Patents by Inventor Leo Widler

Leo Widler 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).

  • Patent number: 9670193
    Abstract: The invention relates to novel trifluoromethyl-oxadiazole derivatives of formula (I), and pharmaceutically acceptable salts thereof, in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, pharmaceutical combinations thereof, and their use as medicaments, particularly for the treatment of neurodegeneration, muscle atrophy or diabetes/metabolic syndrome via inhibition of HDAC4.
    Type: Grant
    Filed: November 26, 2012
    Date of Patent: June 6, 2017
    Assignee: Novartis AG
    Inventors: Christina Hebach, Joerg Kallen, Joachim Nozulak, Marina Tintelnot-Blomley, Leo Widler
  • Publication number: 20140329825
    Abstract: The invention relates to novel trifluoromethyl-oxadiazole derivatives of formula (I), and pharmaceutically acceptable salts thereof, in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, pharmaceutical combinations thereof, and their use as medicaments, particularly for the treatment of neurodegeneration, muscle atrophy or diabetes/metabolic syndrome via inhibition of HDAC4.
    Type: Application
    Filed: November 26, 2012
    Publication date: November 6, 2014
    Applicant: NOVARTIS AG
    Inventors: Christina Hebach, Joerg Kallen, Joachim Nozulak, Marina Tintelnot-Blomley, Leo Widler
  • Patent number: 8569317
    Abstract: A compound of formula (1): wherein R1, R2, R3 and Y are as defined herein, or a pharmaceutically-acceptable and -cleavable ester, or acid addition salt thereof, useful for promoting the release of parathyroid hormone, e.g. for preventing or treating bone conditions which are associated with increased calcium depletion or resorption or in which stimulation of bone formation and calcium fixation in the bone is desirable.
    Type: Grant
    Filed: October 15, 2009
    Date of Patent: October 29, 2013
    Assignee: Novartis AG
    Inventors: Eva Altmann, Rene Beerli, Marc Gerspacher, Johanne Renaud, Sven Weiler, Leo Widler
  • Patent number: 8476286
    Abstract: Use of compound of formula (I), wherein, is, or, and wherein the symbols are as defined, or a pharmaceutically-acceptable and -cleavable ester, or acid addition salt thereof, for the preparation of a medicament for promoting the release of parathyroid hormone, e.g. for preventing or treating bone conditions which are associated with increased calcium depletion or resorption or in which stimulation of bone formation and calcium fixation in the bone is desirable.
    Type: Grant
    Filed: June 14, 2002
    Date of Patent: July 2, 2013
    Assignee: Novartis AG
    Inventors: René Beerli, Ruben A Tommasi, Sven Weiler, Leo Widler
  • Publication number: 20110257131
    Abstract: (Unsubstituted or substituted phenyl)-alkyl-substituted [(imidazol-1-yl)-1-hydroxy-1-phosphono-ethyl]-phosphonic, as well as methods or processes for their manufacture, their use in the manufacture of pharmaceutical formulations, their use in the treatment of diseases, methods of using them in the treatment of diseases, pharmaceutical formulations encompassing them and/or the compounds for use in the treatment of diseases, are disclosed. The compounds are able to inhibit excessive or inappropriate bone resorption. The compounds are of the formula I, wherein one of R1 and R2 are as defined in the specification, and can be in free form, in the form of an ester, and/or of a salt.
    Type: Application
    Filed: December 21, 2009
    Publication date: October 20, 2011
    Applicant: NOVARTIS AG
    Inventors: Simona Cotesta, Wolfgang Jahnke, Jean-Michel Rondeau, Sven Weiler, Leo Widler
  • Publication number: 20110224173
    Abstract: C2-C5-Alkyl-substituted [imidazol-1-yl)-1-hydroxy-1-phosphono-ethyl]-phosphonic acids, as well as methods or processes for their manufacture, their use in the manufacture of pharmaceutical formulations, their use in the treatment of diseases, methods of using them in the treatment of diseases, pharmaceutical formulations encompassing them and/or the compounds for use in the treatment of diseases, are described. The compounds are able to inhibit excessive or inappropriate bone resorption and for the treatment of other diseases which are caused by excessive prenylation of target proteins, such as Hutchinson-Gilford progeria syndrome. The compounds are of the formula I, wherein one of R1 and R2 is hydrogen and the other is C2-C5-alkyl that is branched or unbranched, and can be in free form, in the form of an ester, and/or of a salt.
