Entries |
Document | Title | Date |
20080213289 | RECOMBINANT ANTI-CD30 ANTIBODIES AND USES THEREOF - The present invention relates to methods and compositions for the treatment of Hodgkin's Disease, comprising administering proteins characterized by their ability to bind to CD30, or compete with monoclonal antibodies AC10 or HeFi-1 for binding to CD30, and exert a cytostatic or cytotoxic effect on Hodgkin's disease cells in the absence of effector cells or complement. Such proteins include derivatives of monoclonal antibodies AC10 and HeFi-1. The proteins of the invention can be human, humanized, or chimeric antibodies; further, they can be conjugated to cytotoxic agents such as chemotherapeutic drugs. The invention further relates to nucleic acids encoding the proteins of the invention. The invention yet further relates to a method for identifying an anti-CD30 antibody useful for the treatment or prevention of Hodgkin's Disease. | 09-04-2008 |
20080226659 | METHODS OF TREATMENT USING ANTI-ERBB ANTIBODY-MAYTANSINOID CONJUGATES - 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 anri-ErbB receptor antibody-maytansinoid conjugates. | 09-18-2008 |
20080248053 | MONOMETHYLVALINE COMPOUNDS CAPABLE OF CONJUGATION TO LIGANDS - Auristatin peptides, including MeVal-Val-Dil-Dap-Norephedrine (MMAE) and MeVal-Val-Dil-Dap-Phe (MMAF), were prepared and attached to Ligands through various linkers, including maleimidocaproyl-val-cit-PAB. The resulting ligand drug conjugates were active in vitro and in vivo. | 10-09-2008 |
20080267981 | Compositions and Methods for Delivery of Antitumor Agents - Methods for treating a neoplastic disease with an antibody-cytotoxin conjugate molecule, methods of synthesizing an antibody-cytotoxin conjugate molecule are provided. Compounds that are useful as antibody-cytotoxin conjugate molecule or useful in the synthesis of these molecules are also provided. | 10-30-2008 |
20080279868 | Antibody-Drug Conjugates and Methods of Use - The present disclosure provides antibody-drug conjugates that are potent cytotoxins, wherein the drug is linked to the antibody through a linker. The disclosure is also directed to compositions containing the antibody-drug conjugates, and to methods of treatment using them. | 11-13-2008 |
20080286291 | Betulinol Derivatives as Anti-Hiv Agents - The present invention relates to methods of treating HIV-1 infection in a subject. These methods involve administering to the subject with HIV-1 infection a therapeutically effective amount of a conjugated or immunoconjugated betulinol derivative compound, or a pharmaceutically acceptable salt or derivative thereof, under conditions effective to treat the subject for HIV-1 infection. Also disclosed are methods inhibiting HIV-1 activity in a cell. These methods involve providing a cell infected with HIV-1 and contacting the cell with a conjugated or immunoconjugated betulinol derivative compound, or a pharmaceutically acceptable salt or derivative thereof, under conditions effective to inhibit HIV-1 activity in the cell. | 11-20-2008 |
20090010945 | Partially Loaded Antibodies And Methods Of Their Conjugation - A protein containing one or more activatable groups, e.g., an antibody, is subjected to partial or complete reduction of one or more such bonds to form reactive groups; the resulting protein is reacted with a drug which is reactive with some of the reactive groups, such as certain radiometals, chelating agents, and toxins, so as to form a conjugate useful in, e.g., in vitro diagnosis, in vivo imaging, and therapy. | 01-08-2009 |
20090047296 | MONOMETHYLVALINE COMPOUNDS CAPABLE OF CONJUGATION TO LIGANDS - Auristatin peptides, including MeVal-Val-Dil-Dap-Norephedrine (MMAE) and MeVal-Val-Dil-Dap-Phe (MMAF), were prepared and attached to Ligands through various linkers, including maleimidocaproyl-val-cit-PAB. The resulting ligand drug conjugates were active in vitro and in vivo. | 02-19-2009 |
20090068206 | Delivery of pharmaceutical agents via the human insulin receptor - A humanized murine antibody is provided that binds to the human insulin receptor (HIR). The humanized murine antibody is suitable for use as a Trojan horse to deliver pharmaceutical agents to human organs and tissue that express the HIR. The humanized murine antibody is especially well suited for delivering neuropharmaceutical agents from the blood stream to the brain across the blood brain barrier (BBB). The humanized murine antibody may be genetically fused to the pharmaceutical agent or it may be linked to the pharmaceutical agent using an avidin-biotin conjugation system. | 03-12-2009 |
