Patents by Inventor Ulrich Widmer
Ulrich Widmer 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: 6605723Abstract: The present invention relates to a new process for the preparation of compounds of the formulae and their pharmaceutically acceptable acid addition salts, which are NMDA (N-methyl-D-aspartate)-receptor-subtype selective blockers.Type: GrantFiled: March 15, 2001Date of Patent: August 12, 2003Assignee: Hoffman-La Roche Inc.Inventors: Yvo Crameri, Michelangelo Scalone, Pius Waldmeier, Ulrich Widmer
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Publication number: 20010037026Abstract: The present invention relates to a new process for the preparation of compounds of the formulae 1Type: ApplicationFiled: March 15, 2001Publication date: November 1, 2001Inventors: Yvo Crameri, Michelangelo Scalone, Pius Waldmeier, Ulrich Widmer
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Patent number: 5665718Abstract: The invention relates to compounds of the formula ##STR1## wherein A together with the two carbon atoms denoted by .alpha. and .beta. is one of the residues ##STR2## Q is one of the residues ##STR3## R.sup.1 and R.sup.2 each independently are hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower hydroxyalkyl, lower alkoxy-lower alkyl, (C.sub.3 -C.sub.6)-cycloalkyl, (C.sub.3 -C.sub.6)-cycloalkyl-lower alkyl, amino-lower alkyl, lower alkylamino-lower alkyl, di-lower alkylamino-lower alkyl or aryl-lower alkyl or together with the nitrogen atom are a 5- to 8-membered membered heterocycle optionally containing a further hetero atom or a fused benzene ring,R.sup.3 is hydrogen and R.sup.4 is lower alkyl or R.sup.3 and R.sup.4 together are dimethylene or trimethylene andR.sup.5 and R.sup.6 each independently are hydrogen, halogen, trifluoromethyl, lower alkoxy or nitro,the compounds of formula I having the (S) configuration with reference to the carbon atom denoted by .gamma. when R.sup.3 and R.sup.Type: GrantFiled: January 16, 1996Date of Patent: September 9, 1997Assignee: Hoffmann-La Roche Inc.Inventors: Thierry Godel, Walter Hunkeler, Heinz Stadler, Ulrich Widmer
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Patent number: 5646173Abstract: The invention relates to tricyclic pyrrole derivatives useful as 5-HT selective agents of the formula ##STR1## wherein R.sup.1 to R.sup.4 are, independently, hydrogen, halogen, lower alkyl, phenyl, cycloalkyl or lower alkoxy and R.sup.2 additionally is lower alkoxycarbonyl, acyloxy or mesyloxy;R.sup.5 to R.sup.7 are, independently, hydrogen or lower alkyl;X is --CH.sub.2 CH(C.sub.6 H.sub.5)--, --CH.dbd.C(C.sub.6 H.sub.5)--, --YCH.sub.2 --, --CH.dbd.CH-- or --(CR.sup.11 R.sup.12).sub.n ;R.sup.11 and R.sup.12 are, independently, hydrogen, phenyl, lower alkyl or halogen;n is 1 to 3 andy is O or S,as well as pharmaceutically acceptable salts of basic compounds of formula I with pharmaceutically acceptable acids.Type: GrantFiled: February 21, 1996Date of Patent: July 8, 1997Assignee: Hoffmann-La Roche Inc.Inventors: Michael Bos, Jurgen Wichmann, Ulrich Widmer
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Patent number: 5362738Abstract: The pyridone derivatives of the formula ##STR1## wherein Ra is hydrogen or halogen, Rb is --OR.sup.1 or --NR.sup.2 R.sup.3 ; R.sup.1 is an unsubstituted lower alkyl or a lower alkyl substituted by hydroxy, lower alkoxy, amino, lower alkylamino, di(lower alkyl)amino, di(lower alkyl)carbamoyl or lower alkoxycarbonylamino; R.sup.2 is hydrogen or a lower alkyl group which is unsubstituted or substituted by hydroxy, lower alkoxy, amino, lower alkylamino, di(lower alkyl)-amino, di(lower alkyl)carbamoyl or lower alkoxycarbonyl-amino; and R.sup.3 is hydrogen or lower alkyl optionally unsubstituted or mono- or disubstituted by lower alkyl, hydroxy, lower alkoxy, lower hydroxyalkyl, lower alkoxyalkyl or phenyl; B and the carbon atom denoted by .alpha. taken together is a group of the formula >C.sub..alpha. --CR.sup.4 .dbd.CH--CH.dbd.CH-- and R.sup.4 is hydrogen, fluorine or chlorine, that can be used for the control or treatment of muscle tension, stress, insomnia, anxiety and/or convulsions.Type: GrantFiled: June 1, 1993Date of Patent: November 8, 1994Assignee: Hoffmann-La Roche Inc.Inventors: Serge Burner, Ulrich Widmer
