Patents by Inventor Guido Melzer

Guido Melzer 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: 7060706
    Abstract: Quinazolinones of formula (I) in which R, R1, R2, R3, R4, Y, n and m have the meaning indicated in Patent claim 1, and their salts or solvates as glycoprotein IbIX antagonists
    Type: Grant
    Filed: September 13, 2000
    Date of Patent: June 13, 2006
    Assignee: 3-Dimensional Pharmaceuticals, Inc.
    Inventors: Werner Mederski, Ralf Devant, Gerhard Barnickel, Sabine Bernotat-Danielowski, Guido Melzer, Bertram Cezanne, Daljit Dhanoa, Bao-Ping Zhao, James Rinker, Mark Player, Richard Soll
  • Patent number: 6890930
    Abstract: Quinazolinones of formula (I) in which R, R1, R2, R3, R4, Y, Z, and m have the meaning indicated in patent claim 1, and their salts or solvates as glycoprotein IbIX antagonists.
    Type: Grant
    Filed: September 13, 2000
    Date of Patent: May 10, 2005
    Assignee: 3-Dimensional Pharmaceuticals, Inc.
    Inventors: Werner Mederski, Maria Devant, Gerhard Barnickel, Sabine Bernotat-Danielowski, Guido Melzer, Bertram Cezane, Dalijit Dhanoa, Bao-Ping Zhoa, James Rinker, Mark Player, Richard Soll, Ralf Devant
  • Patent number: 6602876
    Abstract: Compounds of the formula I wherein R1, R2 and R3 have the meanings defined herein, and also their physiologically acceptable salts, inhibit the binding of fibrinogen to the corresponding receptor and can be employed for the treatment of thromboses, osteoporoses, oncoses, apoplexy, cardiac infarct, ischaemias, inflammations, arteriosclerosis and osteolytic disorders.
    Type: Grant
    Filed: November 2, 1995
    Date of Patent: August 5, 2003
    Assignee: Merck Patent GmbH
    Inventors: Joachim Gante, Horst Juraszyk, Peter Raddatz, Hanns Wurziger, Sabine Bernotat-Danielowski, Guido Melzer, Matthias Wiesner, Claus Fittschen
  • Publication number: 20030135055
    Abstract: The invention relates to compounds of the formula I 1
    Type: Application
    Filed: August 21, 2002
    Publication date: July 17, 2003
    Inventors: Dieter Dorsch, Horst Juraszyk, Werner Mederski, Christos Tsaklakidis, Sabine Bernotat-Danielowski, Guido Melzer, Johannes Gleitz, Christopher Barnes, James Vickers
  • Patent number: 6492368
    Abstract: Novel compounds of the formula I in which X, Y, R1, R2 and R3 are as defined in Patent Claim 1 are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic disorders.
    Type: Grant
    Filed: March 31, 2000
    Date of Patent: December 10, 2002
    Assignee: Merck Patent GmbH
    Inventors: Dieter Dorsch, Hanns Wurziger, Guido Melzer, Horst Juraszyk, Sabine Bernotat-Danielowski
  • Patent number: 6492384
    Abstract: The invention relates to novel compounds of formula (I), wherein R, R1, R2, R3, n and p have the meaning defined in claim 1. Compounds are inhibitors of clotting factor Xa and can be used for the prophylaxis and/or therapy of thrombo-embolic disorders.
    Type: Grant
    Filed: December 13, 2001
    Date of Patent: December 10, 2002
    Assignee: Merck Patent GmbH
    Inventors: Werner Mederski, Horst Juraszyk, Hanns Wurziger, Joachim Gante, Dieter Dorsch, Hans-Peter Buchstaller, Sabine Bernotat-Danielowski, Guido Melzer, Soheila Anzali
  • Patent number: 6455529
    Abstract: Compounds of the formula I in which R1, R2 and R3 have the stated meanings, and their physiologically acceptable salts, inhibit the binding of fibrinogen to the corresponding receptor and can be used for the treatment of thromboses, osteoporoses, oncoses, stroke, myocardial infarct, ischemias, inflammations, arteriosclerosis and osteolytic disorders.
