Patents by Inventor Herbert Leinert
Herbert Leinert 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: 6716845Abstract: The present invention pertains to derivatives of 5,5-disubstituted pyrimidine-2,4,6,-trianones having the formula: wherein R1, R2, R3, and R4 are described herein. These compounds have antitumor and antimetastatic activity.Type: GrantFiled: February 25, 2002Date of Patent: April 6, 2004Assignee: Hoffmann-La Roche Inc.Inventors: Dagmar Geppert, Frank Grams, Hans-Willi Krell, Herbert Leinert, Ernesto Menta, Gerd Zimmermann
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Patent number: 6576628Abstract: The invention relates to inhibitors of matrix metalloproteases, more specifically a 3-aryl-succinamido-hydroxamic acid of formula (I) and its salt, ester and derivative thereof, along with methods of producing a compound of formula (I) and pharmaceutical compositions thereof.Type: GrantFiled: July 6, 2000Date of Patent: June 10, 2003Assignee: Roche Diagnostics GmbHInventors: Frank Grams, Gerd Zimmermann, Hans-Willi Krell, Ernesto Menta, Herbert Leinert
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Patent number: 6498252Abstract: Compounds of formula I in which R1 represents a substituted or unsubstituted phenoxy, phenylthio, phenylsulfinyl, phenylsulfonyl, phenylamino or phenylmethyl residue, and R2 represents an optionally substituted aryl or heteroaryl residue, with metallo-proteinase inhibitor activity.Type: GrantFiled: September 29, 2000Date of Patent: December 24, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Frank Grams, Hans-Willi Krell, Herbert Leinert, Ernesto Menta, Gerd Zimmermann
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Publication number: 20020187991Abstract: Derivatives of 5,5-disubstituted pyrimidine-2,4,6-trianones are disclosed. These compounds have antitumor and antimetastatic activity.Type: ApplicationFiled: February 25, 2002Publication date: December 12, 2002Inventors: Dagmar Geppert, Frank Grams, Hans-Willi Krell, Herbert Leinert, Ernesto Menta, Gerd Zimmermann
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Patent number: 6121322Abstract: The invention provides novel azulene derivatives of general formula I ##STR1## wherein R.sub.1 to R.sub.6 have the significance given in the description, as well as their tautomers, enantiomers, diastereomers, racemates and physiologically compatible salts or esters and substances which are hydrolyzed or metabolized in vivo to compounds of formula I.The invention is also concerned with a process and intermediates for the manufacture of the above compounds, pharmaceutical compositions which contain such compounds as well as the use of these compounds in the treatment of inflammatory conditions.Type: GrantFiled: November 24, 1998Date of Patent: September 19, 2000Assignee: Boehringer Mannheim GmbHInventors: Joachim Dickhaut, Walter-Gunar Friebe, Frank Grams, Rainer Haag, Herbert Leinert
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Patent number: 6037334Abstract: Compounds of formula I ##STR1## in which R.sub.1, R.sup.2 are the same or different and denote a hydrogen atom, an alkyl group, a cycloalkyl group, a hydroxyalkyl group, an alkenyl group, an alkinyl group or an aralkyl group or R.sup.1 and R.sup.2 together denote an alkylene residue which, together with the bound oxygen atoms and the phosphorus atom carrying the oxygen atoms, forms a saturated 5-membered to 8-membered ring;R.sup.3 denotes an optionally substituted amino group, an alkyl group, a cycloalkyl residue or an optionally substituted aryl residue;n denotes an integer between 1 and 4,as well as hydrates, solvates and physiologically tolerated salts thereof, their optically active forms, processes for their production as well as pharmaceutical preparations having factor Xa-inhibitory properties which contain these compounds.Type: GrantFiled: July 15, 1999Date of Patent: March 14, 2000Assignee: Roche Diagnostics GmbHInventors: Ralf Kucznierz, Herbert Leinert, Wolfgang von der Saal, Richard Neidlein, Christiane Kehr
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Patent number: 5824679Abstract: The invention concerns novel phosphanoxides of formula 1 in which R.sup.1 means aryl or heteroaryl group. The invention further concern the optically active forms, racemates and diastereomers mixtures of these compounds, a method of preparing them and pharmaceutical compositions containing these compounds, and methods of use to produce a thrombin-inhibiting effect.Type: GrantFiled: February 28, 1997Date of Patent: October 20, 1998Assignee: Boehringer Mannheim GmbHInventors: Wolfgang Von Der Saal, Herbert Leinert, Karlheinz Stegmeier
