Patents by Inventor Simon Goodman
Simon Goodman 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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Publication number: 20040092454Abstract: Novel biphenyl derivatives of the general formula (I) in which R1, R1′, R1″, R2, R2′, R3 and n are as defined in claim 1, their stereoisomers and their physiologically acceptable salts or solvates are novel integrin inhibitors which preferentially inhibit the &agr;v&bgr;6 integrin receptor. The novel compounds can be used, in particular, as medicaments.Type: ApplicationFiled: September 15, 2003Publication date: May 13, 2004Inventors: Oliver Schadt, Alfred Jonczyk, Wolfgang Stahle, Simon Goodman
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Publication number: 20040063644Abstract: 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 1, and physiologically acceptable salts or solvates thereof are integrin inhibitors and can be employed for combating thromboses, cardiac infarction, coronary heart disease, arteriosclerosis, inflammation, tumours. Osteoporosis, infections and restenosis after angioplasty or in pathological processes maintained or propagated by antiogenesis.Type: ApplicationFiled: June 18, 2003Publication date: April 1, 2004Inventors: Wolfgang Stahle, Alfred Joncyk, Oliver Schadt, Simon Goodman
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Publication number: 20040052785Abstract: The invention relates to a combination therapy for the treatment of tumors and tumor metastases comprising administration of receptor tyrosine kinase antagonists/inhibitors, especially ErbB receptor antagonists, more preferably EGF receptor (Her 1) antagonists and anti-angiogenic agents, preferably integrin antagonists, optionally together with agents or therapy forms that have additive or synergistic efficacy when administered together with said combination of antagonists/inhibitors, such as chemotherapeutic agents and or radiation therapy. The therapy can result in a synergistic potential increase of the inhibition effect of each individual therapeutic on tumor cell proliferation, yielding more effective treatment than found by administering an individual component alone.Type: ApplicationFiled: July 9, 2003Publication date: March 18, 2004Inventors: Simon Goodman, Hans-Georg Kreysch
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Patent number: 6683051Abstract: The invention relates to a pharmaceutical preparation [lacuna] 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.Type: GrantFiled: June 4, 2001Date of Patent: January 27, 2004Assignee: Merck Patent GmbHInventors: Alfred Jonczyk, Astrid Perschl, Simon Goodman, Sigrid Rösener, Jutta Haunschild
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Publication number: 20040010023Abstract: The invention relates to novel biphenyl derivatives of the general formula (I), wherein R4 represents an aromatic heterocycle, and to the physiologically acceptable salts or solvates thereof. The inventive compounds are integrin inhibitors and are used for combating thromboses, cardiac infarction, coronary heart diseases, arteriosclerosis, inflammations, tumors, osteoporosis, infections and restenosis following angioplasty or for pathological processes that are maintained or propagated by angiogenesis.Type: ApplicationFiled: February 21, 2003Publication date: January 15, 2004Inventors: Wolfgang Stahle, Gunter Holzemann, Simon Goodman
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Patent number: 6649613Abstract: Diacylhydrazine derivatives of general formula (I) wherein X, Y, Z, R1, 2 and R3 are as defined herein, and their physiologically acceptable salts or solvates thereof, are integrin inhibitors and can be used to combat thromboses, myocardial infarcts, coronary cardiac diseases, arteriosclerosis, inflammations, tumors, osteoporosis, infections, and restenosis following angioplasty or during pathological processes that are maintained or propagated by angiogenesis.Type: GrantFiled: January 14, 2002Date of Patent: November 18, 2003Assignee: Merck Patent GmbHInventors: Günter Hölzemann, Simon Goodman, Horst Kessler, Christoph Gibson, Gabór Sulyok
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Patent number: 6645991Abstract: The invention describes novel compounds of the formula I which are biologically active as ligands of integrin &agr;v&bgr;3 X—Y—Z—R1—CH2—R2(R4)—CH2—CO—R5 in which X, Y, Z, R1, R2, R4 and R5 are as defined in claim 1, and their physiologically acceptable salts and solvates.Type: GrantFiled: June 21, 2002Date of Patent: November 11, 2003Assignee: Merck Patent GmbHInventors: Alfred Jonczyk, Oliver Schadt, Simon Goodman
