Cyclic Peptide Or Cyclic Protein (see Note 8) Patents (Class 930/270)
  • Patent number: 8188216
    Abstract: A library of macrocyclic compounds of the formula (I) where part (A) is a bivalent radical, a —(CH2)y— bivalent radical or a covalent bond; where part (B) is a bivalent radical, a —(CH2)z— bivalent radical, or a covalent bond; where part (C) is a bivalent radical, a —(CH2)t- bivalent radical, or a covalent bond; and where part (T) is a -Y-L-Z- radical wherein Y is CH2 or CO, Z is NH or O and L is a bivalent radical. These compounds are useful for carrying out screening assays or as intermediates for the synthesis of other compounds of pharmaceutical interest. A process for their preparation of these compounds in a combinatorial manner, is also disclosed.
    Type: Grant
    Filed: October 7, 2004
    Date of Patent: May 29, 2012
    Assignee: Tranzyme Pharma Inc.
    Inventors: Pierre Deslongchamps, Yves Dory, Gilles Berthiaume, Luc Ouellet, Ruoxi Lan
  • Patent number: 8008440
    Abstract: A library of macrocyclic compounds of the formula (I) where part (A) is a ?bivalent radical, a —(CH2)y— bivalent radical or a covalent bond; where part (B) is a ?bivalent radical, a —(CH2)z— bivalent radical, or a covalent bond; where part (C) is a ?bivalent radical, a —(CH2)t— bivalent radical, or a covalent bond; and where part (T) is a —Y-L-Z- radical wherein Y is CH2 or CO, Z is NH or O and L is a bivalent radical. These compounds are useful for carrying out screening assays or as intermediates for the synthesis of other compounds of pharmaceutical interest. A process for the preparation of these compounds in a combinatorial manner, is also disclosed.
    Type: Grant
    Filed: December 22, 2006
    Date of Patent: August 30, 2011
    Assignee: Tranzyme Pharma Inc.
    Inventors: Pierre Deslongchamps, Yves Dory, Gilles Berthiaume, Luc Ouellet, Ruoxi Lan
  • Patent number: 7345020
    Abstract: The application concerns a method of identifying compounds that can be used to inhibit undesired human CD4+ T cell immune responses by identifying compounds that block the interaction of CD4 and MHC, class II, gene products and a method of treatment which comprises administering such an identified compound. The compounds that inhibit undesired human CD4+ T cell immune responses can be used to treat disease such as multiple sclerosis and to prevent graft rejection and graft versus host disease. More specifically, the application concerns compounds having molecular weights between about 1400 and 400 that mimic three portions of the human CD4 lymphocyte cell surface antigen. The portions are residues 29-35, the C—C? loop of the D1 domain; residues 317-323, the C—C? loop of the D4 domain; and residues 346-353, the CDR3 or FG ridge of the D4 domain of the CD4 molecule. Specific examples of such compounds include cyclic peptides and peptidomimetic.
    Type: Grant
    Filed: May 7, 2004
    Date of Patent: March 18, 2008
    Assignee: Thomas Jefferson University
    Inventors: Robert Korngold, Ziwei Huang
  • Patent number: 7285534
    Abstract: This invention provides members of the corticiotropin-releasing hormone superfamily and peptide analogs thereof wherein the 38th amino acid from the N-terminus is D-Nle, i.e. [D-Nle38]-CRH peptide. The peptide analogs can be used to treat proliferative disorders of the skin such as melanoma.
    Type: Grant
    Filed: December 6, 2004
    Date of Patent: October 23, 2007
    Assignee: The Regents of the University of California
    Inventors: Edward Wei, Kurt Carlson
  • Patent number: 7214768
    Abstract: This invention relates to an improved process for the minimization of acid-catalyzed reactions of certain echinocandins of the kind disclosed in U.S. Pat. No. 5,378,804. The process involves the use of a boronic acid.
    Type: Grant
    Filed: April 8, 2002
    Date of Patent: May 8, 2007
    Assignee: Merck & Co., Inc.
