Patents Assigned to Praecis Pharmaceuticals, Inc.
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Patent number: 6699833Abstract: Sustained delivery formulations comprising a water-insoluble complex of a peptide and a carrier macromolecule are disclosed. The formulations of the invention allow for loading of high concentrations of peptide in a small volume and for delivery of a pharmaceutically active peptide for prolonged periods, e.g., one month, after administration of the complex. The complexes of the invention can be milled or crushed to a fine powder. In powdered form, the complexes form stable aqueous suspensions and dispersions, suitable for injection. In a preferred embodiment, the peptide of the complex is an LHRH analogue, preferably an LHRH antagonist, and the carrier macromolecule is an anionic polymer, preferably carboxymethylcellulose. Methods of making the complexes of the invention, and methods of using LHRH-analogue-containing complexes to treat conditions treatable with an LHRH analogue, are also disclosed.Type: GrantFiled: July 8, 1999Date of Patent: March 2, 2004Assignee: Praecis Pharmaceuticals, Inc.Inventors: Malcolm L. Gefter, Nicholas Barker, Gary Musso, Christopher J. Molineaux
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Publication number: 20040005307Abstract: Compounds that modulate the aggregation of amyloidogenic proteins or peptides are disclosed. The modulators of the invention can promote amyloid aggregation or, more preferably, can inhibit natural amyloid aggregation. In a preferred embodiment, the compounds modulate the aggregation of natural &bgr; amyloid peptides (&bgr;-AP). In a preferred embodiment, the &bgr; amyloid modulator compounds of the invention are comprised of an A&bgr; aggregation core domain and a modifying group coupled thereto such that the compound alters the aggregation or inhibits the neurotoxicity of natural &bgr; amyloid peptides when contacted with the peptides. Furthermore, the modulators are capable of altering natural &bgr;-AP aggregation when the natural &bgr;-APs are in a molar excess amount relative to the modulators. Pharmaceutical compositions comprising the compounds of the invention, and diagnostic and treatment methods for amyloidogenic diseases using the compounds of the invention, are also disclosed.Type: ApplicationFiled: June 17, 2003Publication date: January 8, 2004Applicant: Praecis Pharmaceuticals, Inc.Inventors: Mark A. Findeis, Howard Benjamin, Marc B. Garnick, Malcolm L. Gefter, Arvind Hundal, Laura Kasman, Gary Musso, Ethan R. Signer, James Wakefield, Michael J. Reed
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Publication number: 20030236197Abstract: Compounds that modulate natural &bgr; amyloid peptide aggregation are provided. The modulators of the invention comprise a peptide, preferably based on a &bgr; amyloid peptide, that is comprised entirely of D-amino acids. Preferably, the peptide comprises 3-5 D-amino acid residues and includes at least two D-amino acid residues independently selected from the group consisting of D-leucine, D-phenylalanine and D-valine. In a particularly preferred embodiment, the peptide is a retro-inverso isomer of a &bgr; amyloid peptide, preferably a retro-inverso isomer of A&bgr;17-21. In certain embodiments, the peptide is modified at the amino-terminus, the carboxy-terminus, or both. Preferred amino-terminal modifying groups alkyl groups. Preferred carboxy-terminal modifying groups include an amide group, an acetate group, an alkyl amide group, an aryl amide group or a hydroxy group.Type: ApplicationFiled: March 24, 2003Publication date: December 25, 2003Applicant: Praecis Pharmaceuticals Inc.Inventors: Mark A. Findeis, Kathryn Phillips, Gary L. Olson, Christopher Self
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Publication number: 20030224992Abstract: The present invention provides transcription factor modulators useful for modulating gene expression in a cell, as well as pharmaceutical compositions containing these transcription factor modulators. The present invention also provides methods for modulating gene transcription in a cell and methods of treating a subject suffering from a transcription factor-associated disorder, such as cancer, inflammatory disorders or autoimmune disorders.Type: ApplicationFiled: March 14, 2003Publication date: December 4, 2003Applicant: Praecis Pharmaceuticals Inc.Inventors: John L. Joyal, Mark A. Findeis, Malcolm J. Kavarana, Barry Morgan, Malcolm L. Gefter