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Patent number: 5795892Abstract: The invention concerns new 4-aminopyridazines of the general formula I ##STR1## in which R.sup.1 denotes an R.sup.2 --SO.sub.2 --O-- or R.sup.2 --SO.sub.2 --NR.sup.3 -- group in whichR.sup.2 denotes a cycloalkyl residue, an unsubstituted or substituted aryl or heteroaryl residue,R.sup.3 denotes a hydrogen atom, an alkyl or alkyloxyalkyl group which can be unsubstituted or substituted once or several times by hydroxy groups wherein the hydroxy groups can be substituted by alkyl, hydroxyalkyl, alkyloxyalkyl, hydroxyalkyloxyalkyl or alkylcarbonyl groups and wherein in each case two vicinal hydroxy groups can be linked together by alkylidene groups,as well as hydrates, solvates and physiologically tolerated salts thereof. The invention also concerns the optically active forms, racemates and mixtures of diastereomers of these compounds, processes for their production and pharmaceutical agents containing these compounds having a thrombin-inhibiting action.Type: GrantFiled: February 28, 1997Date of Patent: August 18, 1998Assignee: Boehringer Manneim GmbHInventors: Wolfgang Von Der Saal, Reinhard Heck, Ralf Kucznierz, Herbert Leinert, Karlheinz Stegmeier
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Patent number: 5756711Abstract: Compounds of the formula I ##STR1## in which R.sub.1 and R.sub.2 represent a possibly substituted C.sub.8 -C.sub.15 -alkyl chain, n the number 0, 1 or 2 and A the residue of a nucleoside, processes for their preparation, as well as antiviral medicaments which contain these compounds.Type: GrantFiled: June 10, 1996Date of Patent: May 26, 1998Assignee: Boehringer Mannheim GmbHInventors: Harald Zilch, Herbert Leinert, Alfred Mertens, Dieter Herrmann
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Patent number: 5563257Abstract: Liponucleotides containing an ether linkage in the 2-position and a thioether, sulfoxide, or sulfone linkage in the 3-position. The nucleoside component of said liponucleotide is AZT or 3'-deoxy-3'-fluorothymidine. These compounds exhibit antiviral activity.Type: GrantFiled: May 9, 1995Date of Patent: October 8, 1996Assignee: Boehringer Mannheim GmbHInventors: Harald Zilch, Herbert Leinert, Alfred Mertens, Dieter Herrmann
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Patent number: 5512564Abstract: The present invention concerns thiazolo- 2,3-a!pyrrole and oxazolo- 1,2-a!pyrrole derivatives of formula I ##STR1## in which HET represents a heterocyclic ring with 3-7 ring atoms which can be substituted by one, two or three residues R.sup.1 which can be the same or different,Y represents an oxygen or sulphur atom, or a SO or SO.sub.2 group,X can be an oxygen or sulphur atom,R denotes an aliphatic residue with 1-9 C-atoms which can be substituted by phenyl or denotes a phenyl ring or a carbocyclic ring with 7-15 C atoms or a heterocyclic ring system each having 5 or 6 ring atoms,in which the aforementioned phenyl rings, carbocyclic rings or heterocyclic ring system can be substituted once or several times, if desired, and R1-R5 denote hydrogen or an aliphatic residue, as well as their tautomers, enantiomers, diastereomers and physiologically tolerated salts.Type: GrantFiled: March 4, 1994Date of Patent: April 30, 1996Assignee: Boehringer Mannheim GmbHInventors: Harald Zilch, Herbert Leinert, Alfred Mertens
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Patent number: 5397794Abstract: The present invention concerns the use of compounds of the general formula I ##STR1## for the preparation of medicaments for the treatment of viral or retroviral infections, whereby R signifies a hydrogen atom or a straight-chained or branched, saturated or unsaturated alkyl radical with 1-7 carbon atoms, which can possibly be substituted by phenyl, or a phenyl ring which can possibly be substituted one or more times by C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, hydroxyl, trifluoromethyl, methylsulphonyl or halogen, such as fluorine, chlorine or bromine, n stands for the numbers 0, 1 or 2, as well as of their pharmacologically compatible salts or tautomers.Type: GrantFiled: July 20, 1993Date of Patent: March 14, 1995Assignee: Boehringer Mannheim GmbHInventors: Harald Zilch, Alfred Mertens, Herbert Leinert, Ulrike Leser, Bernhard Konig, Hans Seidel