    Inventors: Kevin M. Belyk, William R. Leonard
  • Patent number: 7192920
    Abstract: A subject of the invention, in all possible isomer forms as well as their mixtures, is the compounds of formula (I): in which either R1: H or CH3 and R2: cyclohexyl substituted by an amine, a (CH2)b-C?N radical or R1 and R2 together with the nitrogen which carries them form a ring with 3, 4 or 5 carbons optionally substituted by an amine R3: hydrogen, methyl or hydroxyl R4: hydrogen or hydroxyl R: represents a linear, branched or cyclic chain T: hydrogen, methyl, CH2CONH2, CH2C?N, a (CH2)2NH2 or (CH2)2Nalk+X? radical, X halogen and alk alkyl Y: hydrogen, hydroxyl, halogen or OSO3H, W: H or OH, Z: H, CH3. The compounds of formula (I) have antifungal properties.
    Type: Grant
    Filed: September 13, 2005
    Date of Patent: March 20, 2007
    Assignee: Aventis Pharma SA
    Inventors: Patrick Fauveau, Stephen Hawser, Gilles Lebourg, Laurent Schio
  • Patent number: 7022669
    Abstract: A subject of the invention, in all possible isomer forms as well as their mixtures, is the compounds of formula (I): in which either R1: H or CH3 and R2: cyclohexyl substituted by an amine, a (CH2)b-C?N radical or R1 and R2 together with the nitrogen which carries them form a ring with 3, 4 or 5 carbons optionally substituted by an amine R3: hydrogen, methyl or hydroxyl R4: hydrogen or hydroxyl R: represents a linear, branched or cyclic chain T: hydrogen, methyl, CH2CONH2, CH2C?N, a (CH2)2NH2 or (CH2)2Nalk+X? radical, X halogen and alk alkyl Y: hydrogen, hydroxyl, halogen or OSO3H, W: H or OH, Z: H, CH3. The compounds of formula (I) have antifungal properties.
    Type: Grant
    Filed: June 8, 2000
    Date of Patent: April 4, 2006
    Assignee: Aventis Pharma S.A.
    Inventors: Patrick Fauveau, Stephen Hawser, Gilles Lebourg, Laurent Schio
  • Patent number: 6943233
    Abstract: Cyclic peptides which comprise, as a constituent chain or chains thereof, one or two amino acid sequences selected from the amino acid sequence Asn-Val-Ser-Glu-Ala-Asp-Asp-Arg-Tyr-Ile and the amino acid sequence Arg-Ser-Gln-Lys-Glu-Gly-Leu-His-Tyr-Thr, and AIDS vaccines containing at least one of the cyclic peptides as an active ingredient. From the in vivo absorption and antibody expression viewpoint, a substituent group is preferably bound to at least one active group selected from among the carboxyl, amino and hydroxyl groups contained in the cyclic peptides. The cyclic peptides can neutralize the second receptors which the HIV-1 virus utiliizes in the infection of humans therewith.
    Type: Grant
    Filed: October 28, 1999
    Date of Patent: September 13, 2005
    Assignee: Nissui Pharmaceutical Co., Ltd.
    Inventor: Shozo Shoji
  • Patent number: 6902720
    Abstract: The present invention discloses a family of cyclic peptide monomers and supramolecular cyclic peptide structures comprising chromophore residues which possess electronic and electro-optic properties for producing molecular scale electronic and photonic devices made from such materials. More particularly, this invention provides for cyclic peptide nanotube structures formed from a plurality of stacked cyclic peptides comprising chromophore residues that provide molecular scale electronic conductivity and non linear optical behavior. The stackable cyclic peptide is represented by the general formula where R1 is H, CH3 or alkyl; where at least one R2 is a chromophore; where R3 is H, CH3 or a polar or non-polar organic functional group used for controlling peptide stacking and solubility; where n equals 1 or 2; where m equals 4 or 6; and where a first adjacent amino acid residue has an ?-carbon chirality of L and a second adjacent amino acid residue has an ?-carbon chirality of D.
    Type: Grant
    Filed: May 10, 2002
    Date of Patent: June 7, 2005
    Assignee: Worcester Polytechnic Institute
    Inventor: William Grant McGimpsey
  • Patent number: 6849600
    Abstract: This invention relates to peptide analogs of corticotropin-releasing hormone. Particularly, the invention provides analogs wherein the 38th amino acid from the N-terminus is D-Nle, i.e. [D-Nle38]-CRH peptide.
