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).
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Patent number: 9670193Abstract: 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: GrantFiled: November 26, 2012Date of Patent: June 6, 2017Assignee: Novartis AGInventors: Christina Hebach, Joerg Kallen, Joachim Nozulak, Marina Tintelnot-Blomley, Leo Widler
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Publication number: 20140329825Abstract: 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: ApplicationFiled: November 26, 2012Publication date: November 6, 2014Applicant: NOVARTIS AGInventors: Christina Hebach, Joerg Kallen, Joachim Nozulak, Marina Tintelnot-Blomley, Leo Widler
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Patent number: 8569317Abstract: 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: GrantFiled: October 15, 2009Date of Patent: October 29, 2013Assignee: Novartis AGInventors: Eva Altmann, Rene Beerli, Marc Gerspacher, Johanne Renaud, Sven Weiler, Leo Widler
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Patent number: 8476286Abstract: 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: GrantFiled: June 14, 2002Date of Patent: July 2, 2013Assignee: Novartis AGInventors: René Beerli, Ruben A Tommasi, Sven Weiler, Leo Widler
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Publication number: 20110257131Abstract: (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: ApplicationFiled: December 21, 2009Publication date: October 20, 2011Applicant: NOVARTIS AGInventors: Simona Cotesta, Wolfgang Jahnke, Jean-Michel Rondeau, Sven Weiler, Leo Widler
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Publication number: 20110224173Abstract: 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: ApplicationFiled: May 26, 2011Publication date: September 15, 2011Applicant: NOVARTIS AGInventors: Sven Weiler, Leo Widler, Jean-Michel Rondeau, Simona Cotesta, Wolfgang Jahnke
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Patent number: 7977323Abstract: 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: GrantFiled: November 26, 2008Date of Patent: July 12, 2011Assignee: Novartis AGInventors: Sven Weiler, Leo Widler, Jean Michel Rondeau, Simona Cotesta, Wolfgang Jahnke
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Publication number: 20100166765Abstract: 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: ApplicationFiled: August 14, 2006Publication date: July 1, 2010Inventors: Sandra Ammon, Rene Beerli, Leo Widler
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Publication number: 20100099670Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof: wherein R is as defined in the specification.Type: ApplicationFiled: January 21, 2008Publication date: April 22, 2010Inventor: Leo Widler
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Patent number: 7696216Abstract: 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: GrantFiled: December 22, 2003Date of Patent: April 13, 2010Assignee: Novartis AGInventors: Eva Altmann, Rene Beerli, Marc Gerspacher, Johanne Renaud, Sven Weiler, Leo Widler
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Publication number: 20100063075Abstract: 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: ApplicationFiled: October 15, 2009Publication date: March 11, 2010Inventors: Eva Altmann, Rene Beerli, Marc Gerspacher, Johanne Renaud, Sven Weiler, Leo Widler
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Publication number: 20100022565Abstract: 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: ApplicationFiled: February 29, 2008Publication date: January 28, 2010Inventors: Thomas Buhl, Elisabete Goncalves, Oskar Kalb, Lorenz Meinel, Sibylle Reidemeister, Agnes Taillardat, Leo Widler
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Publication number: 20090143337Abstract: 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: ApplicationFiled: November 26, 2008Publication date: June 4, 2009Applicant: NOVARTIS AGInventors: Sven Weiler, Leo Widler, Jean-Michel Rondeau, Simona Cotesta, Wolfgang Jahnke
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Publication number: 20060079685Abstract: 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: ApplicationFiled: December 22, 2003Publication date: April 13, 2006Inventors: Eva Altmann, Rene Beerli, Marc Gerspacher, Johanne Renaud, Sven Weiler, Leo Widler
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Publication number: 20040180912Abstract: 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: ApplicationFiled: December 12, 2003Publication date: September 16, 2004Inventors: Rene Beerli, Ruben Alberto Tommasi, Sven Weiler, Leo Widler
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Patent number: 5229405Abstract: 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: GrantFiled: April 10, 1992Date of Patent: July 20, 1993Assignee: Ciba-Geigy CorporationInventors: Ulrich Feige, Irmgard Wiesenberg, Leo Widler, Pier G. Ferrini, Martin Missbach
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Patent number: 5177091Abstract: 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: GrantFiled: November 20, 1991Date of Patent: January 5, 1993Assignee: Ciba-Geigy CorporationInventors: Ulrich Feige, Irmgard Wiesenberg, Leo Widler, Pier G. Ferrini, Martin Missbach
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Patent number: 5057505Abstract: 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: GrantFiled: May 19, 1989Date of Patent: October 15, 1991Assignee: Ciba-Geigy CorporationInventors: Leo Widler, Knut Jaeggi
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Patent number: 4939130Abstract: 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: GrantFiled: February 27, 1989Date of Patent: July 3, 1990Assignee: Ciba-Geigy CorporationInventors: Knut A. Jaeggi, Leo Widler