    Type: Grant
    Filed: May 3, 1996
    Date of Patent: September 24, 2002
    Assignee: Merck Patent Gesellschaft mit beschraenkter Haftung
    Inventors: Joachim Gante, Hörst Juraszyk, Peter Raddatz, Hanns Wurziger, Sabine Bernotat-Danielowski, Guido Melzer
  • Patent number: 6380430
    Abstract: Novel compounds of the formula I in which X, R1, R2, R3, R4 and R5 have the meaning indicated in Patent Claim 1, are inhibitors of the coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic disorders.
    Type: Grant
    Filed: December 29, 2000
    Date of Patent: April 30, 2002
    Assignee: Merck Patent Gesellschaft mit beschraenkterHaftung
    Inventors: Dieter Dorsch, Horst Juraszyk, Werner Mederski, Joachim Gante, Hanns Wurziger, Hans-Peter Buchstaller, Sabine Bernotat-Danielowski, Guido Melzer
  • Patent number: 6204280
    Abstract: Compounds of the formula I wherein R1, R2 and R3 have the meanings defined herein, and also their physiologically acceptable salts, inhibit the binding of fibrinogen to the corresponding receptor and can be employed for the treatment of thromboses, osteoporoses, oncoses, apoplexy, cardiac infarct, ischaemias, inflammations, arteriosclerosis and osteolytic disorders.
    Type: Grant
    Filed: September 30, 1998
    Date of Patent: March 20, 2001
    Assignee: Merck Patent Gesellschaft mit berschrankter Haftung
    Inventors: Joachim Gante, Horst Juraszyk, Peter Raddatz, Hanns Wurziger, Sabine Bernotat-Danielowski, Guido Melzer, Matthias Wiesner, Claus Fittschen
  • Patent number: 6028090
    Abstract: Novel oxazolidinone derivatives of the formula I ##STR1## in which R.sup.1 is a phenyl radical which is unsubstituted or is monosubstituted by CN, H.sub.2 N--CH.sub.2 --, A.sub.2 N--CH.sub.2 --, H.sub.2 N--C(.dbd.NH)--, H.sub.2 N--C(.dbd.NH)--NH--, H.sub.2 N--C(.dbd.NH)--NH--CH.sub.2 --, HO--NH--C(.dbd.NH)-- or HO--NH--C(.dbd.NH)--NH--,X is O, S, SO, SO.sub.2, --NH-- or --NA--,B is ##STR2## A is alkyl having from 1 to 6 C atoms, R.sup.2 is H, A, Li, Na, K, NH.sub.4 or benzyl,R.sup.3 is H or (CH.sub.2).sub.n --COOR.sup.2,E is, in each case independently of each other, CH or N,Q is O, S or NH,m is 1, 2 or 3, andn is 0, 1, 2 or 3,and physiologically compatible salts thereof are provided, which inhibit the binding of fibrinogen to the corresponding receptor and can be used for treating thrombosis, stroke, cardiac infarction, inflammations, arteriosclerosis, osteoporosis and also tumors.