    Type: Grant
    Filed: March 25, 2002
    Date of Patent: February 1, 2005
    Assignee: The Regents of the University of California, Berkeley
    Inventors: Edward T. Wei, Kurt W. Carlson
  • Patent number: 6809177
    Abstract: The invention relates to a process for the conversion of echinocandin class of peptides to their C4-homotyrosine monodeoxy analogues, particularly mulundocandin to deoxymulundocandin, which consists of a single step selective reduction of C4-htyr (homotyrosine) hydroxyl group of echinocandins to their monodeoxy analogues under neutral conditions without prior protection/deprotection of the equally facile C5-Orn (ornithine) hydroxyl group and purification of the monodeoxy compound from the crude reaction mixture.
    Type: Grant
    Filed: March 29, 2001
    Date of Patent: October 26, 2004
    Assignee: Aventis Pharma Deutschland GmbH.
    Inventors: Triptikumar Mukhopadhyay, Kenia Jayvanti, Erra Koteswara Satya Vijaya Kumar
  • Patent number: 6750321
    Abstract: Peptides are provided that inhibit the interaction of an IGF with any one of its binding proteins and not to a human IGF receptor. These IGF agonist peptides are useful to increase serum and tissue levels of active IGFs in a mammal.
    Type: Grant
    Filed: November 27, 2000
    Date of Patent: June 15, 2004
    Assignee: Genentech, Inc.
    Inventors: Yvonne Man-yee Chen, Ross G. Clark, Andrea G. Cochran, Henry B. Lowman, Iain C. A. F. Robinson, Nicolas J. Skelton
  • Patent number: 6495661
    Abstract: An isolated nucleic acid molecule encoding the outer membrane protein of Pasteurella multocida is provided. Also provided are methods to detect the presence of the nucleic acid molecule, and antibodies specific for the polypeptide encoded by the nucleic acid molecule, in a sample. Further provided are immunogenic compositions comprising the outer membrane polypeptide or protien of Pasteurella multocida, or portions thereof.
    Type: Grant
    Filed: July 21, 1998
    Date of Patent: December 17, 2002
    Assignee: University of Georgia Research Foundation, Inc.
    Inventors: John Robert Glisson, Yugang Luo
  • Patent number: 6420518
    Abstract: Peptides are provided that inhibit the interaction of an IGF with any one of its binding proteins and not to a human IGF receptor. These IGF agonist peptides are useful to increase serum and tissue levels of active IGFs in a mammal.
    Type: Grant
    Filed: June 22, 1999
    Date of Patent: July 16, 2002
    Assignees: Genetech, Inc.
    Inventors: Yvonne Man-yee Chen, Ross G. Clark, Andrea G. Cochran, Henry B. Lowman, Iain C. A. F. Robinson, Nicholas J. Skelton
  • Patent number: 6054556
    Abstract: Cyclic lactam peptides are disclosed which inhibit at various levels of antagonism the melanocortin 1 receptor (MC1R), melanocortin 3 receptor (MC3R), melanocortin 4 receptor (MC4R), and Melanocortin 4 receptor (MC5R).
    Type: Grant
    Filed: November 28, 1997
    Date of Patent: April 25, 2000
    Assignee: The Arizona Board of Regents on Behalf of the University of Arizona
    Inventors: Victor J. Huby, Sejin Lim, Wei Yuan
  • Patent number: 6013626
    Abstract: A cryptophycin compound is provided having the structure: ##STR1## Further provided are methods of producing cryptophycins by total synthesis and methods of using cryptophycins in pharmaceuticals. It is a further object of this invention to use cryptophycins to inhibit the proliferation of mammalian cells. Moreover, methods of using cryptophycins to treat neoplasia is also provided.