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Patent number: 5071868Abstract: A process for the preparation of S- or R-carbazole derivatives of the general formula: ##STR1## in which R is an unsubstituted or substituted amino radical and pharmacologically acceptable salts, by either reacting R-(-)-epichlorohydrin (for the S-carbozole derivative); or reacting an S-epoxide derivative of the general formula: ##STR2## in which R.sub.1 is the residue of a substituted sulphonic acid derivative (for the R-carbazole derivative); with 4-hydroxycarbazole and then with ammonia or a substituted amine of the general formula RH, and recovering the compound or converting it to a pharmacologically acceptable salt.The new R-(+)- and S(-)-carbazole derivatives provided by the inventive process have unexpected beta blocking and vasodilatory properties and are useful in pharmaceutical compositions. R-(+)-carbazole derivatives are also useful for the treatment of glaucoma.Type: GrantFiled: January 28, 1991Date of Patent: December 10, 1991Assignee: Boehringer Mannheim GmbHInventor: Herbert Leinert
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Patent number: 4999361Abstract: The present invention provides compounds of the general formula ##STR1## wherein R.sub.1 is a hydrogen atom, a straight-chained or branched C.sub.1 -C.sub.12 -alkyl radical, a C.sub.3 -C.sub.7 -cycloalkyl radical, a straight-chained or branched C.sub.2 -C.sub.12 -alkenyl radical or an unsubstituted or substituted C.sub.3 -C.sub.7 -mono- or bicycloalkenyl radical, an unsubstituted or singly or multiple substituted monocyclic aromatic or heteroaromatic radical, R.sub.2 and R.sub.3, which can be the same or different, are straight-chained, branched, saturated or unsaturated C.sub.1 -C.sub.6 -aliphatic radicals or, together with the nitrogen atom to which they are attached, form a saturated or unsaturated ring which can contain further heteroatoms and can optionally be substituted by a lower alkyl radical, a lower alkoxy radical or an oxygen atom, R.sub.4 is an unsubstituted or singly or multiple substituted monocyclic aromatic radical, an unsubstituted or substituted five- or six-membered heteroaromatic ring, R.Type: GrantFiled: February 27, 1989Date of Patent: March 12, 1991Assignee: Boehringer Mannheim GmbHInventors: Christos Tsaklakidis, Herbert Leinert, Peter Freund
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Patent number: 4985454Abstract: A process for the preparation of S- or R-carbazole derivatives of the general formula: ##STR1## in which R is an unsubstituted or substituted amino radical and pharmacologically acceptable salts, by either reacting R-(-)-epichlorohydrin (for the S-carbazole derivative); or reacting an S-epoxide derivative of the general formula: ##STR2## in which R.sub.1 is the residue of a substituted sulphonic acid derivative (for the R-carbazole derivative); with 4-hydroxycarbazole and then with ammonia or a substituted amine of the general formula RH, and recovering the compound or converting it to a pharmacologically acceptable salt.The new R-(+)- and S(-)-carbazole derivatives provided by the inventive process have unexpected beta blocking and vasodilatory properties and are useful in pharmaceutical compositions. R-(+)-carbazole derivatives are also useful for the treatment of glaucoma.Type: GrantFiled: January 19, 1989Date of Patent: January 15, 1991Assignee: Boehringer Mannheim GmbHInventor: Herbert Leinert
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Patent number: 4937337Abstract: The present invention provides compounds of the general formula: ##STR1## wherein R.sub.1 is a straight-chained or branched C.sub.1 -C.sub.12 -alkyl radical which can be substituted by a phenyl, naphthyl or C.sub.3 -C.sub.7 -cycloalkyl radical, a straight-chained or branched C.sub.2 -C.sub.12 -alkenyl radical which can be substituted by a C.sub.3 -C.sub.7 -cycloalkyl, phenyl or naphthyl radical, a C.sub.3 -C.sub.7 -cycloalkyl radical or an unsubstituted or mono- or polysubstituted mono- or bicyclic aromatic radical, in which the substituents can be halogen atoms, carboxyl groups or C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy or C.sub.1 -C.sub.4 -alkoxycarbonyl radicals, R.sub.2 and R.sub.3, which can be the same or different, are straight-chained, branched, saturated or unsaturated C.sub.1 -C.sub.6 -alkyl radicals or, together with the nitrogen atom to which they are attached, form a saturated or unsaturated ring which can contain further heteroatoms and can possibly be substituted by a C.sub.1 -C.sub.Type: GrantFiled: March 10, 1989Date of Patent: June 26, 1990Assignee: Boehringer Mannheim GmbHInventors: Herbert Leinert, Christos Tsaklakidis, Peter Freund