    Type: Application
    Filed: May 26, 2011
    Publication date: September 15, 2011
    Applicant: NOVARTIS AG
    Inventors: Sven Weiler, Leo Widler, Jean-Michel Rondeau, Simona Cotesta, Wolfgang Jahnke
  • Patent number: 7977323
    Abstract: C2-C5-Alkyl-substituted [(imidazol-1-yl)-1-hydroxy-1-phosphono-ethyl]-phosphonic acids, as well as methods or processes for their manufacture, their use in the manufacture of pharmaceutical formulations, their use in the treatment of diseases, methods of using them in the treatment of diseases, pharmaceutical formulations encompassing them and/or the compounds for use in the treatment of diseases, are described. The compounds are able to inhibit excessive or inappropriate bone resorption and for the treatment of other diseases which are caused by excessive prenylation of target proteins, such as Hutchinson-Gilford progeria syndrome. The compounds are of the formula I, wherein one of R1 and R2 is hydrogen and the other is C2-C5-alkyl that is branched or unbranched, and can be in free form, in the form of an ester, and/or of a salt.
    Type: Grant
    Filed: November 26, 2008
    Date of Patent: July 12, 2011
    Assignee: Novartis AG
    Inventors: Sven Weiler, Leo Widler, Jean Michel Rondeau, Simona Cotesta, Wolfgang Jahnke
  • Publication number: 20100166765
    Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof, wherein the groups R2, R3, R4, Q, X and Y are as defined in the specification, is useful in the treatment of bone conditions related to increased calcium depletion or resorption.
    Type: Application
    Filed: August 14, 2006
    Publication date: July 1, 2010
    Inventors: Sandra Ammon, Rene Beerli, Leo Widler
  • Publication number: 20100099670
    Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof: wherein R is as defined in the specification.
    Type: Application
    Filed: January 21, 2008
    Publication date: April 22, 2010
    Inventor: Leo Widler
  • Patent number: 7696216
    Abstract: A compound of formula (I): wherein R1, R2, R3 and Y are as defined herein, or a pharmaceutically-acceptable and -cleavable ester, or acid addition salt thereof, useful for promoting the release of parathyroid hormone, e.g. for preventing or treating bone conditions which are associated with increased calcium depletion or resorption or in which stimulation of bone formation and calcium fixation in the bone is desirable.
    Type: Grant
    Filed: December 22, 2003
    Date of Patent: April 13, 2010
    Assignee: Novartis AG
    Inventors: Eva Altmann, Rene Beerli, Marc Gerspacher, Johanne Renaud, Sven Weiler, Leo Widler
  • Publication number: 20100063075
    Abstract: A compound of formula (1): wherein R1, R2, R3 and Y are as defined herein, or a pharmaceutically-acceptable and -cleavable ester, or acid addition salt thereof, useful for promoting the release of parathyroid hormone, e.g. for preventing or treating bone conditions which are associated with increased calcium depletion or resorption or in which stimulation of bone formation and calcium fixation in the bone is desirable.
    Type: Application
    Filed: October 15, 2009
    Publication date: March 11, 2010
    Inventors: Eva Altmann, Rene Beerli, Marc Gerspacher, Johanne Renaud, Sven Weiler, Leo Widler
  • Publication number: 20100022565
    Abstract: Provided is a pharmaceutical composition comprising a calcilytic agent which, when administered orally to a subject induces a rapid and short-lasting absorption of the calcilytic agent and/or a rapid and short-lasting release of the parathyroid hormone.