    Type: Grant
    Filed: March 7, 1995
    Date of Patent: January 11, 2000
    Assignees: The University of Hawaii, Wayne State University
    Inventors: Richard E. Moore, Marcus A. Tius, Russell A. Barrow, Jian Liang, Thomas H. Corbett, Frederick A. Valeriote, Trimurtulu Golakoti, Thomas K. Hemscheidt
  • Patent number: 5955423
    Abstract: A cryptophycin compound is provided having the structure: ##STR1## Further provided are methods for producing novel cryptophycins from the Nostoc sp. of blue-green algae (cyanobacteria). Pharmaceutical compositions comprising novel cryptophycins are also provided, as are methods for using cryptophycins to inhibit the proliferation of hyperproliferative cells. Further provided are methods for using cryptophycins to inhibit the proliferation of hyperproliferative cells with drug resistant phenotypes, and to treat pathological conditions, such as neoplasia.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: September 21, 1999
    Assignees: The University of Hawaii, Wayne State University
    Inventors: Richard E. Moore, Charles D. Smith, Gregory M. L. Patterson, Susan L. Mooberry, Thomas H. Corbett, Frederick A. Valeriote, Trimurtulu Golakoti
  • Patent number: 5952298
    Abstract: A cryptophycin compound is provided having the structure: ##STR1## Further provided are methods for producing novel cryptophycins from the Nostoc sp. of blue-green algae (cyanobacteria). Pharmaceutical compositions comprising novel cryptophycins are also provided, as are methods for using cryptophycins to inhibit the proliferation of hyperproliferative cells. Further provided are methods for using cryptophycins to inhibit the proliferation of hyperproliferative cells with drug resistant phenotypes, and to treat pathological conditions, such as neoplasia.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: September 14, 1999
    Assignees: The University Of Hawaii, Wayne State University
    Inventors: Richard E. Moore, Charles D. Smith, Gregory M.L. Patterson, Susan L. Mooberry, Thomas H. Corbett, Frederick A. Valeriote, Trimurtulu Golakoti
  • Patent number: 5869448
    Abstract: The present invention contemplates a cyclic peptide that inhibits the binding between the VLA-4 receptor expressed on inflammatory leukocytes and the fibronectin CS-1 peptide expressed on endothelial cells that are involved in immunoinflammatory disease states. Pharmaceutical compositions containing a contemplated cyclic peptide and processes for treating immunoinflammatory conditions using a binding-inhibitory cyclic peptide are also disclosed.
    Type: Grant
    Filed: August 25, 1995
    Date of Patent: February 9, 1999
    Assignee: Cytel Corporation
    Inventors: Thomas S. Arrhenius, Anna Tempczyk, Mariano J. Elices, Zhong-Li Zheng
  • Patent number: 5834586
    Abstract: Dehydrodidemnin B with useful biological activity has formula (1). It can be isolated from natural sources or synthesized, and it forms active derivatives.
    Type: Grant
    Filed: July 25, 1994
    Date of Patent: November 10, 1998
    Assignee: Pharma Mar, S.A.
    Inventors: Kenneth L. Rinehart, Anna M. Lithgow-Bertelloni
  • Patent number: 5792746
    Abstract: Ceretain aza cyclohexapeptide compounds have been found to have superior antibiotic properties. Novel processes for their preparation are also described.
    Type: Grant
    Filed: October 28, 1996
    Date of Patent: August 11, 1998
    Assignee: Merck & Co., Inc.
    Inventors: James M. Balkovec, Frances Aileen Bouffard, Regina M. Black
  • Patent number: 5786325
    Abstract: Provided are pharmaceutical formulations, and methods of inhibiting fungal and parasitic activity using a compound of formula I ##STR1## where: R', R", R'", R.sup.x1, R.sup.x2, R.sup.y1, R.sup.y2, R.sup.y3, R.sup.y4, and R.sup.0 are as defined above; andR.sup.2 is ##STR2## each R.sup.2a is independently hydroxy, halo, nitro, amino, trifluoromethyl, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy or C.sub.1 -C.sub.6 alkylthio;a is 1, 2, 3 or 4;R.sup.3 is C.sub.1 -C.sub.12 alkyl, C.sub.1 -C.sub.12 alkoxy or --O--(CH.sub.2).sub.m --?O--(CH.sub.2).sub.n !.sub.p --O--(C.sub.1 -C.sub.12 alkyl);m is 2, 3 or 4;n is 2, 3 or 4; andp is 0 or 1;or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 11, 1996
    Date of Patent: July 28, 1998
    Assignee: Eli Lilly and Company
    Inventors: Peter S. Borromeo, William W. Turner, Jr.
