Patents Represented by Attorney, Agent or Law Firm Alex Andrus
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Patent number: 8343955Abstract: Benzoxazepin compounds of Formula I, including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z1 is CR1 or N; Z2 is CR2 or N; Z3 is CR3 or N; Z4 is CR4 or N; and B is a pyrazolyl, imidazolyl, or triazolyl ring fused to the benzoxepin ring, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: GrantFiled: May 22, 2012Date of Patent: January 1, 2013Assignee: Genentech, Inc.Inventors: Nicole Blaquiere, Steven Do, Danette Dudley, Adrian Folkes, Robert Heald, Timothy Heffron, Mark Jones, Aleksandr Kolesnikov, Chudi Ndubaku, Alan G. Olivero, Stephen Price, Steven Staben, Lan Wang
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Patent number: 8242104Abstract: Benzoxazepin compounds of Formula I, including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z1 is CR1 or N; Z2 is CR2 or N; Z3 is CR3 or N; Z4 is CR4 or N; and B is a pyrazolyl, imidazolyl, or triazolyl ring fused to the benzoxepin ring, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: GrantFiled: September 27, 2010Date of Patent: August 14, 2012Assignee: F. Hoffman-La Roche AGInventors: Nicole Blaquiere, Steven Do, Danette Dudley, Adrian Folkes, Robert Heald, Timothy Heffron, Mark Jones, Aleksandr Kolesnikov, Chudi Ndubaku, Alan G. Olivero, Stephen Price, Steven Staben, Lan Wang
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Patent number: 8173650Abstract: Formula I (Ia and Ib) compounds wherein (i) X1 is N and X2 is S, (ii) X1 is CR7 and X2 is S, (iii) X1 is N and X2 is NR2, or (iv) X1 is CR7 and X2 is O, including stereoisomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological, and cancer. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: GrantFiled: May 26, 2010Date of Patent: May 8, 2012Assignee: Genentech, Inc.Inventors: Georgette Castanedo, Bryan Chan, David Goldstein, Rama Kondru, Matthew Lucas, Wylie Palmer, Stephen Price, Brian Safina, Pascal Pierre Alexandre Savy, Eileen Mary Seward, Daniel P. Sutherlin, Zachary K. Sweeney
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Patent number: 8168633Abstract: Thiazolopyrimidine compounds of formula I, where W represents a thiazole ring, selectively inhibit the p110 delta subtype of PI3 Kinase (PI3K), and are useful for treating diseases and disorders arising from abnormal cell growth, function or behavior associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.Type: GrantFiled: January 7, 2011Date of Patent: May 1, 2012Assignee: Genentech, Inc.Inventors: Timothy Colin Hancox, Neil Anthony Pegg, Mandy Christine Beswick, Toby Jonathan Blench, Elsa Amandine Dechaux, Jahusz Jozef Kulagowski, Alan John Nadin, Stephen Price
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Patent number: 8158624Abstract: Purine compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: GrantFiled: May 29, 2009Date of Patent: April 17, 2012Assignee: Genetech, Inc.Inventors: Georgette Castanedo, Irina Chuckowree, Adrian Folkes, Daniel P. Sutherlin, Nan Chi Wan
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Patent number: 8158625Abstract: Formula I (Ia and Ib) compounds wherein (i) X1 is N and X2 is S, (ii) X1 is CR7 and X2 is S, (iii) X1 is N and X2 is NR2, (iv) X1 is CR7 and X2 is O, or (v) X1 is CR7 and X2 is NR2, including stereoisomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological, and cancer. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: GrantFiled: May 26, 2010Date of Patent: April 17, 2012Assignee: Genentech, Inc.Inventors: Georgette Castanedo, David Goldstein, Rama Kondru, Matthew Lucas, Wylie Palmer, Stephen Price, Brian Safina, Pascal Pierre Alexandre Savy, Eileen Mary Seward, Daniel P. Sutherlin, Zachary K. Sweeney
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Patent number: 8142784Abstract: The present invention relates to antibody-drug conjugate compounds of Formula I: Ab-(L-D)p??I where one or more maytansinoid drug moieties (D) are covalently linked by L to an antibody (Ab) which binds to an ErbB receptor, or which binds to one or more tumor-associated antigens or cell-surface receptors. These compounds may be used in methods of diagnosis or treatment of cancer, and other diseases and disorders.Type: GrantFiled: December 2, 2008Date of Patent: March 27, 2012Assignee: Genentech, Inc.Inventors: Allen J. Ebens, Jr., Frederic S. Jacobson, Paul Polakis, Ralph H. Schwall, Mark X. Sliwkowski, Susan D. Spencer
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Patent number: 7947839Abstract: Bis 1,8 naphthalimide compounds including antibody drug conjugate (ADC) are described. Pharmaceutical compositions comprising an effective amount of a 1,8 bis-naphthalimide compound for treatment of hyperproliferative disorders and other disorders are described. Methods are described for killing or inhibiting the proliferation of tumor cells or cancer cells including administering to a patient an effective amount of a 1,8 bis-naphthalimide compound.Type: GrantFiled: January 30, 2006Date of Patent: May 24, 2011Assignee: Genentech, Inc.Inventors: Lewis J. Gazzard, Edward HyungSuk Ha, David Y. Jackson, Joann M. Um
