents N or CR6; R3 represents H or fluorine; R4 is H, (C1-C3) alkyl, or cycloalkyl; R5 is the residue of a naturally occurring amino acid, of the enantiomer of a naturally occurring amino acid or of dimethylaminoglycine; R6 represents H, alkoxy or halogen; and n is 0 or 1; and to salts (in particular pharmaceutically acceptable salts) of compounds of formula I. These chimeric compounds are useful in the manufacture of medicaments for the treatment of infections (e.g. bacterial infections).Type: ApplicationFiled: May 8, 2009Publication date: October 1, 2009Applicant: Actelion Pharmaceuticals Ltd.Inventors: Christian HUBSCHWERLEN, Hans Locher, Philippe Panchaud, Jean-Luc Specklin
-
Patent number: 7557214Abstract: The present invention describes intermediates (ZP) for a novel and efficient synthesis of compounds in which the pharmacophores of quinolone and oxazolidinone are linked to one another by way of a chemically stable linker.Type: GrantFiled: September 3, 2004Date of Patent: July 7, 2009Assignee: Morphochem Aktiengesellschaft für Kombinatorische ChemieInventors: Christian Hubschwerlen, Jean-Luc Specklin, Jean Phillippe Surivet, Daniel Baeschlin
-
Publication number: 20090105232Abstract: The invention relates to antibiotic cyclohexyl or piperidinyl carboximide derivatives of formula (I) wherein R1 represents hydrogen, halogen, (C1-C4)alkyl, (C1-C4)alkoxy, cyano or COOR2, R2 being (C1-C4)alkyl; one or two of U, V, W and X represent(s) N and the remaining represent each CH, or, in the case of X, may also represent CRX, RX being a halogen atom; either B represents N and A represents CH2CH2 or CH(OR3)CH2, or B represents CH or C(OR4) and A represents OCH2, CH2CH(OR5), CH(OR6)CH2, CH(OR7)CH(OR8), CH?CH or CH2CH2; each of R3, R4, R5, R6, R7, and R8 represents independently hydrogen, SO3H, PO3H2, CH2OPO3H2 or COR9, R9 being either CH2CH2COOH or such that R9—COOH is naturally occurring amino acid or dimethylaminoglycine; and to salts of such compounds of formula (I).Type: ApplicationFiled: March 22, 2007Publication date: April 23, 2009Applicant: ACTELION PHARMACEUTICALS LTD.Inventors: Christian Hubschwerlen, Jean-Philippe Surivet, Georg Rueedi, Cornelia Zumbrunn-Acklin