  • Patent number: 5777073
    Abstract: Novel cyclic CRF antagonist peptides are created by shortening the N-terminus of a CRF family peptide by 8-11 residues and adding an acyl group. CML is preferably present in what would be the 27-position of the native CRF sequence, and D-Tyr may be incorporated at the N-terminus to facilitate labelling. The cyclizing bond is preferably created between the side chains of the residues in positions 30 and 33; but it may alternatively be created between the residues in either of positions 28 and 29 with those in positions 31 and 32 or with those in positions 32 and 33, respectively. The side chain of Lys in position 33 is preferably linked to the side chain of Glu in position 30 by a lactam bridge to form the cyclic peptide. Disclosed CRF antagonists include:(cyclo 30-33) ?Ac-Asp.sup.9, D-Phe.sup.12, Nle.sup.21,38, CML.sup.27,40, Glu.sup.30, Lys.sup.33 !r/hCRF(9-41),(cyclo 30-33) ?Ac-Asp.sup.9, D-Phe.sup.12, Nle.sup.21,38, CML.sup.27,37, Glu.sup.30, Lys.sup.33 !r/hCRF(9-41),(cyclo 30-33) ?Ac-Asp.sup.9, D-Phe.sup.
    Type: Grant
    Filed: May 30, 1997
    Date of Patent: July 7, 1998
    Assignee: The Salk Institute for Biological Studies
    Inventor: Jean E. F. Rivier
  • Patent number: 5773411
    Abstract: This invention relates to novel cyclic compounds linked by a heterocyclic ring system, which are useful as antagonists of the platelet glycoprotein IIb/IIIa complex, to pharmaceutical compositions containing such cyclic compounds, and to methods of using these compounds for the inhibition of platelet aggregation. A representative compound of the invention is cyclo-(D-Val-N(Me)Arg-Gly-Asp-?5-aminomethyl!-2-furoate).
    Type: Grant
    Filed: November 14, 1994
    Date of Patent: June 30, 1998
    Assignee: The DuPont Merck Pharmaceutical Company
    Inventors: Gregory James Wells, John Wityak, Anju Parthasarathy, William Frank DeGrado, Sharon Anne Jackson, Shaker Ahmed Mousa
  • Patent number: 5767069
    Abstract: Nonimmunosuppressant cyclosporin derivatives having cyclophilin-binding activity, for example, the compound, ?MeIle!.sup.4 -ciclosporin, are useful in inhibiting HIV-1 replication in treating AIDS and AIDS related disorders.
    Type: Grant
    Filed: April 24, 1995
    Date of Patent: June 16, 1998
    Assignee: Novartis AG
    Inventors: Soo Young Ko, Hans Kobel, Brigitte Besemer-Rosenwirth, Dieter Seebach, Rene P. Traber, Roland Wenger, Pietro Bollinger
  • Patent number: 5736509
    Abstract: Cyclic peptides and pharmaceutically acceptable salts and esters thereof are provided. The cyclic peptides and pharmaceutically acceptable salts and esters thereof mimic surface features of the C-terminus of endothelin and thereby can be used modulate or alter the activity of the endothelin family of peptides. More particularly, cyclic pentapeptides, cyclic hexapeptides, cyclic heptapeptides and pharmaceutically acceptable derivatives of the peptides that specifically inhibit the activity of endothelin are provided. Among the cyclic peptides are those that have the formula: cyclo(X.sup.1 -X.sup.2 -X.sup.3 -X.sup.4 -D-Trp): X.sup.1 is D-Tyr or D-Asp; X.sup.2 is Phe, Ala, Ac.sub.3 c or Pro; X.sup.3 is D-His, D-Ala, D-Val, Gly or .beta.-Ala; and X.sup.4 is His, Ala, .beta.-Ala, Aib, Gly, D-His-gly or Leu; cyclo(X.sup.1 -L-Phe-X.sup.3 -X.sup.4 -X.sup.5) in which X.sup.1 is D-Tyr, D-Asp or D-Glu, X.sup.3 is selected from among D-His, .beta.-Ala-D-His or gly-D-His; X.sup.4 is Ser, Gly or .beta.-Ala, and X.sup.
    Type: Grant
    Filed: November 10, 1994
    Date of Patent: April 7, 1998
    Assignee: Texas Biotechnology Corporation
    Inventors: Vitukudi Narayanaiyengar Balaji, Ming Fai Chan
  • Patent number: 5731408
    Abstract: Cyclic lactam peptides, seven amino acids in length, having D-2'-naphthylalanine (D-2'-Nal) or D-para-iodo-phenylalanine D-(p-I)Phe at position 4 of the peptide provided potent and specific antagonists of the two neural melanocortin receptors and of the peripheral receptor. In particular, the peptide ##STR1## was found to be a potent antagonist of the MC3 and MC4 receptors with partial agonist activity, and a full agonist of the MC1 and MC5 receptors; the peptide ##STR2## was found to be a potent antagonist of the MC3 and MC4 receptors with partial agonist activity. Both peptides have antagonist activities in the classical frog skin bioassay for pigmentation at the MC1 receptor.