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Publication number: 20030187289Abstract: Novel biphenyl derivatives of the general formula (I), in which Y, R R1, R2, R3, R4, m, o and p are as defined in claim 1, and their physiologically acceptable salts and solvates are integrin inhibitors and can be employed for combating thrombosis, cardiac infarction, coronary heart disease, arteriosclerosis, inflammation, tumours, osteoporosis, infections aid restenosis after angioplasty or in pathological processes which are maintained or propagated by angiogenesis.Type: ApplicationFiled: February 21, 2003Publication date: October 2, 2003Inventors: Wolfgang Stahle, Simon Goodman
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Publication number: 20030143157Abstract: 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.Type: ApplicationFiled: July 31, 2002Publication date: July 31, 2003Inventors: Sally J. DeNardo, Patricia A. Burke, Gerald L. DeNardo, Simon Goodman, Siegfried Matzku
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Patent number: 6534478Abstract: Compounds of the formula I cyclo-(aArg-aGly-aAsp-aX-aY) I in which aArg, aGly, aAsp, aX and aY have the meanings indicated in claim 1, and their salts, can be used as integrin inhibitors, in particular for the prophylaxis and treatment of diseases of the circulation, in thrombosis, cardiac infarct, coronary heart diseases, arteriosclerosis, in pathological processes which are supported or propagated by angiogenesis and in tumour therapy.Type: GrantFiled: March 23, 2000Date of Patent: March 18, 2003Assignee: Merck Patent Gesellschaft MitInventors: Alfred Jonczyk, Simon Goodman, Horst Kessler, Jochen Wermuth, Jörg Schmitt
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Publication number: 20030045728Abstract: Indol-3-yl derivatives of the general formula I 1Type: ApplicationFiled: August 9, 2002Publication date: March 6, 2003Inventors: Matthias Wiesner, Simon Goodman, Rudolf Gottschlich
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Patent number: 6521646Abstract: Compounds of the formula (I) and their physiologically acceptable salts and solvates are useful as integrin-inhibiting substances. They are especially useful in the prophylaxis and treatment of cardiovascular disorders, of thrombosis, cardiac infarction, coronary heart diseases, arteriosclerosis, osteoporosis, in pathological conditions that are caused or propagated by angiogenesis and in tumor therapy.Type: GrantFiled: October 15, 2001Date of Patent: February 18, 2003Assignee: Merck Patent GmbHInventors: Wolfgang Stähle, Rudolf Gottschlich, Simon Goodman
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Publication number: 20020169680Abstract: A method and apparatus for distributed computing in a network data processing system. A task is accepted for distributed computing. Work units are sent to a plurality of data processing systems on a network, wherein each data processing system within the plurality of data processing systems includes a software for accepting a work unit, processing the work unit to generate a result, and returning the result, wherein the software is monitored for compliance with an operation policy requiring a connection to the network and allocating a period of time for processing work units. Results are received from the plurality of data processing systems. These data processing systems may be individually owned by consumers in which the systems are provided at no cost or some lower cost in return for making available processing resources for processing work units.Type: ApplicationFiled: May 10, 2001Publication date: November 14, 2002Applicant: International Business Machines CorporationInventors: Craig Henry Becker, Robert Simon Goodman, Stewart Earle Nickolas, Wayne Elmo Vicknair
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Patent number: 6333308Abstract: Compounds of the formula I cyclo-(Arg-X-Asp-R1) I in which X is Gly, Ala or NH—NH—CO, R1 is a radical of the formula II and R2,R3 and R4 have the meanings indicated in claim 1, and their salts, can be used as integrin inhibitors, in particular for the prophylaxis and treatment of disorders of the circulation, in thrombosis, cardiac infarct, coronary heart disorders, arteriosclerosis, in pathological processes which are supported or propagated by angiogenesis and in tumour therapy.Type: GrantFiled: October 7, 1999Date of Patent: December 25, 2001Assignee: Merck KGaAInventors: Gunter Holzemann, Claus Fittschen, Simon Goodman