20090142361 | DRUG CONJUGATE COMPOSITION - The invention provides a lyophilized composition comprising a therapeutically effective amount of a conjugate comprising an antibody chemically coupled to a maytansinoid. The invention further provides a method for killing a cell in a human comprising administering to the human the reconstituted composition such that the antibody binds to the surface of the cell and the cytotoxicity of the maytansinoid is activated, whereby the cell is killed. | 06-04-2009 |
20090191225 | Stably Tethered Structures of Defined Compositions with Multiple Functions or Binding Specificities - The present invention concerns methods and compositions for stably tethered structures of defined compositions with multiple functionalities and/or binding specificities. Particular embodiments concern stably tethered structures comprising a homodimer of a first monomer, comprising a dimerization and docking domain attached to a first precursor, and a second monomer comprising an anchoring domain attached to a second precursor. The first and second precursors may be virtually any molecule or structure, such as antibodies, antibody fragments, antibody analogs or mimetics, aptamers, binding peptides, fragments of binding proteins, known ligands for proteins or other molecules, enzymes, detectable labels or tags, therapeutic agents, toxins, pharmaceuticals, cytokines, interleukins, interferons, radioisotopes, proteins, peptides, peptide mimetics, polynucleotides, RNAi, oligosaccharides, natural or synthetic polymeric substances, nanoparticles, quantum dots, organic or inorganic compounds, etc. The disclosed methods and compositions provide a simple, easy to purify way to obtain any binary compound attached to any monomeric compound, or any trinary compound. | 07-30-2009 |
20090232833 | POLYALKYLENE OXIDES HAVING HINDERED ESTER-BASED BIODEGRADABLE LINKERS - The present invention provides polymeric delivery systems including hindered ester moieties. Methods of making the polymeric delivery systems and methods of treating mammals using the same are also disclosed. | 09-17-2009 |
20090246211 | Molecular constructs suitable for targeted conjugates - The present invention relates generally to effective drug-linker constructs suitable for conjugation with ligands. The present invention also discloses methods of conjugating these constructs with peptides to form the compound of formula I. These methods are readily extended to any hydroxyl, amine or sulfur bearing biologically active molecules. | 10-01-2009 |
20090274713 | CROSS-LINKERS AND THEIR USES - Charged or pro-charged cross-linking moieties and conjugates of cell binding agents and drugs comprising the charged or pro-charged cross-linking moieties and method of making the same. | 11-05-2009 |
20090324621 | Drug conjugates and their use for treating cancer, an autoimmune disease or an infectious disease - Drug-Linker-Ligand Conjugates are disclosed in which a Drug is linked to a Ligand via a peptide-based Linker unit. In one embodiment, the Ligand is an Antibody. Drug-Linker compounds and Drug compounds are also disclosed. Methods for treating cancer, an autoimmune disease or an infectious disease using the compounds and compositions of the invention are also disclosed. | 12-31-2009 |
20100021483 | HUMANIZED ANTI-5T4 ANTIBODIES AND ANTI-5T4/CALICHEAMICIN CONJUGATES - Chimeric and humanized anti-5T4 antibodies and antibody/drug conjugates and methods for preparing and using the same. | 01-28-2010 |
20100028370 | MEGALIN-BASED DELIVERY OF THERAPEUTIC COMPOUNDS TO THE BRAIN AND OTHER TISSUES - The present invention is directed to a methods and compositions for receptor mediated drug delivery, particularly across the blood-brain barrier. | 02-04-2010 |
20100034837 | ANTHRACYCLINE DERIVATIVE CONJUGATES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS ANTITUMOR COMPOUNDS - The present invention relates to conjugates of therapeutically useful anthracyclines with carriers such as polyclonal and monoclonal antibodies, proteins or peptides of natural or synthetic origin; methods for their preparation, pharmaceutical composition containing them and use thereof in treating certain mammalian tumors. | 02-11-2010 |