    Type: Grant
    Filed: April 10, 1995
    Date of Patent: March 24, 1998
    Assignee: Arizona Board of Regents on behalf of the University of Arizona
    Inventors: Mac E. Hadley, Victor J. Hruby, Shubh D. Sharma
  • Patent number: 5696083
    Abstract: This invention relates to personal care compositions, and, more specifically, to a composition comprising a pyrithione salt or acid, polymyxin antibiotic, and a suitable carrier. The pyrithione plus the polymyxin provide antimicrobial efficacy to the personal care composition. The personal care composition is useful in a variety of dermatological items, such as soaps, shampoos, and skin care medicaments.
    Type: Grant
    Filed: August 11, 1994
    Date of Patent: December 9, 1997
    Assignee: Olin Corporation
    Inventor: John D. Nelson, Jr.
  • Patent number: 5693612
    Abstract: 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: Grant
    Filed: April 28, 1995
    Date of Patent: December 2, 1997
    Assignee: Merck Patent Gesellschaft mit Beschrankter Haftung
    Inventors: Alfred Jonczyk, Gunter Holzemann, Simon Goodman, Horst Kessler, Roland Haubner, Jochen Wermuth
  • Patent number: 5684128
    Abstract: An improved process for the preparation of side chain derivatives of cyclohexapeptidyl lipopeptides represented by the formula ##STR1## wherein R.sup.1 is fully defined, is disclosed.
    Type: Grant
    Filed: February 20, 1996
    Date of Patent: November 4, 1997
    Assignee: Merck & Co., Inc.
    Inventors: James M. Balkovec, Frances A. Bouffard, James F. Dropinski, Akinlolu A. Adefarati, Jan S. Tkacz
  • Patent number: 5677419
    Abstract: Analogs of porcine Vasoactive Intestinal Peptide are disclosed. The analogs have been cyclized by the covalent attachment, via an amide bond, of the side-chain carboxy terminus of one amino acid in the peptide chain to the side-chain amino terminus of another amino acid in the peptide chain. The claimed compounds are useful for the treatment of asthma.
    Type: Grant
    Filed: September 19, 1994
    Date of Patent: October 14, 1997
    Assignee: Hoffmann-La Roche Inc.
    Inventors: David Robert Bolin, Margaret O'Donnell
  • Patent number: 5668105
    Abstract: Compounds represented by the formula (Seq ID Nos. 1-6) ##STR1## wherein all substituents are fully defined, are disclosed. These compounds exhibit utilities as antibiotic and antifungal agents and for the treatment and prevention of Pneumocystis infections.
    Type: Grant
    Filed: March 12, 1996
    Date of Patent: September 16, 1997
    Assignee: Merck & Co., Inc.
    Inventors: James M. Balkovec, Frances A. Bouffard, Milton L. Hammond
  • Patent number: 5646245
    Abstract: An improved process for the preparation of side chain derivatives of cyclohexapeptidyl lipopeptides represented by the formula ##STR1## wherein R.sup.1 is fully defined, is disclosed.
    Type: Grant
    Filed: May 16, 1996
    Date of Patent: July 8, 1997
    Inventors: James M. Balkovec, Frances A. Bouffard, James F. Dropinski, Akinlolu A. Adefarati, Jan S. Tkacz
  • Patent number: 5552521
    Abstract: There is disclosed a novel process for preparing aza cyclohexapeptides of the formula ##STR1## where all variables are defined herein.
    Type: Grant
    Filed: February 10, 1995
    Date of Patent: September 3, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Kevin M. Belyk, Dean R. Bender, Regina M. Black, David L. Hughes, William Leonard
  • Patent number: 5543496
    Abstract: Cyclic compounds based on a modified bradykinin sequence are potent bradykinin receptor antagonists. Amino acid substitutions are made at postions 2 and 5 or 6 to facilitate the cyclization of the peptide through covalent bonding of the amino acid side chains.The analogs produced are useful in treating conditions and diseases of a mammal and human in which an excess of bradykinin or related kinins are produced or injected such as by insect bites.