    Type: Application
    Filed: February 29, 2008
    Publication date: January 28, 2010
    Inventors: Thomas Buhl, Elisabete Goncalves, Oskar Kalb, Lorenz Meinel, Sibylle Reidemeister, Agnes Taillardat, Leo Widler
  • Publication number: 20090143337
    Abstract: C2-C5-Alkyl-substituted [(imidazol-1-yl)-1-hydroxy-1-phosphono-ethyl]-phosphonic acids, as well as methods or processes for their manufacture, their use in the manufacture of pharmaceutical formulations, their use in the treatment of diseases, methods of using them in the treatment of diseases, pharmaceutical formulations encompassing them and/or the compounds for use in the treatment of diseases, are described. The compounds are able to inhibit excessive or inappropriate bone resorption and for the treatment of other diseases which are caused by excessive prenylation of target proteins, such as Hutchinson-Gilford progeria syndrome. The compounds are of the formula I, wherein one of R1 and R2 is hydrogen and the other is C2-C5-alkyl that is branched or unbranched, and can be in free form, in the form of an ester, and/or of a salt.
    Type: Application
    Filed: November 26, 2008
    Publication date: June 4, 2009
    Applicant: NOVARTIS AG
    Inventors: Sven Weiler, Leo Widler, Jean-Michel Rondeau, Simona Cotesta, Wolfgang Jahnke
  • Publication number: 20060079685
    Abstract: A compound of formula (I): wherein R1, R2, R3 and Y are as defined herein, or a pharmaceutically-acceptable and -cleavable ester, or acid addition salt thereof, useful for promoting the release of parathyroid hormone, e.g. for preventing or treating bone conditions which are associated with increased calcium depletion or resorption or in which stimulation of bone formation and calcium fixation in the bone is desirable.
    Type: Application
    Filed: December 22, 2003
    Publication date: April 13, 2006
    Inventors: Eva Altmann, Rene Beerli, Marc Gerspacher, Johanne Renaud, Sven Weiler, Leo Widler
  • Publication number: 20040180912
    Abstract: Use of compound of formula (I), wherein, is, or, and wherein the symbols are as defined, or a pharmaceutically-acceptable and-cleavable ester, or acid addition salt thereof, for the preparation of a medicament for promoting the release of parathyroid hormone, e.g. for preventing or treating bone conditions which are associated with increased calcium depletion or resorption or in which stimulation of bone formation and calcium fixation in the bone is desirable.
    Type: Application
    Filed: December 12, 2003
    Publication date: September 16, 2004
    Inventors: Rene Beerli, Ruben Alberto Tommasi, Sven Weiler, Leo Widler
  • Patent number: 5229405
    Abstract: Compounds of the formula I ##STR1## in which R.sub.1 is lower alk-2-en-1-yl, lower alk-3-en-2-yl, lower alk-2-yn-1-yl or lower alkyl substituted in the 2,3-position by radicals which can be eliminated to give a double bond, R.sub.2 is hydrogen and R.sub.3 is methyl which is unsubstituted or substituted by radicals which can be eliminated together with hydrogen R.sub.2 to give a double bond or R.sub.2 and R.sub.3 are both hydrogen or lower alkyl or are together methylene and R.sub.4 is a group of the formula Ia, Ib or Ic ##STR2## in which R.sub.5 is hydrogen, lower alkyl, lower alk-2-en-1-yl or lower alk-2-yn-1-yl and R.sub.6 is a group of the formula Id or Ie ##STR3## in which R.sub.1, R.sub.2, R.sub.3 and R.sub.5 are as defined, and their pharmaceutically acceptable salts can be used in a novel manner for the treatment of diseases of the rheumatoid type.
