Merck Patent Gmbh

Merck Patent Gesellschaft MIT Beschrankter Haftung

Merck Patent Gesellschaft MIT

University of California

Merck Patent Gesellschaft

Merck Kgaa

Simon Lawrence Goodman

Alfred Jonczyk

Horst Kessler

Beate Diefenbach

Oliver Schadt

Matthias Wiesner

Francesc Mitjans

Wolfgang Staehle

Gunter Holzemann

Rudolf Gottschlich

Peter Raddatz

Claudia Wilm

Jaume Adan

Diane Hahn

G&uuml;nter H&ouml;lzemann

J&ouml;rg Simon Schmitt

Arne Sutter

Kin-Ming Lo

Marcus Koppitz

Christiane Amendt

Sally Joan Denardo

Matthias Grell

Christoph Gibson

Jochen Wermuth

Gerald Louis Denardo

Friedrich Rippmann

Claus Fittschen

Klaus Duecker

Jutta Haunschild

Jaume Piulats

Elisabet Rosell

Roland Haubner

Burkhard Scharm

Joachim M&auml;rz

Marcus Eber

Wolfgang St&auml;hle

Patricia A Burke

Michael Dechantsreiter

Alex Brown

Georgette Thumshirn

Dirk Weber

Tom Mikkelsen

Dirk Gottschling

Wolfgang Stähle

Gab&oacute;r Sulyok

Detelv Güssow

Joerg Hoheisel

Kerstin Matzku, Legal Representative

Eilish Cullen

Raj Mehta

Joachim März

Sigrid R&ouml;sener

Astrid Perschl

Marcus Frohme

Andreas Harstrick

Ulrike Grimm

Michael Weller

Stefan Krueger

Michael Prof Weller

Johannes Nippgen

Roger Stupp

Curzio Ruegg

Martin Andreas Picard

The present invention relates to a pharmaceutical composition of oligopeptides, preferably cyclic oligopeptides, said composition further comprising one or more lipophilic and/or amphiphilic compounds, in the presence or absence of water as the main ingredients, the use of the lipophilic and/or amphiphilic compounds for making pharmaceutical compositions of said oligopeptides, and methods of making said pharmaceutical composition.

Method of treating disorders using a pharmaceutical composition of oligopeptides

The invention relates to antibodies that are capable to bind the extracellular domain of integrin. Another object of the invention concerns the use of said antibodies for detecting integrins in archival formalin fixed paraffin embedded (FFPE) tissue. The invention also relates to methods for preparing monoclonal rabbit antibodies, wherein the immunogen is an insect expression culture-derived recombinant extracellular integrin domain, and another method for screening anti-integrin antibodies that discriminate between closest integrin homologues and that are especially suited for immunohistochemistry in FFPE material.

Antibodies for the detection of integrin complexes in FFPE material

The invention relates to engineered antibodies which specifically bind to integrin receptors, especially the alpha V integrin receptor subunit. The antibodies comprise the antigen binding sites (CDRs) of a known mouse anti-integrin antibody, as well as hybrid light chain variable sequences, mutated heavy chain variable sequences (Frs) and modified heavy chain constant sequences. The novel antibodies have improved immunogenic and expression properties and elicit excellent anti-angiogenic as well as anti-tumor activities in humans in monotherapy but also and above all in combination with other angiogenesis and tumor inhibiting agents.

Engineered anti-alpha V-integrin hybrid antibodies

The invention relates to a novel purified recombinant &#x3b1;&#x3b2;adhesion receptor which shows an unimpaired ligand binding activity, and a process for preparing said soluble non-membrane bound receptor in excellent yields by recombinant techniques using a baculovirus-insect cell expression system. The so-synthesized soluble receptor may be used very easily as screening tool for new therapeutic compounds which may inhibit the natural &#x3b1;&#x3b2;adhesion receptor. Such therapeutic compounds which can be discovered very easily, fast and without health risk by means of the soluble receptors according to the invention may be, for example, RGD peptides or non-peptidic compounds mimicking the natural ligand epitopes. The invention relates, furthermore, to a corresponding process for preparing recombinant full-length &#x3b1;&#x3b2;adhesion receptor in excellent yields, additionally using detergents to dissolve the membrane bound receptor from the surface of the host cell.