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Patent number: 7893060Abstract: Thiazolopyrimidines of formula (I): wherein W represents a thiazole ring; R1 and R2 form, together with the N atom to which they are attached, a group of the following formula (IIa): in which A is a ring system; m is 0, 1 or 2; R3 is H or C1-C6 alkyl; and R4 is an indole group which is unsubstituted or substituted; and the pharmaceutically acceptable salts thereof are inhibitors of PI3K and are selective for the p110? isoform, which is a class Ia PD kinase, over both other class Ia and class Ib kinases. The compounds may be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.Type: GrantFiled: June 12, 2008Date of Patent: February 22, 2011Assignee: F. Hoffmann-La Roche AGInventors: Timothy Colin Hancox, Neil Anthony Pegg, Mandy Christine Beswick, Toby Jonathan Blench, Elsa Amandine Dechaux, Janusz Jozef Kulagowski, Alan John Nadin, Stephen Price
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Patent number: 7723485Abstract: Cysteine engineered anti-MUC16 antibodies are engineered by replacing one or more amino acids of a parent anti-MUC16 antibody with non cross-linked, reactive cysteine amino acids. Methods of design, preparation, screening, and selection of the cysteine engineered anti-MUC16 antibodies are provided. Cysteine engineered anti-MUC16 antibodies (Ab) are conjugated with one or more drug moieties (D) through a linker (L) to form cysteine engineered anti-MUC16 antibody-drug conjugates having Formula I: Ab-(L-D)p??I where p is 1 to 4. Diagnostic and therapeutic uses for cysteine engineered antibody drug compounds and compositions are disclosed.Type: GrantFiled: May 7, 2008Date of Patent: May 25, 2010Assignee: Genentech, Inc.Inventors: Jagath R. Junutula, William Mallet
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Patent number: 7662936Abstract: Methods to detect, screen, and quantitate biological samples after administration of antibody conjugates, antibody-drug conjugates of Formula I, antibodies, and fragments and metabolites thereof, by affinity separation, chromatography, and mass spectrometry are disclosed. Ab-(L-D)p??I wherein Ab is an antibody; D is a drug moiety; L is a linker covalently attached to Ab, and covalently attached to D; and p is 1, 2, 3, 4, 5, 6, 7, or 8.Type: GrantFiled: April 6, 2005Date of Patent: February 16, 2010Assignee: Genentech, Inc.Inventors: Miryam Kadkhodayan, Emily Mann
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Patent number: 7575748Abstract: The application concerns methods of treatment using anti-ErbB receptor antibody-maytansinoid conjugates, and articles of manufacture suitable for use in such methods. In particular, the invention concerns ErbB receptor-directed cancer therapies, using anti-ErbB receptor antibody-maytansinoid conjugates.Type: GrantFiled: July 17, 2006Date of Patent: August 18, 2009Assignee: Genentech, Inc.Inventors: Sharon Erickson, Ralph Schwall, Mark Sliwkowski, Walter Blattler
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Patent number: 7521541Abstract: Antibodies are engineered by replacing one or more amino acids of a parent antibody with non cross-linked, highly reactive cysteine amino acids. Antibody fragments may also be engineered with one or more cysteine amino acids to form cysteine engineered antibody fragments (ThioFab). Methods of design, preparation, screening, and selection of the cysteine engineered antibodies are provided. Cysteine engineered antibodies (Ab), optionally with an albumin-binding peptide (ABP) sequence, are conjugated with one or more drug moieties (D) through a linker (L) to form cysteine engineered antibody-drug conjugates having Formula I: Ab-(L-D)p??I where p is 1 to 4. Diagnostic and therapeutic uses for cysteine engineered antibody drug compounds and compositions are disclosed.Type: GrantFiled: September 22, 2005Date of Patent: April 21, 2009Assignee: Genetech Inc.Inventors: Charles W. Eigenbrot, Jagath Reddy Junutula, Henry Lowman, Helga E. Raab, Richard Vandlen
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Patent number: 7399869Abstract: Amino terminus-blocked peptide boronate compounds of Formulas I and II are useful for inhibiting Fibroblast Activation Protein (FAP) and other proteases, and for treating disorders mediated by FAP. Methods of using the amino terminus blocked peptide boronate compounds, and stereoisomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Type: GrantFiled: May 18, 2006Date of Patent: July 15, 2008Assignee: Genentech, Inc.Inventors: Frederick Cohen, Wayne J. Fairbrother, Clifford Quan, Daniel P. Sutherlin, Beni B. Wolf