    Type: Grant
    Filed: April 10, 1992
    Date of Patent: July 20, 1993
    Assignee: Ciba-Geigy Corporation
    Inventors: Ulrich Feige, Irmgard Wiesenberg, Leo Widler, Pier G. Ferrini, Martin Missbach
  • Patent number: 5177091
    Abstract: Compounds of formula I ##STR1## wherein X and Y are each independently of the other thio or sulfynyl, R.sub.1 is lower alk-2-en-1-yl, lower alk-3-en-2-yl, lower alk-2--yn-1-yl, or lower alkyl that is substituted in the 2,3-position by radicals that can be eliminated to form a double bond, R.sub.2 is hydrogen and R.sub.3 is unsubstituted methyl or methyl substituted by a radical that can be eliminated together with hydrogen Rhd 2 to form a double bond, or R.sub.2 and R.sub.3 are each hydrogen or lower alkyl or together are methylene, R.sub.4 is free or protected hydroxy, or hydrogen, and R.sub.5 is hydrogen, lower alkyl, lower alk-2-en-1-yl, lower alk-2-yn-1-yl, or lower alkyl that is substituted in the 2,3-position by radicals that can be eliminated to form a double bond, and their pharmaceutically acceptable salts may be used in a novel manner for the treatment of disorders of the rheumatoid type.
    Type: Grant
    Filed: November 20, 1991
    Date of Patent: January 5, 1993
    Assignee: Ciba-Geigy Corporation
    Inventors: Ulrich Feige, Irmgard Wiesenberg, Leo Widler, Pier G. Ferrini, Martin Missbach
  • Patent number: 5057505
    Abstract: Heteroarylaminomethanediphosphonic acids of the formula ##STR1## in which R.sub.1 represents an optionally benzo- or cyclohexeno-fused 5-membered heteroaryl radical that contains, as hetero atom(s), either from 2 to 4 N-atoms or 1 or 2 N-atoms as well as 1 O-atom or S-atom and that is unsubstituted or is substituted by lower alkyl; by phenyl that is unsubstituted or is substituted by lower alkyl, lower alkoxy and/or by halogen; by lower alkoxy; by hydroxy; by di-lower alkylamino; by lower alkylthio and/or by halogen; and R.sub.2 represents hydrogen or lower alkyl, and their salts, have a regulatory action on the calcium metabolism and can be used as active ingredients in medicaments for the treatment of illnesses that can be attributed to disorders of the calcium metabolism. They are manufactured, for example, as follows: in a compound of the formula ##STR2## in which X.sub.1 represents a functionally modified phosphono group X and X.sub.
    Type: Grant
    Filed: May 19, 1989
    Date of Patent: October 15, 1991
    Assignee: Ciba-Geigy Corporation
    Inventors: Leo Widler, Knut Jaeggi
  • Patent number: 4939130
    Abstract: Alkanediphosphonic acids, in particular heteroarylalkanediphosphonic acids of formula ##STR1## wherein R.sub.1 is a 5-membered heteroaryl radical which may be fused with benzene or cyclohexene nuclei and which contains, as hetero atoms, 2 to 4 N-atoms or 1 or 2 N-atoms as well as 1 O- or S-atom, and which is unsubstituted or C-substituted by lower alkyl, phenyl or phenyl which is substituted by lower alkyl, lower alkoxy and/or halogen, or by lower alkoxy, hydroxy, di-lower alkylamino, lower alkylthio and/or halogen, and/or is N-substituted at a N-atom which is capable of substitution by lower alkyl, lower alkoxy and/or halogen, and R.sub.2 is hydrogen, hydroxy, amino, lower alkylthio or halogen, and salts thereof, have regulatory action on calcium metabolism and can be used as medicaments for the treatment of diseases associated with impairment of calcium metabolism. The compounds are obtained for example by converting, in a compound of formula ##STR2## wherein X.sub.
    Type: Grant
    Filed: February 27, 1989
    Date of Patent: July 3, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Knut A. Jaeggi, Leo Widler