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Patent number: 5326769Abstract: The compound (S)-1-[(10-chloro-6,7-dihydro-4-oxo-3-phenyl-4H-benzo[a]quino-lizin-1-yl)c arbonyl]-3-ethoxypyrrolidine of the formula ##STR1## which has valuable pharmacological properties, is described. In particular, the compound of formula I has a non-sedating, hypnotic, that is, sleep-promoting, activity and can accordingly be used for the treatment of sleep disorders.Type: GrantFiled: March 24, 1993Date of Patent: July 5, 1994Assignee: Hoffmann-La Roche Inc.Inventors: Richard R. Scherschlicht, Ulrich Widmer
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Patent number: 5321021Abstract: The compounds are of the class of bi- and tricyclic pyridone derivatives of the formula ##STR1## wherein various substituents are as described in the specification, useful in the control of prevention of muscle tensions, stress conditions, insomnia, anxiety states and/or convulsions.Type: GrantFiled: April 24, 1991Date of Patent: June 14, 1994Assignee: Hoffmann-La Roche Inc.Inventors: Ulf Fischer, Fernand Schneider, Ulrich Widmer
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Patent number: 5281711Abstract: The compound (S)-1-[(10-chloro-6,7-dihydro-4-oxo-3-phenyl-4H-benzo[a]quino-lizin-1-yl)c arbonyl]-3-ethoxypyrrolidine of the formula ##STR1## which has valuable pharmacological properties, is described. In particular, the compound of formula I has a non-sedating, hypnotic, that is, sleep-promoting, activity and can accordingly be used for the treatment of sleep disorders.Type: GrantFiled: January 6, 1992Date of Patent: January 25, 1994Assignee: Hoffmann-La Roche Inc.Inventors: Richard R. Scherschlicht, Ulrich Widmer
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Patent number: 5258387Abstract: The novel pyridone derivatives of the formula ##STR1## wherein Ra is hydrogen or halogen, Rb is --OR.sup.1 or --NR.sup.2 R.sup.3 ; R.sup.1 is an unsubstituted lower alkyl or a lower alkyl substituted by hydroxy, lower alkoxy, amino, lower alkylamino, di(lower alkyl)amino, di(lower alkyl)carbamoyl or lower alkoxycarbonylamino; R.sup.2 is hydrogen or a lower alkyl group which is unsubstituted or substituted by hydroxy, lower alkoxy, amino, lower alkylamino, di(lower alkyl)-amino, di(lower alkyl)carbamoyl or lower alkoxycarbonyl-amino; and R.sup.3 is hydrogen or lower alkyl or R.sup.2 and R.sup.3 taken together with the nitrogen atom to which they are attached is a 1-azetidinyl, 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, 4-thiomorpholinyl or 1-piperazinyl which is unsubstituted or mono- or disubstituted by lower alkyl, hydroxy, lower alkoxy, lower hydroxyalkyl, lower alkoxyalkyl or phenyl; B and the carbon atom denoted by a taken together is a group of the formula >C.sub..alpha. --S--CH.dbd.CH-- or >C.Type: GrantFiled: May 26, 1992Date of Patent: November 2, 1993Assignee: Hoffmann-La Roche Inc.Inventors: Serge Burner, Ulrich Widmer
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Patent number: 5246960Abstract: Racemic compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and n are as described herein, enantiomers and diastereomers thereof, and salts of these esters with weak acids, are described. These compounds inhibit pancreas lipase and are useful agents in the treatment of obesity, hyperlipaemia, atherosclerosis and arteriosclerosis.Type: GrantFiled: September 14, 1992Date of Patent: September 21, 1993Assignee: Hoffmann-La Roche Inc.Inventors: Pierre Barbier, Fernand Schneider, Ulrich Widmer