    Type: Grant
    Filed: November 6, 1997
    Date of Patent: February 22, 2000
    Assignee: Merck Patent Gesellschaft mit Beschrankter Haftung
    Inventors: Joachim Gante, Horst Juraszyk, Peter Raddatz, Hanns Wurziger, Guido Melzer, Sabine Bernotat-Danielowski
  • Patent number: 5908843
    Abstract: Novel piperazine derivatives of formula I:Y--(C.sub.m H.sub.2m --CHR.sup.1).sub.n --CO--(NH--CHR.sup.2 --CO).sub.r -- Zwherein ##STR1## R.sup.1, R.sup.2 and R.sup.7 are each, independently, --C.sub.t H.sub.2t --R.sup.9, benzyl, hydroxybenzyl, imidazolylmethyl or indolylmethyl;R.sup.3 is H or H.sub.2 N--C(.dbd.NH)--;R.sup.4 and R.sup.6 are each, independently, (H,H) or .dbd.O;R.sup.5 is H, H.sub.2 N--C(.dbd.NH)-- or H.sub.2 N--C(.dbd.NH)--NH;R.sup.8 is OH, OA or NHOH;R.sup.9 is H, OH, NH.sub.2, SH, SA, COOH, CONH.sub.2 or NH--C(.dbd.NH)--NH.sub.2 ;A is in each case, independently, alkyl having 1-4 C atoms;m and t are each, independently, 0, 1, 2, 3 or 4;n and r are each, independently, 0 or 1; andp is 0, 1 or 2,inhibit the binding of fibrinogen to the fibrinogen receptor and can be used for the treatment of thrombosis, apoplexy, cardiac infarctus, inflammation, arteriosclerosis and tumors.
    Type: Grant
    Filed: January 31, 1994
    Date of Patent: June 1, 1999
    Assignee: Merck Patent Gesellschaft mit Beschrankter Haftung
    Inventors: Joachim Gante, Peter Raddatz, Horst Juraszyk, Sabine Bernotat-Danielowski, Guido Melzer
  • Patent number: 5866540
    Abstract: The present invention relates to pharmaceutical compositions which contain at least one cyclopeptide of formula I (a)-(r):(a) cyclo(-Arg-Gly-Asp-D-Phe-Val-Ala);(b) cyclo(-Arg-Gly-Asp-D-Phe-Leu-Ala);(c) cyclo(-Arg-Gly-Asp-Phe-Val-D-Ala);(d) cyclo(-Arg-Gly-Asp-Phe-Leu-D-Ala);(e) cyclo(-Arg-Gly-Asp-D-Phe-Val-Gly);(f) cyclo(-Arg-Gly-Asp-D-Phe-Leu-Gly);(g) cyclo(-D-Arg-Gly-Asp-Phe-Val-Ala);(h) cyclo(-D-Arg-Gly-Asp-Phe-Val-Gly);(i) cyclo(-Arg-Gly-Asp-Phe-Pro-Gly);(j) cyclo(-Arg-Gly-Asp-Phe-D-Pro-Gly);(k) cyclo(-Arg-Gly-Asp-Phe-Pro-Ala);(l) cyclo(-Arg-Gly-Asp-Phe-D-Pro-Ala);(m) cyclo(-D-Arg-Gly-Asp-Phe-Val);(n) cyclo(-Arg-D-Ala-Asp-Phe-Val);(o) cyclo(-Arg-Gly-Asp-D-Phe-Val);(p) cyclo(-Arg-Ala-Asp-D-Phe-Val);(q) cyclo(-Arg-Gly-Asp-Phe-D-Val);(r) cyclo(-Arg-Gly-D-Asp-Phe-Val);or a salt thereof. The pharmaceutical compositions can be used as cell adhesion inhibitors, e.g., in the treatment of thrombosis, myocardial infarct, apoplexy, arteriosclerosis, inflammations, angina pectoris, and/or tumors.
    Type: Grant
    Filed: January 4, 1995
    Date of Patent: February 2, 1999
    Assignee: Merck Patent Gesellschaft mit Beschrankter Haftung
    Inventors: Alfred Jonczyk, Gunter Holzemann, Brunhilde Felding-Habermann, Guido Melzer, Beate Diefenbach, David A. Cheresh, Horst Kessler, Marion Gurrath, Gerhard Muller
  • Patent number: 5776937
    Abstract: Compounds of the formula I ##STR1## wherein R.sup.1 and Y have the meanings indicated, and also their physiologically acceptable salts, inhibit the binding of fibrinogen to the corresponding receptor and can be employed for the treatment of thromboses, osteoporoses, oncoses, apoplexy, cardiac infarct, inflammations, arteriosclerosis and osteolytic disorders.