20100062008 | DRUG CONJUGATES AND THEIR USE FOR TREATING CANCER, AN AUTOIMMUNE DISEASE OR AN INFECTIOUS DISEASE - Drug-Linker-Ligand Conjugates are disclosed in which a Drug is linked to a Ligand via a peptide-based Linker unit. In one embodiment, the Ligand is an Antibody. Drug-Linker compounds and Drug compounds are also disclosed. Methods for treating cancer, an autoimmune disease or an infectious disease using the compounds and compositions of the invention are also disclosed. | 03-11-2010 |
20100074910 | Achievement of a high therapeutic index through molecular imaging guided targeted drug treatment - The present disclosure provides methods for treating cancer in a patient in need of such treatment, the method includes prequalifying a patient's therapeutic treatment by performing a molecular imaging procedure to the patient using a labeled biomarker specific for a cancer target at the tumor site; and administering a therapeutic effective amount of a compound comprising a targeting agent linked to a chemotherapeutic or a targeting agent linked to an antibody. Embodiments of the present invention also include compounds and compositions for using such methods. | 03-25-2010 |
20100092495 | POTENT CELL-BINDING AGENT DRUG CONJUGATES - The present invention relates to the use of about 2 to about 8 drug molecules, for example, maytansinoid, per cell binding agent, such as an antibody, and maximal efficacy as compared to a drug load of lesser or higher number of drugs linked to such a cell binding agent. | 04-15-2010 |
20100092496 | CHEMICAL LINKERS AND CONJUGATES THEREOF - The present disclosure provides drug-ligand conjugates that are potent cytotoxins, wherein the drug is linked to the ligand through either a peptidyl, hydrazine, or disulfide linker. The disclosure is also directed to compositions containing the drug-ligand conjugates, and to methods of treatment using them. | 04-15-2010 |
20100104589 | Immunoconjugates with an Intracellularly-Cleavable Linkage - The present invention relates to therapeutic conjugates with improved ability to target various diseased cells containing a targeting moiety (such as an antibody or antibody fragment), a linker and a therapeutic moiety, and further relates to processes for making and using the conjugates. | 04-29-2010 |
20100119529 | ELASTIN-LIKE POLYMER DELIVERY VEHICLES - In invention concerns elastin-like polymer (ELP) drug delivery compositions and methods for the use thereof. In some aspects ELP delivery vehicles may be used to deliver therapeutic drugs such as Hsp90 antagonists. Furthermore, embodiments of the invention concern in vivo delivery with ELP compositions directed to target sites by the application of local hyperthermia therapy. Methods of the invention may have particular utility in the delivery of geldanamycin and related drugs. | 05-13-2010 |
20100136033 | METHODS OF TREATMENT USING ANTI-ErbB ANTIBODY-MAYTANSINOID CONJUGATES - 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. | 06-03-2010 |
20100183636 | ANTI-CD70 ANTIBODY-DRUG CONJUGATES AND THEIR USE FOR THE TREATMENT OF CANCER AND IMMUNE DISORDERS - Disclosed are anti-CD70 antibodies and derivatives thereof conjugated to cytotoxic, immunosuppressive, or other therapeutic agents, as well as pharmaceutical compositions and kits comprising the antibody- and antibody derivative-drug conjugates. Also disclosed are methods, for the treatment of CD70-expressing cancers and immunological disorders, comprising administering to a subject the disclosed pharmaceutical compositions. | 07-22-2010 |
20100255014 | Protein Complex Using An Immunoglobulin Fragment and Method For The Preparation Thereof - Disclosed are a protein conjugate with improved in vivo duration and stability and the use thereof. The protein conjugate includes a physiologically active polypeptide, a non-peptide polymer and an immunoglobulin Fc fragment. Since the three components are covalently linked, the protein conjugate has extended in vivo duration and enhanced stability for the physiologically active polypeptide. The protein conjugate maintains the in vivo activity at relatively high levels and remarkably increases the serum half-life for the physiologically active polypeptide, with less risk of inducing undesirable immune responses. Thus, the protein conjugate is useful for developing long-acting formulations of various polypeptide drugs. | 10-07-2010 |
