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).
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Patent number: 7060706Abstract: 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 antagonistsType: GrantFiled: September 13, 2000Date of Patent: June 13, 2006Assignee: 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
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Patent number: 6890930Abstract: 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: GrantFiled: September 13, 2000Date of Patent: May 10, 2005Assignee: 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
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Patent number: 6602876Abstract: 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: GrantFiled: November 2, 1995Date of Patent: August 5, 2003Assignee: Merck Patent GmbHInventors: Joachim Gante, Horst Juraszyk, Peter Raddatz, Hanns Wurziger, Sabine Bernotat-Danielowski, Guido Melzer, Matthias Wiesner, Claus Fittschen
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Publication number: 20030135055Abstract: The invention relates to compounds of the formula I 1Type: ApplicationFiled: August 21, 2002Publication date: July 17, 2003Inventors: Dieter Dorsch, Horst Juraszyk, Werner Mederski, Christos Tsaklakidis, Sabine Bernotat-Danielowski, Guido Melzer, Johannes Gleitz, Christopher Barnes, James Vickers
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Patent number: 6492368Abstract: 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: GrantFiled: March 31, 2000Date of Patent: December 10, 2002Assignee: Merck Patent GmbHInventors: Dieter Dorsch, Hanns Wurziger, Guido Melzer, Horst Juraszyk, Sabine Bernotat-Danielowski
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Patent number: 6492384Abstract: 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: GrantFiled: December 13, 2001Date of Patent: December 10, 2002Assignee: Merck Patent GmbHInventors: Werner Mederski, Horst Juraszyk, Hanns Wurziger, Joachim Gante, Dieter Dorsch, Hans-Peter Buchstaller, Sabine Bernotat-Danielowski, Guido Melzer, Soheila Anzali
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Patent number: 6455529Abstract: 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: GrantFiled: May 3, 1996Date of Patent: September 24, 2002Assignee: Merck Patent Gesellschaft mit beschraenkter HaftungInventors: Joachim Gante, Hörst Juraszyk, Peter Raddatz, Hanns Wurziger, Sabine Bernotat-Danielowski, Guido Melzer
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Patent number: 6380430Abstract: 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: GrantFiled: December 29, 2000Date of Patent: April 30, 2002Assignee: Merck Patent Gesellschaft mit beschraenkterHaftungInventors: Dieter Dorsch, Horst Juraszyk, Werner Mederski, Joachim Gante, Hanns Wurziger, Hans-Peter Buchstaller, Sabine Bernotat-Danielowski, Guido Melzer
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Patent number: 6204280Abstract: 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: GrantFiled: September 30, 1998Date of Patent: March 20, 2001Assignee: Merck Patent Gesellschaft mit berschrankter HaftungInventors: Joachim Gante, Horst Juraszyk, Peter Raddatz, Hanns Wurziger, Sabine Bernotat-Danielowski, Guido Melzer, Matthias Wiesner, Claus Fittschen
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Patent number: 6028090Abstract: 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: GrantFiled: November 6, 1997Date of Patent: February 22, 2000Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Joachim Gante, Horst Juraszyk, Peter Raddatz, Hanns Wurziger, Guido Melzer, Sabine Bernotat-Danielowski
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Patent number: 5908843Abstract: 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: GrantFiled: January 31, 1994Date of Patent: June 1, 1999Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Joachim Gante, Peter Raddatz, Horst Juraszyk, Sabine Bernotat-Danielowski, Guido Melzer
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Patent number: 5866540Abstract: 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: GrantFiled: January 4, 1995Date of Patent: February 2, 1999Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Alfred Jonczyk, Gunter Holzemann, Brunhilde Felding-Habermann, Guido Melzer, Beate Diefenbach, David A. Cheresh, Horst Kessler, Marion Gurrath, Gerhard Muller
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Patent number: 5776937Abstract: 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: GrantFiled: November 7, 1995Date of Patent: July 7, 1998Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Joachim Gante, Horst Juraszyk, Peter Raddatz, Hanns Wurziger, Sabine Bernotat-Danielowski, Guido Melzer
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Patent number: 5723480Abstract: 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: GrantFiled: May 29, 1996Date of Patent: March 3, 1998Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Joachim Gante, Horst Juraszyk, Peter Raddatz, Hanns Wurziger, Guido Melzer, Sabine Bernotat-Danielowski
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Patent number: 5710131Abstract: 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: GrantFiled: February 28, 1995Date of Patent: January 20, 1998Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Jurgen Hemberger, Guido Melzer
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Patent number: 5705481Abstract: 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: GrantFiled: May 8, 1995Date of Patent: January 6, 1998Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Alfred Jonczyk, Gunter Holzemann, Brunhilde Felding-Habermann, Friedrich Rippmann, Guido Melzer, Beate Diefenbach
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Patent number: 5627197Abstract: 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: GrantFiled: February 14, 1996Date of Patent: May 6, 1997Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Joachim Gante, Horst Juraszyk, Peter Raddatz, Hanns Wurziger, Sabine Bernotat-Danielowski, Guido Melzer
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Patent number: 5614531Abstract: 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: GrantFiled: February 17, 1995Date of Patent: March 25, 1997Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Horst Juraszyk, Joachim Gante, Hanns Wurziger, Sabine Bernotat-Danielowski, Guido Melzer
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Patent number: 5614535Abstract: 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: GrantFiled: August 18, 1995Date of Patent: March 25, 1997Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Horst Juraszyk, Joachim Gante, Hanns Wurziger, Sabine Bernotat-Danielowski, Guido Melzer
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Patent number: 5561148Abstract: 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: GrantFiled: September 22, 1994Date of Patent: October 1, 1996Assignee: Merck Patent Gesellschaft Mit Beshrankter HaftungInventors: Joachim Gante, Horst Juraszyk, Peter Raddatz, Hanns Wurziger, Guido Melzer, Sabine Bernotat-Danielowski