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Patent number: 5175186Abstract: Compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 independently C.sub.1-17 -alkyl which is saturated or optionally interrupted by up to 8 double or triple bonds and/or optionally interrupted by an O or S atom, which is present in other than the .alpha.-position to an unsaturated C atom; or phenyl, benzyl or --C.sub.6 H.sub.4 --X--C.sub.6 H.sub.5 ring-substituted by 0 to 3 C.sub.1-6 -alkyl-(O or S).sub.1 or 0 groups, and X is oxygen, sulfur or (CH.sub.2).sub.0-3, with the proviso that when R.sup.1 is n-hexyl and R.sup.2 is undecyl or 2Z,5Z-undecadienyl, at least one of the asymmetric C-atoms present in the oxetanone ring and in the .beta.-position to the latter has the R-configuration, an enantiomer or a diastereomer thereof are described. These compounds inhibit pancreas lipase and are useful agents in the treatment of obesity, hyperlipemia, atherosclerosis and arteriosclerosis.Type: GrantFiled: March 19, 1990Date of Patent: December 29, 1992Assignee: Hoffmann-La Roche Inc.Inventors: Pierre Barbier, Fernand Schneider, Ulrich Widmer
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Patent number: 5143912Abstract: The novel pyridone derivatives of the formula ##STR1## wherein Ra is hydrogen or halogen, Rb is --NR.sup.2 R.sup.3 wherein R.sup.2 and R.sup.3 taken together with the nitrogen atom to which they are attached is a 1-azetidinyl, 1-pyrrolidinyl, 1-piperidinyl which is unsubstituted or mono- or disubstituted by lower alkyl, hydroxy, lower alkoxy, lower hydroxyalkyl, lower alkoxyalkyl or phenyl; B and the carbon atom denoted by .alpha. taken together is a group of the formula >C.sub..alpha. --CR.sup.4 .dbd.CH--CH.dbd.CH-- and R.sup.4 is hydrogen, fluorine or chlorine, can be used for the control or prevention of illnesses. In particular, they have muscle relaxant, sedative-hypnotic, anxiolytic and/or anticonvulsive activity and can accordingly be used in the control or prevention of muscle tensions, stress conditions, insomnia, anxiety states and/or convulsions.Type: GrantFiled: August 2, 1991Date of Patent: September 1, 1992Assignee: Hoffmann-La Roche, Inc.Inventors: Serge Burner, Ulrich Widmer
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Patent number: 5114934Abstract: The compounds of the formula ##STR1## wherein R.sub.a, R.sub.b, R.sub.c, R.sub.d are defined in the specification and pharmaceutically acceptable addition salts are disclosed. The compounds of formula I have valuable pharmacological properties and can be used for the control of prevention of illnesses. In particular, they have muscle relaxant, seditive-hypnotic, anxiolytic and/or anticonvulsive activity and can accordingly be used in the control or prevention of muscle tensions, stress conditions, isomnia, anxiety states and/or convulsions.Type: GrantFiled: June 1, 1989Date of Patent: May 19, 1992Assignee: Hoffman-La Roche, Inc.Inventors: Ulf Fischer, Fernand Schneider, Ulrich Widmer
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Patent number: 5082842Abstract: The compounds of the formula ##STR1## wherein Ra, Rb, Rc, Rd, Re and Rf are defined in the specification, and the pharmaceutically acceptable acid addition salts of compounds of formula A which have one or more basic substituents are described. The compounds of formula A have valuable pharmacological properties and can be used for the control or prevention of illnesses. In particular, they have muscle relaxant, sedative-hypnotic, anxiolytic and/or anticonvulsive activity and can accordingly be used in the control or prevention of muscle tensions, stress conditions, insomnia, anxiety states and/or convulsions.Type: GrantFiled: October 16, 1989Date of Patent: January 21, 1992Assignee: Hoffmann-La Roche Inc.Inventor: Ulrich Widmer