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Patent number: 7375078Abstract: The present invention provides heterocyclic linker compounds useful for linking drug moieties to ligands. The compounds also include drug-ligand conjugates comprising a ligand capable of targeting a selected cell population, and a drug connected to the ligand by a heterocyclic linker moiety. The linker moiety comprises a peptide sequence that is a substrate for an intracellular enzyme, for example a cathepsin, that cleaves the peptide at an amide bond. The peptide further contains a self-immolating moiety which connects the drug and the protein peptide sequence. Upon cleavage of the peptide sequence by an intracellular enzyme the self-immolating moiety cleaves itself from the drug moiety such that the drug moiety is in an underivatized and active form.Type: GrantFiled: February 22, 2005Date of Patent: May 20, 2008Assignee: Genentech, Inc.Inventor: Bainian Feng
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Patent number: 7057025Abstract: Binary probe and clamp compositions conduct methods for target hybridization detection. Where the probe is a substrate for exonuclease cleavage, the composition provides quantitation and detection of PCR products, by real-time and end-point measurements. Where the probe is an amplification primer, the composition provides an improved method for labelling and detection of PCR products. Probes and clamps may be labelled with fluorescent dyes, quenchers, hybridization-stabilizing moieties, chemiluminescent dyes, and affinity ligands. Clamps may be nucleic acid analogs, such as 2-aminoethylglycine PNA.Type: GrantFiled: March 28, 2002Date of Patent: June 6, 2006Assignee: Applera CorporationInventors: Kenneth J. Livak, Michael Egholm, Michael W. Hunkapiller
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Patent number: 7038063Abstract: Atropisomeric energy-transfer dye compounds are disclosed. A variety of molecular biology applications utilize atropisomeric xanthene fluorescent dyes as labels for substrates such as nucleotides, nucleosides, polynucleotides, polypeptides and carbohydrates. Methods include DNA sequencing, DNA fragment analysis, PCR, SNP analysis, oligonucleotide ligation, amplification, minisequencing, and primer extension.Type: GrantFiled: November 18, 2003Date of Patent: May 2, 2006Assignee: Applera CorporationInventors: Linda G. Lee, Meng C. Taing, Barnett B. Rosenblum
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Patent number: 7018431Abstract: Sulfonated diarylrhodamine compounds are useful as fluorescent labels of nucleosides, nucleotides, polynucleotides, and polypeptides. The compounds find particular application in the area of fluorescent nucleic acid analysis, e.g., automated DNA sequencing and fragment analysis, detection of probe hybridization in hybridization arrays, detection of nucleic acid amplification products, and the like.Type: GrantFiled: June 24, 2003Date of Patent: March 28, 2006Assignee: Applera CorporationInventors: Steven M. Menchen, Scott C. Benson, Joe Y. L. Lam, Weiguo Zhen, Daqing Sun, Barnett B. Rosenblum, Shaheer H. Khan, Meng Taing
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Patent number: 6979530Abstract: Polypeptides labelled with a donor and acceptor pair of dyes selected from a dibenzorhodamine dye and a diamino-benzophenoxazine dye are peptide conjugates which are useful for intracellular and bead-based assays with fluorescence detection. Peptide conjugates with a caspase-recognition site undergo cleavage into peptide fragments which may be detected, located, and quantitated by the changes in fluorescence. Intracellular cleavage of peptide conjugates is correlated with apoptosis.Type: GrantFiled: May 21, 2001Date of Patent: December 27, 2005Assignee: Applera CorporationInventors: Xiongwei Yan, Sheri Miraglia, Pau Miau Yuan
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Patent number: 6919445Abstract: Dibenzorhodamine compounds having the structure are disclosed, including nitrogen- and aryl-substituted forms thereof. In addition, two intermediates useful for synthesizing such compounds are disclosed, a first intermediate having the structure including nitrogen- and aryl-substituted forms thereof, and a second intermediate having the structure including nitrogen- and aryl-substituted forms thereof, wherein substituents at positions C-14 to C18 taken separately are selected from the group consisting of hydrogen, chlorine, fluorine, lower alkyl, carboxylic acid, sulfonic acid, —CH2OH, alkoxy, phenoxy, linking group, and substituted forms thereof. The invention further includes energy transfer dyes comprising the dibenzorhodamine compounds, nucleosides labeled with the dibenzorhodamine compounds, and nucleic acid analysis methods employing the dibenzorhodamine compounds.Type: GrantFiled: May 20, 2003Date of Patent: July 19, 2005Assignee: Applera CorporationInventors: Scott C. Benson, Joe Y. L. Lam, Steven Michael Menchen