[object Object]

Novel biphenyl derivatives of the general formula (I) in which R, R, R, R, R, Rand n are as defined in claim 1, their stereoisomers and their physiologically acceptable salts or solvates are novel integrin inhibitors which preferentially inhibit the &#x3b1;&#x3b2;integrin receptor. The novel compounds can be used, in particular, as medicaments. 

Novel biphenyl derivatives of the general formula I in which R, R, R, R, R, R3 and n are as defined in Patent claim, stereoisomers thereof and physiologically acceptable salts or solvates thereof are novel integrin inhibitors which preferentially inhibit the &#x3b1;&#x3b2;integrin receptor. The novel compounds can be used, in particular, as medicaments 

Novel urea and urethane derivatives of general formula (I) in which R1, R2, R3, R5, R5', X, Y, B, m, n and o are as defined in Patent Claim, and physiologically acceptable salts or solvates thereof are integrin inhibitors and can be employed for combating thromboses, cardiac infarction, coronary heart disease, arteriosclerosis, inflammation, tumors. Osteoporosis, infections and restenosis after angioplasty or in pathological processes maintained or propagated by antiogenesis.

Urea and urethane derivatives as integrin inhibitors

HUTUDO1 polypeptides and polynucleotides and methods for producing such polypeptides by recombinant techniques are disclosed. Also disclosed are methods utilizing HUTUDO1 polypeptides and polynucleotides in diagnostic assays.

Identification of a human N-terminal acetyltransferase gene

Isoquinoline derivatives of the general formula (I) in which X, Y, Z, R, Rand n are as defined in Patent Claim (), and physiologically acceptable salts or solvates thereof, are integrin inhibitors and can be employed for combating thromboses, cardiac infarction, coronary heart diseases, arteriosclerosis, inflammation, tumors, osteoporosis, infections and restenosis after angioplasty or in pathological processes which are maintained or propagated by angiogenesis.

Isoquinoline derivatives

ERK-7 polypeptides and polynucleotides and methods for producing such polypeptides by recombinant techniques are disclosed. Also disclosed are methods for utilizing ERK-7 polypeptides and polynucleotides in diagnostic assays.

Human extracellular signal regulated kinases

A method of treating tumors, such as prostate tumors, breast tumors, non-Hodgkin's lymphoma, and the like, includes the sequential steps of administering to the patient at least one dose of an antiangiogenic cyclo-arginine-glycine-aspartic acid-containing pentapeptide (cRGD pentapeptide); administering to the patient an anti-tumor effective amount of a radioimmunotherapeutic agent (RIT); and then administering to the patient at least one additional dose of cRGD pentapeptide. The cRGD pentapeptide is preferably cyclo-(Arg-Gly-Asp-D-Phe-[N-Me]-Val), and the RIT is preferably a radionuclide-labeled chelating agent-ligand complex in which chelating agent is chemically bonded to a tumor-targeting molecule, such as a monoclonal antibody.

Method of treating tumors

 The invention relates to compounds having formula (I), wherein R, R, R, R, R, R, R, R, Z, m and n have the meaning cited in claim 1, and to the physiologically acceptable salts and solvates which can be used as integrin inhibitors, especially in the prophylaxis and treatment of circulatory diseases, in case of thrombosis, myocardial infarction, coronary heart diseases, arteriosclerosis, osteoporosis, pathologic processes caused or propagated by angiogenesis and in tumor therapy.

Chromenone and chromanone derivatives as integrin inhibitors

Indol-3-yl derivatives

The invention relates to a pharmaceutical preparation &lsqb;lacuna&rsqb; cyclo(Arg-Gly-Asp-D-Phe-NMe-Val) and/or one of its physiologically acceptable salts and at least one chemotherapeutic agent and/or one of its physiologically acceptable salts and/or an angiogenesis inhibitor and/or one of its physiologically acceptable salts.

Pharmaceutical preparation containing a cyclopeptide and a chemotherapeutic agent or an angiogenesis inhibitor

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Darmstadt, Germany

Simon Lawrence Goodman