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Publication number: 20030175685Abstract: The invention provides methods and compositions for screening and identifying peptides which modulate a biological process in an organism, cell or tissue. The present invention further provides methods of using the identified peptides or analogues thereof to treat a disease or condition associated with an aberrant biological process in a subject.Type: ApplicationFiled: February 22, 2002Publication date: September 18, 2003Applicant: Praecis Pharmaceuticals Inc.Inventor: Malcolm L. Gefter
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Publication number: 20030171296Abstract: Sustained delivery formulations comprising a water-insoluble complex of a peptidic compound (e.g., a peptide, polypeptide, protein, peptidomimetic or the like) and a carrier macromolecule are disclosed. The formulations of the invention allow for loading of high concentrations of peptidic compound in a small volume and for delivery of a pharmaceutically active peptidic compound for prolonged periods, e.g., one month, after administration of the complex. The complexes of the invention can be milled or crushed to a fine powder. In powdered form, the complexes form stable aqueous suspensions and dispersions, suitable for injection. In a preferred embodiment, the peptidic compound of the complex is an LHRH analogue, preferably an LHRH antagonist, and the carrier macromolecule is an anionic polymer, preferably carboxymethylcellulose. Methods of making the complexes of the invention, and methods of using LHRH-analogue-containing complexes to treat conditions treatable with an LHRH analogue, are also disclosed.Type: ApplicationFiled: December 27, 2000Publication date: September 11, 2003Applicant: Praecis Pharmaceuticals, Inc.Inventors: Malcolm L. Gefter, Nicholas Barker, Gary Musso, Christopher J. Molineaux
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Patent number: 6610658Abstract: Compounds that modulate natural &bgr; amyloid peptide aggregation are provided. The modulators of the invention comprise a peptide, preferably based on a &bgr; amyloid peptide, that is comprised entirely of D-amino acids. Preferably, the peptide comprises 3-5 D-amino acid residues and includes at least two D-amino acid residues independently selected from the group consisting of D-leucine, D-phenylalanine and D-valine. In a particularly preferred embodiment, the peptide is a retro-inverso isomer of a &bgr; amyloid peptide, preferably a retro-inverso isomer of A&bgr;17-21. In certain embodiments, the peptide is modified at the: amino-terminus, carboxy-terminus, or both. Preferred amino-terminal modifying groups alkyl groups. Preferred carboxy-terminal modifying groups include an amide group, an acetate group, an alkyl amide group, an aryl amide group or a hydroxy group.Type: GrantFiled: March 3, 2000Date of Patent: August 26, 2003Assignee: Praecis Pharmaceuticals Inc.Inventors: Mark A. Findeis, Kathryn Phillips, Gary L. Olson, Christopher Self
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Publication number: 20030109671Abstract: The present invention provides angiogenesis inhibitor compounds comprising a MetAP-2 inhibitory core coupled to a peptide, as well as pharmaceutical compositions comprising the angiogenesis inhibitor compounds and a pharmaceutically acceptable carrier. The present invention also provides methods of treating an angiogenic disease, e.g., cancer, in a subject by administering to the subject a therapeutically effective amount of one or more of the angiogenesis inhibitor compounds of the invention.Type: ApplicationFiled: May 2, 2002Publication date: June 12, 2003Applicant: Praecis Pharmaceuticals Inc.Inventors: Gary L. Olson, Christopher Self, Lily Lee, Charles Michael Cook, Jens Birktoft, Barry Morgan, Christopher C. Arico-Muendel
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Publication number: 20030086870Abstract: Improved methods for detecting lesions in dense breast tissue are disclosed. The methods of the invention generally feature administration to a subject of an LHRH antagonist in an amount and for a period of time sufficient to reduce the density of breast tissue prior to generating an image of the breast tissue, for example by mammography, to detect a lesion in the breast tissue. Packaged formulations for reducing breast density in a subject prior to generating an image of the subject's breast tissue, comprising an LHRH antagonist packaged with instructions for using the LHRH antagonist to reduce breast density in a subject prior to imaging the breast tissue, are also disclosed.Type: ApplicationFiled: December 12, 2002Publication date: May 8, 2003Applicant: Praecis Pharmaceuticals Inc.Inventor: Marc B. Garnick
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Publication number: 20030083262Abstract: The present invention provides methods and compositions for treating inflammatory disorders, e.g., asthma, lung inflammation or cancer.Type: ApplicationFiled: August 27, 2002Publication date: May 1, 2003Applicant: Praecis Pharmaceuticals Inc.Inventors: Gerhard Hannig, Douglas Lazarus
