Patents by Inventor Leo Alig

Leo Alig 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: 5726185
    Abstract: Acetic acid derivatives of the formula ##STR1## wherein L, M, T and Q have the significance given in the description, can be used for the treatment or prophylaxis of illnesses which are caused by the binding of adhesive proteins to blood platelets and by blood platelet aggregation and cell-cell adhesion, and are manufactured by cleaving protecting groups in the corresponding protected compounds or by converting the cyano group into the amidino group in corresponding nitriles.
    Type: Grant
    Filed: December 1, 1994
    Date of Patent: March 10, 1998
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Paul Hadvary, Marianne Hurzeler Muller, Marcel Muller, Beat Steiner, Thomas Weller
  • Patent number: 5670515
    Abstract: N-Acyl-.alpha.-aminocarboxylic acid derivatives of the formula ##STR1## wherein L, R' to R'" and Q have the definitions given in the specification, are for the treatment or prophylaxis of illnesses which are caused by the binding of adhesive proteins to blood platelets, by blood platelet aggregation and cell-cell adhesion. They are manufactured by cleaving off protecting groups in corresponding protected compounds or by converting the cyano group into the amidino group in corresponding nitriles.
    Type: Grant
    Filed: May 25, 1995
    Date of Patent: September 23, 1997
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Paul Hadvary, Marianne Hurzeler, Marcel Muller, Beat Steiner, Thomas Weller
  • Patent number: 5663297
    Abstract: Disclosed herein are peptide of the formulaR--CONH--CH.sub.2 --CONH--CH(R')--CH.sub.2 COOH Iwherein R and R' are as defined herein. The claimed peptide derivatives inhibit platelet aggregation and as such are useful in the treatment of thrombosis.
    Type: Grant
    Filed: May 30, 1995
    Date of Patent: September 2, 1997
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Albrecht Edenhofer, Marcel Muller, Arnold Trzeciak, Thomas Weller
  • Patent number: 5658928
    Abstract: N-Acyl-.alpha.-aminocarboxylic acid derivatives of the formula ##STR1## wherein L, R' to R'" and Q have the significance given in the description, can be used for the treatment or prophylaxis of illnesses which are caused by the binding of adhesive proteins to blood platelets and by blood platelet aggregation and cell-cell adhesion.
    Type: Grant
    Filed: September 21, 1994
    Date of Patent: August 19, 1997
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Paul Hadvary, Marianne Hurzeler, Marcel Muller, Beat Steiner, Thomas Weller
  • Patent number: 5545658
    Abstract: N-Acyl-.alpha.-aminocarboxylic acid derivatives of the formula ##STR1## wherein L, R' to R'" and Q have the significance given in the description, can be used for the treatment or prophylaxis of illnesses which are caused by the binding of adhesive proteins to blood platelets and by blood platelet aggregation and cell-cell adhesion.
    Type: Grant
    Filed: May 25, 1995
    Date of Patent: August 13, 1996
    Assignee: Hoffman-La Roche Inc.
    Inventors: Leo Alig, Paul Hadvary, Marianne H urzeler, Marcel M uller, Beat Steiner, Thomas Weller
  • Patent number: 5430024
    Abstract: Acetic acid derivatives of formulaH.sub.2 N(NH)C--X--Y--CO--Z--CH(Q.sup.1)COOQ.sup.2 Iand hydrates, solvates and physiologically acceptable salts thereof are useful to inhibit the binding of adhesive proteins to blood platelets and also to inhibit blood platelet aggregation and cell-cell adhesion.
    Type: Grant
    Filed: September 20, 1993
    Date of Patent: July 4, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Albrecht Edenhofer, Marcel Muller, Arnold Trzeciak, Thomas Weller
  • Patent number: 5399585
    Abstract: Novel carboxamides and sulfonamides are described having of the formulaR.sup.1 --A--(W).sub.a --X--(CH.sub.2).sub.b --(Y).sub.c --B--Z--COOR(I),in which R.sup.1, A, W, X, Y, B, Z, R, a, b and c are as provided in the description. These compounds are useful in the treatment of thromboses, apoplexy, myocardial infarct, inflammations, arteriosclerosis as well as in the treatment and prevention of tumors. These novel compounds are prepared by eliminating the protective groups in corresponding compounds with protected amidino or guanidino groups.
    Type: Grant
    Filed: August 30, 1993
    Date of Patent: March 21, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Albrecht Edenhofer, Marcel Muller, Arnold Trzeciak, Thomas Weller
  • Patent number: 5378712
    Abstract: N-Acyl-.alpha.-aminocarboxylic acid derivatives of the formula ##STR1## wherein L, R' to R"' and Q have the significance given in the description, can be used for the treatment or control of illnesses which are caused by the binding of adhesive proteins to blood platelets and by blood platelet aggregation and cell-cell adhesion.