    Type: Grant
    Filed: July 25, 1994
    Date of Patent: August 6, 1996
    Assignee: Scios Nova Inc.
    Inventors: Donald J. Kyle, Sarvajit Chakravarty
  • Patent number: 5521156
    Abstract: Antagonists of neurokinin A which are novel cyclic hexapeptide and octapeptide compounds are described. The antagonism is confirmed using conventional competitive binding and biochemical assays as well as conventional physiological tests and the use of these derivatives in a variety of conditions in which neurokinin A is implicated is also described.
    Type: Grant
    Filed: February 3, 1994
    Date of Patent: May 28, 1996
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Thomas J. Owen, Elizabeth M. Kudlacz, Scott L. Harbeson, Stephen H. Buck
  • Patent number: 5516757
    Abstract: There are disclosed novel semi-synthetic lipopeptides of the formula (Seq. ID Nos. 1-6) ##STR1## wherein the substituents are defined herein, which show utility as antifungal and anti-Pneumocystis agents. Pharmaceutical compositions containing said compounds are also disclosed.
    Type: Grant
    Filed: September 16, 1994
    Date of Patent: May 14, 1996
    Assignee: Merck & Co., Inc.
    Inventor: James M. Balkovec
  • Patent number: 5516756
    Abstract: The present invention is directed to novel aza cyclohexapeptide compounds of the formula ##STR1## where all substituents are defined herein, which are useful as antifungal agents and for the treatment of Pneumocystis carinii infections. Compositions containing the compounds of the invention are also disclosed.
    Type: Grant
    Filed: October 31, 1994
    Date of Patent: May 14, 1996
    Assignee: Merck & Co., Inc.
    Inventors: James M. Balkovec, Frances A. Bouffard, James F. Dropinski
  • Patent number: 5514651
    Abstract: The present invention relates to aza cyclohexapeptide compounds of the formula (Seq ID Nos. 1-10) ##STR1## which may be useful as antibiotics, antifungal agents and for the treatment of Pneumocystis carinii infections.
    Type: Grant
    Filed: September 16, 1994
    Date of Patent: May 7, 1996
    Assignee: Merck & Co., Inc.
    Inventors: James M. Balkovec, Frances A. Bouffard, James F. Dropinski
  • Patent number: 5514650
    Abstract: Ceretain aza cyclohexapeptide compounds have been found to have superior antibiotic properties. Novel processes for their preparation are also described.
    Type: Grant
    Filed: August 29, 1994
    Date of Patent: May 7, 1996
    Assignee: Merck & Co., Inc.
    Inventors: James M. Balkovec, Regina M. Black, Frances A. Bouffard
  • Patent number: 5493007
    Abstract: A peptide containing the tripeptide recognition sequences RGD or KGD in a cycle and an exocyclic group bearing a positive charge is provided. The compound is provided in therapeutic form for administration to a mammal and exhibits high specificity and potency as a platelet aggregation inhibitor without undesireable side effects.
    Type: Grant
    Filed: September 23, 1994
    Date of Patent: February 20, 1996
    Assignee: Genentech, Inc.
    Inventors: John P. Burnier, Thomas Gadek, Robert S. McDowell
  • Patent number: 5430018
    Abstract: Certain aminoalkyl substituted amides which have a cyclohexapeptidyl group and which are found to have antibiotic activity with physical properties suitable for use in therapeutic compositions are described.
    Type: Grant
    Filed: October 17, 1991
    Date of Patent: July 4, 1995
    Assignee: Merck & Co., Inc.
    Inventor: Robert A. Zambias
  • Patent number: 5378804
    Abstract: Aza cyclohexapeptide compounds are disclosed with a nitrogen attached to the cyclohexapeptide ring at the 5-carbon of the 4-hydroxyornithine component. Such compounds are represented by the formula: ##STR1## The compounds are disclosed as having antifungal, antiprotozoal and anti-Pneumocystis carinii activity.
    Type: Grant
    Filed: March 16, 1993
    Date of Patent: January 3, 1995
    Assignee: Merck & Co., Inc.
    Inventors: James M. Balkovec, Regina M. Black, Frances A. Bouffard
  • Patent number: 5360788
    Abstract: This invention relates to personal care compositions, and, more specifically, to a composition comprising a pyrithione salt or acid, a basic lipopeptide, and a suitable carrier. The pyrithione plus the lipopeptide provide antimicrobial efficacy to the personal care composition. The personal care composition is useful in a variety of dermatological items, such as soaps, shampoos, and skin care medicaments.