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Patent number: 6548477Abstract: The present invention provides angiogenesis inhibitor compounds comprising a MetAP-2 inhibitory core coupled to a peptide, as well as pharmaceutical compositions comprising the angiogenesis inhibitor compounds and a pharmaceutically acceptable carrier. The present invention also provides methods of treating an angiogenic disease, e.g., cancer, in a subject by administering to the subject a therapeutically effective amount of one or more of the angiogenesis inhibitor compounds of the invention.Type: GrantFiled: November 1, 2000Date of Patent: April 15, 2003Assignee: Praecis Pharmaceuticals Inc.Inventors: Gary L. Olson, Christopher Self, Lily Lee, Charles Michael Cook, Jens J. Birktoft
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Patent number: 6540979Abstract: Improved methods for detecting lesions in dense breast tissue are disclosed. The methods of the invention generally feature administration to a subject of an LHRH antagonist in an amount and for a period of time sufficient to reduce the density of breast tissue prior to generating an image of the breast tissue, for example by mammography, to detect a lesion in the breast tissue. Packaged formulations for reducing breast density in a subject prior to generating an image of the subject's breast tissue, comprising an LHRH antagonist packaged with instructions for using the LHRH antagonist to reduce breast density in a subject prior to imaging the breast tissue, are also disclosed.Type: GrantFiled: January 18, 2001Date of Patent: April 1, 2003Assignee: Praecis Pharmaceuticals, Inc.Inventor: Marc B. Garnick
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Publication number: 20030045680Abstract: The present invention provides peptide compounds which bind to the androgen receptor. In preferred embodiments, the peptide compounds of the invention inhibit binding of the androgen receptor DNA binding domain to DNA, in particular, the androgen responsive elements. These compounds are useful for the treatment of androgen-associated disorders including, for example, prostate cancer.Type: ApplicationFiled: March 12, 2002Publication date: March 6, 2003Applicant: Praecis Pharmaceuticals Inc.Inventors: John L. Joyal, John Mueller, Vibha B. Oza, Mark A. Findeis
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Publication number: 20020193298Abstract: The present invention provides angiogenesis inhibitor compounds comprising a MetAP-2 inhibitory core coupled to a peptide, as well as pharmaceutical compositions comprising the angiogenesis inhibitor compounds and a pharmaceutically acceptable carrier. The present invention also provides methods of treating an angiogenic disease, e.g., cancer, in a subject by administering to the subject a therapeutically effective amount of one or more of the angiogenesis inhibitor compounds of the invention.Type: ApplicationFiled: October 5, 2001Publication date: December 19, 2002Applicant: Praecis Pharmaceuticals Inc.Inventors: Gary L. Olson, Christopher Self, Lily Lee, Charles Michael Cook, Jens Birktoft
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Publication number: 20020176841Abstract: Sustained delivery pharmaceutical compositions comprising a solid ionic complex of a pharmaceutically active compound and an ionic macromolecule are provided by the present invention. The pharmaceutical compositions of the invention allow for loading of high concentrations of pharmaceutically active compounds and for delivery of a pharmaceutically active compound for prolonged periods of time, e.g., one month, after administration. Methods for preparing these pharmaceutical compositions, as well as methods of using them to treat a subject are also provided.Type: ApplicationFiled: March 19, 2002Publication date: November 28, 2002Applicant: Praecis Pharmaceuticals Inc.Inventors: Nicholas Barker, Janet L. Wolfe
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Patent number: 6475806Abstract: An anchor library is described. A collection of recombinant vectors having a nucleic acid encoding a displayed peptide sequence is provided. The displayed peptide sequence of each of the vectors comprises X1(Y1)c1X2(Y2)c2X3(Y3)c3X4, wherein each X1, X2, X3 and X4 is an amino acid residue and any of X1, X2, X3 and X4 can be the same or different from any one other, wherein each Y1, Y2 and Y3 is alanine or glycine or a combination of alanine and glycine that is respectively c1, c2 and c3 amino acid residues long and any of Y1, Y2 and Y3 if present can be the same or different from any one other, wherein each of c1, c2 and c3 is 0 to about 20, wherein X1 and X4 are each attached to an amino acid residue that flanks the displayed peptide sequence. Preferably, at least about 105 to about 108 permutations of all possible permutations of the displayed peptide sequence are present in the anchor library.Type: GrantFiled: June 7, 1995Date of Patent: November 5, 2002Assignee: Praecis Pharmaceuticals, Inc.Inventors: Howard Benjamin, Ethan Signer, Malcolm Gefter