    Type: Grant
    Filed: March 19, 1992
    Date of Patent: January 3, 1995
    Assignee: Hoffmann-La Roche Inc
    Inventors: Leo Alig, Paul Hadvary, Marianne Hurzeler, Marcel Muller, Beat Steiner, Thomas Weller
  • Patent number: 5273982
    Abstract: Acetic acid derivatives of formulaH.sub.2 N(NH)C--X--Y--CO--Z--CH(Q.sup.1)COOQ.sup.2 Iand hydrates, solvates and physiologically acceptable salts thereof are useful to inhibit the binding of adhesive proteins to blood platelets and also to inhibit blood platelet aggregation and cell-cell adhesion.
    Type: Grant
    Filed: March 5, 1991
    Date of Patent: December 28, 1993
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Albrecht Edenhofer, Marcel Muller, Arnold Trzeciak, Thomas Weller
  • Patent number: 5256812
    Abstract: Novel carboxamides and sulfonamides are described having of the formulaR.sup.1 --A--(W).sub.a --X--(CH.sub.2).sub.b --(Y).sub.c --B--Z--COOR(I),in which R.sup.1, A, W, X, Y, B, Z, R, a, b and c are as provided in the description. These compounds are useful in the treatment of thromboses, apoplexy, myocardial infarct, inflammations, arteriosclerosis as well as in the treatment and prevention of tumors. These novel compounds are prepared by eliminating the protective groups in corresponding compounds with protected amidino or guanidino groups.
    Type: Grant
    Filed: September 6, 1991
    Date of Patent: October 26, 1993
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Albrecht Edenhofer, Marcel Muller, Arnold Trzeciak, Thomas Weller
  • Patent number: 5166218
    Abstract: Tertiary and secondary amines of the formulas ##STR1## and ##STR2## wherein n is the integer 1 or 2,R is hydrogen, lower-alkanoyl or phenyl-lower-alkanoyl,X.sup.1 is phenoxymethyl optionally mono-fluorinated or mono-chlorinated in the ortho-position,X.sup.2 is lower-alkyl, phenoxymethyl optionally mono-fluorinated or mono-chlorinated in the ortho-position or phenyl optionally monosubstituted by fluorine, chlorine, trifluoromethyl or lower-alkoxy,Y is hydrogen or methyl, andZ is a phenyl or thienyl residue substituted as hereinafter described,and the physiologically and pharmaceutically compatible salts are described. The compounds of formulas I and V-1 have catabolic activity and can be used for the treatment of obesity and diabetes mellitus or for the treatment of conditions which are associated with an increased protein breakdown, or as feed additives for fattening animals. The compounds of formulas I and V-1 can be prepared starting from corresponding primary amines.
    Type: Grant
    Filed: August 12, 1991
    Date of Patent: November 24, 1992
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Marcel Muller
  • Patent number: 5084466
    Abstract: Novel carboxamides and sulfonamides are described having of the formulaR.sup.1 --A--(W).sub.a --X--(CH.sub.2).sub.b --(Y).sub.c --B--Z--COOR (I),in which R.sup.1, A, W, X, Y, B, Z, R, a, b and c are as provided in the description. These compounds are useful in the treatment of thromboses, apoplexy, myocardial infarct, inflammations, arteriosclerosis as well as in the treatment and prevention of tumors. These novel compounds are prepared by eliminating the protective groups in corresponding compounds with protected amidino or guanidino groups.
    Type: Grant
    Filed: January 16, 1990
    Date of Patent: January 28, 1992
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Albrecht Edenhofer, Marcel Muller, Arnold Trzeciak, Thomas Weller
  • Patent number: 5064863
    Abstract: Tertiary and secondary amines of the formulas ##STR1## wherein n is the integer 1 or 2, p0 R is hydrogen, lower-alkanoyl or phenyl-lower-alkanoyl,X.sup.1 is phenoxymethyl optionally mono-fluorinated or mono-chlorinated in the ortho-position,X.sup.2 is lower-alkyl, phenoxymethyl optionally mono-fluorinated or mono-chlorinated in the ortho-position or phenyl optionally monosubstituted by fluorine, chlorine, trifluoromethyl or lower-alkoxy,Y is hydrogen or methyl, andZ is a phenyl or thienyl residue substituted as hereinafter described,and the physiologically and pharmaceutically compatible salts are described. The compounds of formulas I and V-1 have catabolic activity and can be used for the treatment of obesity and diabetes mellitus or for the treatment of conditions which are associated with an increased protein breakdown, or as feed additives for fattening animals. The compounds of formulas I and V-1 can be prepared starting from corresponding primary amines.
    Type: Grant
    Filed: December 10, 1987
    Date of Patent: November 12, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Marcel Muller
  • Patent number: 5039805
    Abstract: The compound of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 have the significance given in the description, can be used as medicaments for the therapy and prophylaxis of disorders such as thromboses, stroke, cardiac infarct, inflammations and arteriosclerosis as well as for the treatment of tumours.