    Type: Grant
    Filed: November 10, 1992
    Date of Patent: November 1, 1994
    Assignee: Olin Corporation
    Inventor: John D. Nelson
  • Patent number: 5350574
    Abstract: This invention provides a molecule comprising cyclosporine A or a congener of cyclosporine A which is photochemically attached to a ligand containing a reactive group. This invention also provides a composition of matter which comprises a conjugate of a compound and the aforementioned molecule wherein the compound is bound to the molecule through the reactive group. This invention further provides an antibody directed to the aforementioned composition of matter specific for cyclosporine A or congener of cyclosporine A. This invention also provides methods for detecting the presence of cyclosporine A or congener thereof, methods for detecting the concentration of cyclosporine A or congener thereof, as well as a method of monitoring levels of cyclosporine A or congener of cyclosporine A in a subject.
    Type: Grant
    Filed: May 13, 1991
    Date of Patent: September 27, 1994
    Assignee: The Trustees of Columbia University in the City of New York
    Inventors: Bernard F. Erlanger, William L. Cleveland, Nicholas A. Cacalano
  • Patent number: 5348940
    Abstract: Certain propionitrile compounds which have a cyclohexapeptidyl nucleus and which are found to have antibiotic activity with physical properties suitable for use in therapeutic compositions are described. A novel process for their preparation is also described.
    Type: Grant
    Filed: September 3, 1992
    Date of Patent: September 20, 1994
    Assignee: Merck & Co., Inc.
    Inventors: James M. Balkovec, Robert A. Zambias
  • Patent number: 5258493
    Abstract: Disclosed herein are cyclic peptide derivatives of the formula ##STR1## wherein A is absent or the tripeptide radical Thr.rarw.Gly.rarw.Ala, R.sup.1 is benzyl or benzyl monosubstituted at position 4 of the aromatic ring with halo, hydroxy, lower alkyl or lower alkoxy, R.sup.2 and R.sup.4 each independently is hydrogen or lower alkyl, R.sup.3 is lower alkyl or lower alkyl monosubstituted with a hydroxy, R.sup.5 is lower alkyl, Y is oxo or thioxo and Z is hydroxy or NR.sup.6 R.sup.7 wherein R.sup.6 and R.sup.7 each independently is hydrogen or lower alkyl. The derivatives are useful for treating herpes infections.
    Type: Grant
    Filed: March 16, 1992
    Date of Patent: November 2, 1993
    Assignee: Bio-Mega/Boehringer Ingelheim Research Inc.
    Inventors: Julian Adams, John DiMaio, Raymond Plante
  • Patent number: 5198421
    Abstract: There is disclosed a monophosphorylated cyclic lipopeptide compound obtained by biophosphorylating a cyclic lipopeptide related to echinocandins and having a peptide skeleton bearing several hydroxy groups wherein in the phosphorylated cyclic lipopeptide, the phosphate group is attached to the hydroxy group of the 4-hydroxyproline component of the lipopeptide. The compounds are useful for the control of fungi and parasites.
    Type: Grant
    Filed: April 26, 1991
    Date of Patent: March 30, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Shieh-Shung T. Chen, David J. Mathre, Brian R. Petuch, Robert A. Reamer
  • Patent number: 5192742
    Abstract: New glycopeptide antibiotics MM 49728, MM 55266, MM 55267/1, MM 55267/2 and MM 55268 are produced by fermentation of Amycolatopsis sp. NCIB 40089.
    Type: Grant
    Filed: December 18, 1991
    Date of Patent: March 9, 1993
    Assignee: Beecham Group PLC
    Inventors: Nigel J. Coates, Rachel Sykes, Christopher J. Davis, Lawrence M. Curtis
  • Patent number: RE39887
    Abstract: Dehydrodidemnin B with useful biological activity has formula (1). It can be isolated from natural sources or synthesized, and it forms active derivatives.
    Type: Grant
    Filed: June 2, 2005
    Date of Patent: October 16, 2007
    Assignee: Pharma Mar, S.A.
    Inventors: Kenneth L. Rinehart, Anna M. Lithgow-Bertelloni