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Patent number: 4927834Abstract: The present invention provides compounds of the general formula: ##STR1## wherein R.sub.1 is a straight-chained or branched C.sub.1 -C.sub.12 -alkyl radical which can be substituted by phenyl, naphthyl or a C.sub.3 -C.sub.7 -cycloalkyl radical; a straight-chained or branched C.sub.2 -C.sub.6 -alkenyl radical which can be substituted by a C.sub.3 -C.sub.7 -cycloalkyl radical or a phenyl or naphthyl radical; a C.sub.3 -C.sub.7 -cycloalkyl radical or a mono- or bicyclic aromatic radical which is unsubstituted or substituted one or more times, the substituents being C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, carboxyl or carbethoxy, R.sub.2 and R.sub.3, which can be the same or different, are straight-chained or branched, saturated or unsaturated C.sub.1 -C.sub.6 -alkyl radicals which are optionally substituted by hydroxyl, C.sub.1 -C.sub.3 -alkoxy or C.sub.1 -C.sub.3 -alkoxy-C.sub.1 -C.sub.Type: GrantFiled: August 11, 1988Date of Patent: May 22, 1990Assignee: Boehringer Mannhein GmbHInventors: Herbert Leinert, Christos Tsaklakidis, Gisbert Sponer
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1,2-diamino compounds, process for their preparation and pharmaceutical compositions containing them
Patent number: 4923889Abstract: Compounds are disclosed, including 2-diethylamino-3-isobutoxy-N-phenyl-N-2-furanyl-methyl-propylamine and compounds of the formula: ##STR1## wherein R.sub.1 is an iso-C.sub.4 -C.sub.6 -alkyl radical; A is a valency bond or a straight-chained or branched alkyl radical containing up to 6 carbon atoms; R.sub.4 is a phenyl radical which is unsubstituted or substituted one or more times by C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.1 -C.sub.3 -alkoxy, C.sub.2 -C.sub.6 -alkenyloxy, hydroxy-C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkylenedioxy, hydroxy-C.sub.1 -C.sub.3 -alkoxy, C.sub.1 -C.sub.3 -alkoxy-C.sub.1 -C.sub.3 -alkoxy, C.sub.1 -C.sub.6 -alkylamino, di(C.sub.1 -C.sub.6 -alkyl)amino, C.sub.1 -C.sub.3 -alkoxycarbonyl-C.sub.1 -C.sub.3 -alkoxy, C.sub.1 -C.sub.6 -alkylthio, C.sub.1 -C.sub.6 -alkylsulphinyl, C.sub.1 -C.sub.6 -alkylsulphonyl, C.sub.1 -C.sub.6 -alkylsulphonyloxy, carboxyl, C.sub.1 -C.sub.3 -alkoxycarbonyl, aminocarbonyl, mono- or di(C.sub.1 -C.sub.6 -alkyl)aminocarbonyl, halo-C.Type: GrantFiled: August 11, 1988Date of Patent: May 8, 1990Assignee: Boehringer Mannheim GmbHInventors: Herbert Leinert, Christos Tsaklakidis, Gisbert Sponer -
Patent number: 4880805Abstract: The present invention is concerned with the use of compounds of the general formula: ##STR1## wherein A is an optionally substituted phenyl or heteroaromatic radical, R.sub.6 and R.sub.7 are hydrogen or lower alkyl, X is an alkylene chain containing up to 6 carbon atoms, Y is a valency bond or a >C.dbd.O group and B is an optionally substituted phenyl or heteroaromatic radical, as well as of their pharmacologically acceptable salts for the treatment of blood flow disturbances. The present invention also provides pharmaceutical compositions which contain these compounds.Type: GrantFiled: July 21, 1988Date of Patent: November 14, 1989Assignee: Boehringer Mannheim GmbHInventors: Erwin Bohm, Jens-Peter Holck, Wolfgang Kampe, Herbert Leinert, Bernd Muller-Beckmann, Klaus Strein
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Patent number: 4824963Abstract: A process for the preparation of S- or R-carbazole derivatives of the general formula: ##STR1## in which R is an unsubstituted or substituted amino radical and pharmacologically acceptable salts, by either reacting R-(-)-epichlorohydrin (for the S-carbazole derivative); or reacting an S-epoxide derivative of the general formula: ##STR2## in which R.sub.1 is the residue of a substituted sulphonic acid derivative (for the R-carbazole derivative); with 4-hydroxycarbazole and then with ammonia or a substituted amine of the general formula RH, and recovering the compound or converting it to a pharmacologically acceptable salt.The new R-(+)- and S-(-)-carbozole derivatives provided by the inventive process have unexpected beta blocking and vasodilatory properties and are useful in pharmaceutical compositions. R-(+)-carbazole derivatives are also useful for the treatment of glaucoma.Type: GrantFiled: May 13, 1987Date of Patent: April 25, 1989Assignee: Boehringer Mannheim GmbHInventor: Herbert Leinert