    Type: Grant
    Filed: November 24, 1989
    Date of Patent: August 13, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Albrecht Edenhofer, Marcel Muller, Arnold Trzeciak, Thomas Weller
  • Patent number: 5017619
    Abstract: The invention is directed to phenethanolamine derivatives and their pharmaceutically compatible salts, having the formula ##STR1## wherein n is the number 1 or 2; L.sup.1 and L.sup.2 are hydrogen, C.sub.1-3 -(alkyl)carbonyl or C.sub.1-3 (alkoxy) carbonyl; T is hydrogen or methyl; X.sup.1 and X.sup.2 are phenyl or phenyl which is monosubstituted in the m-position by Br, Cl, F, CF.sub.3 and NO.sub.2 ; Y is --(CH.sub.2).sub.1-6 --O--G, --(CH.sub.2).sub.1-6 --CH.dbd.CH--C(O)--Z, --C(O)--Z or --CH(COOR").sub.2 ; G is C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy-C.sub.1-4 -alkyl or --(CH.sub.2).sub.1-4 --Q; Q is phenoxy, phenyl, p-fluorophenyl or p-phenoxyphenyl; Z is a --OR or --N(R,R'); R and R' are hydrogen or C.sub.1-4 -alkyl or R and R' together with the N-atom to which they are attached form a 5- or 6-membered saturated ring which optionally contains an O-atom or an additional N-atom; and R" is C.sub.1-4 -alkyl.
    Type: Grant
    Filed: December 16, 1988
    Date of Patent: May 21, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Marcel Muller
  • Patent number: 4988714
    Abstract: Pyridine-ethanolamines of the formula ##STR1## wherein n, X, Y, R.sup.1, R.sup.2 and R.sup.3 have the significances given in the description, their corresponding enantiomers, diastereomers, and racemates as well as the physiologically compatible salts thereof are described. The compounds of formula I have catabolic activity and can be used for the treatment of obesity and of diabetes mellitus or of conditions which are associated with an increased protein breakdown, or as feed additives for fattening animals. The compounds of formula I can be prepared by alkylating the primary or secondary amines corresponding to the secondary or tertiary amines of formula I.
    Type: Grant
    Filed: August 26, 1988
    Date of Patent: January 29, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Marcel Muller
  • Patent number: 4892886
    Abstract: [p-[2-[[(S)-2-hydroxy-3-phenoxypropyl]amino]-ethyl]phenoxy]acetic acid and its physiologically compatible salts, which have catabolic activity and can be used for the treatment of obesity, of diabetes and of conditions which are associated with increased protein breakdown or as feed additives for fattening animals, as described. The compounds are prepared starting from esters corresponding to the aforementioned acid.
    Type: Grant
    Filed: May 10, 1989
    Date of Patent: January 9, 1990
    Assignee: Hoffman-La Roche Inc.
    Inventors: Leo Alig, Marcel Muller
  • Patent number: 4871755
    Abstract: The oxazolidines of the formula ##STR1## wherein n signifies the number 1 or 2.T signifies lower carbalkoxy.X signifies phenoxymethyl optionally mono-fluorinated or mono-chlorinated in the ortho-position or phenyl optionally monosubstituted by fluorine, chlorine, trifluoromethyl or lower-alkoxy.Y signifies hydrogen or methyl, andZ signifies a phenyl or thienyl residue substituted in a defined manner.and the physiologically compatible salts thereof have catabolic activity and can be used for the treatment of obesity and diabetes mellitus or for the treatment of conditions which are associated with an increased protein breakdown, or as feed additives for fattening animals. They are manufactured starting from corresponding primary amines.
    Type: Grant
    Filed: February 5, 1988
    Date of Patent: October 3, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Marcel Muller
  • Patent number: 4800206
    Abstract: Pyridine-ethanolamines of the formula ##STR1## wherein n, X, Y, R.sup.1, R.sup.2 and R.sup.3 have the significances given in the description, their corresponding enantiomers, diastereomers, and racemates as well as the pysiologically compatible salts thereof are describe. The compounds of formula I have catabolic activity and can be used for the treatment of obesity and of diabetes mellitus or of conditions which are associated with an increased protein breakdown, or as feed additives for fattening animals. The compounds of formula I can be prepared by alkylating the primary or secondary amines corresponding to the secondary or tertiary amines of formula I.
    Type: Grant
    Filed: June 3, 1987
    Date of Patent: January 24, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Marcel Muller
  • Patent number: 4743604
    Abstract: The oxazolidines of the formula ##STR1## wherein n signifies the number 1 or 2,T signifies lower carbalkoxy,X signifies phenoxymethyl optionally mono-fluorinated or mono-chlorinated in the ortho-position or phenyl optionally monosubstituted by fluorine, chlorine, trifluoromethyl or lower-alkoxy,Y signifies hydrogen or methyl, andZ signifies a phenyl or thienyl residue substituted in a defined manner,and the physiologically compatible salts thereof have catabolic activity and can be used for the treatment of obesity and diabetes mellitus or for the treatment of conditions which are associated with an increased protein breakdown, or as feed additives for fattening animals. They are manufactured starting from corresponding primary amines.
    Type: Grant
    Filed: November 1, 1984
    Date of Patent: May 10, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Marcel Muller