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Patent number: 6326403Abstract: Compounds of the formula I wherein X, Y, Z, R1 and R2 are as defined in claim 1, and their salts and solvates, can be used as integrin inhibitors in particular for the prophylaxis and treatment of circulatory disorders, for thrombosis, cardiac infarction, coronary heart diseases, arteriosclerosis, for pathological processes which are maintained or propagated by angiogenesis and in tumour therapy.Type: GrantFiled: January 12, 2001Date of Patent: December 4, 2001Assignee: Merck Patent Gesellschaft mitInventors: Günter Hölzemann, Simon Goodman, Horst Kessler, Christoph Gibson, Jörg Simon Schmitt
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Patent number: 6127335Abstract: The invention concerns cyclopeptides of formula (I): Cyclo-(Arg-Gly-Asp-X-Y) in which X is Cha, Nal, Phe, 2-R.sup.1 -Phe, 3-R.sup.1 -Phe, 4-R.sup.1 -Phe, homo-Phe, Phg, Thi, Trp, Tyr or derivatives of Tyr, whereby the OH group can be etherified by alkyl groups containing 1-18 C-atoms and the amino-acid groups given can also be derivatives, R.sup.1 is NH.sub.2, NO.sub.2, I Br, Cl, F, alkyl with 1-18 C-atoms, Ar, Ar--O or.sup.3 H, Y is Gly in which the .alpha. N-atom may be substituted by R.sup.2 and/or the .alpha. C-atom may be substituted by R.sup.3 and/or R.sup.4, with the provision that Gly has at least one of the substituents specified, Ar is phenyl which may be substituted by one or two of groups NH.sub.2, NO.sub.2, I, Br, Cl, F, alkyl with 1-6 C-atoms or .sup.3 H, R.sup.2, R.sup.3 or R.sup.4, independently of each other, are alkyl with 1-18 C-atoms or R.sup.2 and R.sup.3 or R.sup.3 and R.sup.4 together in each case are a branched or unbranched alklyene chain with 3 to 18 C-atoms so that either the .Type: GrantFiled: April 8, 1999Date of Patent: October 3, 2000Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Alfred Jonczyk, Simon Goodman, Beate Diefenbach, Horst Kessler, Marcus Koppitz
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Patent number: 6001961Abstract: The invention relates to novel cyclopeptides of the formula Icyclo-(nArg-nGly-nAsp-nD-nE) I,in whichD and E in each case independently of one another are Gly, Ala, .beta.-Ala, Asn, Asp, Asp(OR), Arg, Cha, Cys, Gln, Glu, His, Ile, Leu, Lys, Lys(Ac), Lys(AcNH.sub.2), Lys(AcSH), Met, Nal, Nle, Orn, Phe, 4-Hal-Phe, homo-Phe, Phg, Pro, Pya, Ser, Thr, Tia, Tic, Trp, Tyr or Val, which amino acid residues can also be derivatized,R is alkyl having 1-18 carbon atoms,Hal is F, Cl, Br, I,Ac is alkanoyl having 1-10 carbon atoms, aroyl having 7-11 carbon atoms or aralkanoyl having 8-12 carbon atoms,n denotes no substituent or an alkyl radical R, benzyl or an aralkyl radical having 7-18 carbon atoms on the alpha-amino function of the relevant amino acid residue,with the proviso that at least one amino acid residue has a substituent n and that, where residues of optically active amino acids and amino acid derivatives are involved, both the D and the L forms are included, and also their physiologically acceptable salts.Type: GrantFiled: September 16, 1996Date of Patent: December 14, 1999Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Alfred Jonczyk, Simon Goodman, Beate Diefenbach, Arne Sutter, Gunter Holzemann, Horst Kessler, Michael Dechantsreiter
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Patent number: 5985278Abstract: The invention relates to a novel monoclonal antibody, a hybridoma cell line producing said antibody, DNA sequences coding for said antibody, and amino acid sequences. The monoclonal antibody, a preferred embodiment of which is named 17E6, has the following properties:reacting only with the .alpha.V-chain of human .alpha.V-integrins,blocking the attachment to the integrin substrate of the .alpha.V-integrin bearing cell,triggering reversal of established cell matrix interaction caused by .alpha.V-integrins,blocking tumor development, andshowing no cytotoxic activity.Type: GrantFiled: December 19, 1995Date of Patent: November 16, 1999Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Francesc Mitjans, Jaume Piulats, Elisabet Rosell, Jaume Adan, Simon Goodman, Diane Hahn
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Patent number: 5693612Abstract: The invention relates to novel cyclopeptides of the formula Icyclo-(Arg-A-Asp-R.sup.1 -R.sup.2) Iin whichA, R.sup.1 and R.sup.2 have the meaning given in claim 1, 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, bones and in tumour therapy, and as antimicrobial and antiviral active compounds.Type: GrantFiled: April 28, 1995Date of Patent: December 2, 1997Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Alfred Jonczyk, Gunter Holzemann, Simon Goodman, Horst Kessler, Roland Haubner, Jochen Wermuth