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Patent number: 5036066Abstract: The compounds are of the class of bi- and tricyclic pyridone derivatives of the formula ##STR1## wherein the various substituent are as described in the specification, useful in the control of prevention of muscle tensions stress conditions, insomnia, anxiety states and/or convulsions.Type: GrantFiled: October 16, 1989Date of Patent: July 30, 1991Assignee: Hoffmann-La Roche Inc.Inventors: Ulf Fischer, Fernand Schneider, Ulrich Widmer
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Patent number: 4983746Abstract: The invention is directed to a process for the manufacture of pancreatic lipase-inhibiting oxetanone ethyl esters of the formula ##STR1## wherein X is undecyl or 2Z,5Z-undecadienyl; C.sub.6 is n-hexyl; Y is isobutyl and Z is formyl or Y is carbamoylmethyl and Z is acetyl;which process comprises esterifying the corresponding oxetanone ethanols, or hydrogenating the 3-undecenyl group in corresponding oxetanone ethyl ester starting materials to the undecyl group X, or N-formylating or N-acetylating corresponding primary amines.Type: GrantFiled: August 8, 1989Date of Patent: January 8, 1991Assignee: Hoffmann-La Roche Inc.Inventors: Pierre Barbier, Fernand Schneider, Ulrich Widmer
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Patent number: 4931463Abstract: Racemic compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and n are as described herein, enantiomers and diastereomers thereof, and salts of these esters with weak acids, are described. These compounds inhibit pancreas lipase and are useful agents in the treatment of obesity, hyperlipaemia, atherosclerosis and arteriosclerosis.Type: GrantFiled: December 17, 1987Date of Patent: June 5, 1990Assignee: Hoffmann-La Roche Inc.Inventors: Pierre Barbier, Fernand Schneider, Ulrich Widmer
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Patent number: 4889848Abstract: Compounds of the formula ##STR1## wherein Q.sup.1 and the nitrogen atom taken together are a group of the formula >N--CH.sub.2 CH.sub.2 -- (a), >N--CH.sub.2 CH.sub.2 CH.sub.2 -- (b), >N--CH.dbd.CH-- (c), >N--CH.sub.2 --CH.dbd.CH-- (d), >N--CH.sub.2 --S(O).sub.p -- (e), >N--CH.sub.2 CH.sub.2 --S(O).sub.p -- (f) or >N--CH.dbd.CH--S(O).sub.p -- (g), p is the integer 0, 1 or 2, Ra is a phenyl, pyridyl or thienyl group which is optionally substituted by halogen, trifluoromethyl, nitro, lower alkyl or lower alkoxy, Rb and Rc each, independently, are hydrogen, halogen, trifluoromethyl, lower alkyl, lower alkoxy or nitro and the dotted line signifies an optional bond, or Rb and Rc together with the carbon atom denoted by .alpha. are a group of the formula >C.alpha.--S--CH.dbd.CH-- (h), >C.alpha.--CH.dbd.CH--S-- (i) or >C.alpha.--CH.dbd.CH--CH.dbd.Type: GrantFiled: January 5, 1988Date of Patent: December 26, 1989Assignee: Hoffmann-La Roche Inc.Inventors: Ulf Fischer, Fernand Schneider, Ulrich Widmer
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Patent number: 4889854Abstract: The compounds of the formula ##STR1## wherein Ra, Rb, Rc, Rd, Re and Rf are as hereinafter described, compounds of formula A which have one or more basic substituents are described and have valuable pharmacological properties. In particular, they have muscle relaxant, sedative-hypnotic, anxiolytic and/or anticonvulsive activity and can be used for the control or prevention of muscle tensions, stress conditions, insomnia, anxiety states and/or convulsions.Type: GrantFiled: May 25, 1988Date of Patent: December 26, 1989Assignee: Hoffman-La Roche Inc.Inventor: Ulrich Widmer
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Patent number: 4735940Abstract: Compounds of the formula ##STR1## or a pharmaceutically acceptable acid addition salt of a compound of formula I which has one or more basic substituents, are described.The compounds of formula I possess pronounced muscle relaxant, sedative-hypnotic, anticonvulsive and anxiolytic properties and have low toxicity.Type: GrantFiled: October 31, 1985Date of Patent: April 5, 1988Assignee: Hoffmann-La Roche Inc.Inventors: Ulf Fischer, Fernand Schneider, Ulrich Widmer