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Publication number: 20020151493Abstract: The present invention provides angiogenesis inhibitor compounds comprising a MetAP-2 inhibitory core coupled to a peptide, as well as pharmaceutical compositions comprising the angiogenesis inhibitor compounds and a pharmaceutically acceptable carrier. The present invention also provides methods of treating an angiogenic disease, e.g., cancer, in a subject by administering to the subject a therapeutically effective amount of one or more of the angiogenesis inhibitor compounds of the invention.Type: ApplicationFiled: November 1, 2001Publication date: October 17, 2002Applicant: Praecis Pharmaceuticals Inc.Inventors: Gary L. Olson, Christopher Self, Lily Lee, Charles Michael Cook, Jens Birktoft, Barry Morgan, Christopher C. Arico-Muendel
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Publication number: 20020133001Abstract: The present invention provides therapeutic agents suitable for treating an amyloidogenic disorder, as well as pharmaceutical compositions comprising the therapeutic agents and a pharmaceutically acceptable carrier. The present invention also provides methods of treating an amyloidogenic disorder, e.g., Alzheimer's disease, in a subject by administering to the subject a therapeutically effective amount of one or more of the compounds of the invention.Type: ApplicationFiled: November 27, 2001Publication date: September 19, 2002Applicant: Praecis Pharmaceuticals Inc.Inventors: Malcolm L. Gefter, David I. Israel, John L. Joyal, Michael Gosselin
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Publication number: 20020103134Abstract: Compounds that modulate natural &bgr; amyloid peptide aggregation are provided. The modulators of the invention comprise a peptide, preferably based on a &bgr; amyloid peptide, that is comprised entirely of D-amino acids. Preferably, the peptide comprises 3-5 D-amino acid residues and includes at least two D-amino acid residues independently selected from the group consisting of D-leucine, D-phenylalanine and D-valine. In a particularly preferred embodiment, the peptide is a retro-inverso isomer of a &bgr; amyloid peptide, preferably a retro-inverso isomer of A&bgr;17-21. In certain embodiments, the peptide is modified at the amino-terminus, the carboxy-terminus, or both. Preferred amino-terminal modifying groups include cyclic, heterocyclic, polycyclic and branched alkyl groups. Preferred carboxy-terminal modifying groups include an amide group, an alkyl amide group, an aryl amide group or a hydroxy group.Type: ApplicationFiled: June 29, 2001Publication date: August 1, 2002Applicant: Praecis Pharmaceuticals Inc.Inventors: Mark A. Findeis, Malcolm L. Gefter, Gary Musso, Ethan R. Signer, James Wakefield, Susan Molineaux, Joseph Chin, Jung-Ja Lee, Michael Kelley, Sonja Komar-Panicucci, Christopher C. Arico-Muendel, Kathryn Phillips, Neil J. Hayward
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Publication number: 20020098173Abstract: Compounds that modulate the aggregation of amyloidogenic proteins or peptides are disclosed. The modulators of the invention can promote amyloid aggregation or, more preferably, can inhibit natural amyloid aggregation. In a preferred embodiment, the compounds modulate the aggregation of natural &bgr; amyloid peptides (&bgr;-AP). In a preferred embodiment, the &bgr; amyloid modulator compounds of the invention are comprised of an A&bgr; aggregation core domain and a modifying group coupled thereto such that the compound alters the aggregation or inhibits the neurotoxicity of natural &bgr; amyloid peptides when contacted with the peptides. Furthermore, the modulators are capable of altering natural &bgr;-AP aggregation when the natural &bgr;-APs are in a molar excess amount relative to the modulators. Pharmaceutical compositions comprising the compounds of the invention, and diagnostic and treatment methods for amyloidogenic diseases using the compounds of the invention, are also disclosed.Type: ApplicationFiled: October 4, 2001Publication date: July 25, 2002Applicant: Praecis Pharmaceuticals, Inc.Inventors: Mark A. Findeis, Howard Benjamin, Marc B. Garnick, Malcolm L. Gefter, Arvind Hundal, Laura Kasman, Gary Musso, Ethan R. Signer, James Wakefield, Michael J. Reed