    Type: Grant
    Filed: November 7, 1995
    Date of Patent: July 7, 1998
    Assignee: Merck Patent Gesellschaft mit Beschrankter Haftung
    Inventors: Joachim Gante, Horst Juraszyk, Peter Raddatz, Hanns Wurziger, Sabine Bernotat-Danielowski, Guido Melzer
  • Patent number: 5723480
    Abstract: Novel oxazolidinone derivatives of the formula I ##STR1## in which R.sup.1 is a phenyl radical which is unsubstituted or is monosubstituted by CN, H.sub.2 N--CH.sub.2 --, A.sub.2 N--CH.sub.2 --, H.sub.2 N--C(.dbd.NH)--, H.sub.2 N--C(.dbd.NH)--NH--, H.sub.2 N--C(.dbd.NH)--NH--CH.sub.2 --, HO--NH--C(.dbd.NH)-- or HO--NH--C(.dbd.NH)--NH--,X is O, S, SO, SO.sub.2, --NH-- or --NA--,B is ##STR2## A is alkyl having from 1 to 6 C atoms, R.sup.2 is H, A, Li, Na, K, NH.sub.4 or benzyl,R.sup.3 is H or (CH.sub.2).sub.n --COOR.sup.2,E is, in each case independently of each other, CH or N,Q is O, S or NH,m is 1, 2 or 3, andn is 0, 1, 2 or 3,and physiologically compatible salts thereof are provided, which inhibit the binding of fibrinogen to the corresponding receptor and can be used for treating thrombosis, stroke, cardiac infarction, inflammations, arteriosclerosis, osteoporosis and also tumors.
    Type: Grant
    Filed: May 29, 1996
    Date of Patent: March 3, 1998
    Assignee: Merck Patent Gesellschaft Mit Beschrankter Haftung
    Inventors: Joachim Gante, Horst Juraszyk, Peter Raddatz, Hanns Wurziger, Guido Melzer, Sabine Bernotat-Danielowski
  • Patent number: 5710131
    Abstract: A protein isolated from crude extracts of Hirudo medicinalis is disclosed, which strongly inhibits the binding to collagen of platelets and their subsequent activation, which leads to platelet aggregation and thrombus formation. Additionally the protein prevents binding of von Willebrand factor to collagen. Described is a method for isolation and purification of the protein as well as its use for blocking collagen-stimulated platelet aggregation. The new protein (Brandinin) has a molweight of approximately 15 kD, binds to collagen but has no collagen-cleaving activity. The protein is useful in the prophylaxis, prevention and treatment of thrombotic diseaeses and for coating of blood-contacting materials, rendering them thromboresistant.
    Type: Grant
    Filed: February 28, 1995
    Date of Patent: January 20, 1998
    Assignee: Merck Patent Gesellschaft Mit Beschrankter Haftung
    Inventors: Jurgen Hemberger, Guido Melzer
  • Patent number: 5705481
    Abstract: The invention relates to novel cyclopeptides of the formula Icyclo-(A-B-C-D-Arg) Iin whichA and B are each independently of one another Ala, Asn, Asp, Arg, Cys, Gln, Glu, Gly, His, Ile, Leu, Lys, Met, Phe, Pro, Ser, Thr, Trp, Tyr or Val;C is Asp or Asp(O--C.sub.1-4 -alkyl); andD is Gly or Ala;at least two of the amino acid radicals stated being present in the D-form;and their salts.These compounds act as integrin inhibitors and can be used in particular for the prophylaxis and treatment of disorders of the circulation and in tumor therapy.
    Type: Grant
    Filed: May 8, 1995
    Date of Patent: January 6, 1998
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Alfred Jonczyk, Gunter Holzemann, Brunhilde Felding-Habermann, Friedrich Rippmann, Guido Melzer, Beate Diefenbach
  • Patent number: 5627197
    Abstract: Compounds of the formula I ##STR1## wherein R.sup.1 and Y have the meanings indicated herein, and also their physiologically acceptable salts, inhibit the binding of fibrinogen to the corresponding receptor and can be employed for the treatment of thromboses, osteoporoses, oncoses, apoplexy, cardiac infarct, inflammations, arteriosclerosis and osteolytic disorders.
    Type: Grant
    Filed: February 14, 1996
    Date of Patent: May 6, 1997
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Joachim Gante, Horst Juraszyk, Peter Raddatz, Hanns Wurziger, Sabine Bernotat-Danielowski, Guido Melzer
  • Patent number: 5614531
    Abstract: Compounds of the formula I ##STR1## and the corresponding 5,6,7,8-tetrahydroimidazo[1,2-a]pyridine derivatives, their physiologically acceptable salts and/or solvates, inhibit the binding of fibrinogen to the corresponding receptor and can be used for the treatment of thromboses, osteoporosis, oncoses, stroke, myocardial infarct, inflammations, arteriosclerosis and osteolytic disorders.
    Type: Grant
    Filed: February 17, 1995
    Date of Patent: March 25, 1997
    Assignee: Merck Patent Gesellschaft Mit Beschrankter Haftung
    Inventors: Horst Juraszyk, Joachim Gante, Hanns Wurziger, Sabine Bernotat-Danielowski, Guido Melzer
  • Patent number: 5614535
    Abstract: Compounds of the formula I ##STR1## in which R.sup.1 and X have the meanings herein defined, their physiologically unobjectionable salts and/or solvates inhibit the binding of fibrinogen to the corresponding receptor and can be employed for the treatment of thromboses, osteoporosis, tumoral diseases, apoplexy, cardiac infarction, inflammations, arteriosclerosis and osteolytic disorders.
    Type: Grant
    Filed: August 18, 1995
    Date of Patent: March 25, 1997
    Assignee: Merck Patent Gesellschaft Mit Beschrankter Haftung
    Inventors: Horst Juraszyk, Joachim Gante, Hanns Wurziger, Sabine Bernotat-Danielowski, Guido Melzer
  • Patent number: 5561148
    Abstract: Novel oxazolidinone derivatives of the formula I ##STR1## in which R.sup.1 is a phenyl radical which is unsubstituted or is monosubstituted by CN, H.sub.2 N--CH.sub.2 --, A.sub.2 N--CH.sub.2 --, H.sub.2 N--C(.dbd.NH)--, H.sub.2 N--C(.dbd.NH)--NH--, H.sub.2 N--C(.dbd.NH)--NH--CH.sub.2 --, HO--NH--C(.dbd.NH)-- or HO--NH--C(.dbd.NH)--NH--,X is O, S, SO, SO.sub.2, --NH-- or --NA--,B is ##STR2## or ##STR3## A is alkyl having from 1 to 6 C atoms,R.sup.2 is H, A, Li, Na, K, NH.sub.4 or benzyl,R.sup.3 is H or (CH.sub.2).sub.n --COOR.sup.2,E is, in each case independently of each other, CH or N,Q is O, S or NH,m is 1, 2 or 3, andn is 0, 1, 2 or 3,and physiologically compatible salts thereof are provided, which inhibit the binding of fibrinogen to the corresponding receptor and can be used for treating thrombosis, stroke, cardiac infarction, inflammations, arteriosclerosis, osteoporosis and also tumors.
    Type: Grant
    Filed: September 22, 1994
    Date of Patent: October 1, 1996
    Assignee: Merck Patent Gesellschaft Mit Beshrankter Haftung
    Inventors: Joachim Gante, Horst Juraszyk, Peter Raddatz, Hanns Wurziger, Guido Melzer, Sabine Bernotat-Danielowski