20100260786 | METHODS OF TREATING DRUG-RESISTANT CANCERS - Methods of treating a refractory or drug resistant cancer, cell proliferative disorder and tumor cells are provided. | 10-14-2010 |
20110002947 | LEPTOMYCIN DERIVATIVES - Leptomycin derivatives having a moiety, such as a sulfide or a disulfide, that can conjugate to a cell binding reagent such as an antibody are disclosed. The therapeutic use of such leptomycin derivative conjugates is also described; such conjugates have therapeutic use because they can deliver cytotoxic leptomycin derivatives to a specific cell population in a targeted fashion. | 01-06-2011 |
20110020373 | IGE DIRECTED DNA VACCINATION - This invention is directed to a novel approach for focusing and expressing DNA vaccinates in Antigen Presenting Cells (APCs) mediated through targeting IgE receptors (FcεRs) on APC and driving DNA expression through provision of an APC specific regulatory element This vaccine can be used in the prevention or treatment of allergic disease. | 01-27-2011 |
20110250216 | METHODS FOR KILLING PSMA-EXPRESSING, TAXANE-RESISTANT CANCER CELLS - Methods of killing prostate-specific membrane antigen (PSMA)-expressing, taxane-resistant cancer cells are provided. In particular, PSMA-expressing, taxane-resistant cancer cells are contacted with an antibody-drug conjugate (ADC) that comprises an antibody or antigen-binding fragment thereof that specifically binds to PSMA conjugated to monomethylauristatin norephedrine or monomethylauristatin phenylalanine. | 10-13-2011 |
20110256157 | PYRROLOBENZODIAZEPINES AND CONJUGATES THEREOF - Conjugates and compounds for making conjugates which are PBD molecules linked via the N10 position are disclosed, along with the use of the conjugates for treating proliferative diseases, including cancer. | 10-20-2011 |
20110268751 | Weekly Dosing Regimens for Anti-CD30 VC-PAB-MMAE Antibody Drug-Conjugates - Methods for the treatment of CD30-expressing cancers are provided. The methods comprise administering to a subject in need thereof a weekly dose of from about 0.8 mg/kg to about 1.8 mg/kg of an antibody-drug conjugate compound having formula (I); or a pharmaceutically acceptable salt thereof; wherein: mAb is an anti-CD30 antibody unit, S is a sulfur atom of the antibody, A—is a Stretcher unit, and p is from about 3 to about 5. | 11-03-2011 |
20110280891 | SITE-SPECIFIC ATTACHMENT OF DRUGS OR OTHER AGENTS TO ENGINEERED ANTIBODIES WITH C-TERMINAL EXTENSIONS - The present invention provides antibodies (e.g., IgG antibodies) having C-terminal cysteine-containing extensions that facilitate antibody conjugation to a partner molecule (e.g. a drug, toxin, marker molecule, protein, radioisotope, or other therapeutic agent). Methods of making, screening and selecting the antibodies of the invention are provided. | 11-17-2011 |
20110287036 | NOVEL CANCER TARGETING THERAPY USING COMPLEX OF SUBTANCE CAPABLE OF BINDING SPECIFICALLY TO CONSTITUENT FACTOR OF CANCER STROMA AND ANTI-TUMOR COMPOUND - The present invention is intended to provide a pharmaceutical for tumor treatment that stays specifically in interstitium for a long time and exhibits an effect, and provides a complex consisting of a substance having specific binding affinity for stroma and an antitumor compound bound to the substance via a linker. | 11-24-2011 |
20110300162 | DRUG CONJUGATE COMPOSITION - The invention provides a liquid composition and a lyophilized composition comprising a therapeutically effective amount of a conjugate comprising an antibody chemically coupled to a maytansinoid. The invention further provides a method for killing a cell in a human comprising administering to the human either of the compositions such that the antibody binds to the surface of the cell and the cytotoxicity of the maytansinoid is activated, whereby the cell is killed. | 12-08-2011 |
20120100160 | Methods for Inducing Mixed Chimerism - Fusion protein-siRNA complexes that specifically target activated T cells, and methods of use thereof, are described. | 04-26-2012 |
20120107332 | Beta-Glucuronide-Linker Drug Conjugates - Ligand Drug conjugate compounds comprising a β-glucuronide-based linker and methods of using such compounds are provided. | 05-03-2012 |
20120121615 | ALANINYL MAYTANSINOL ANTIBODY CONJUGATES - Linker-drug intermediates of Formula I are conjugated to antibodies to form antibody-drug conjugates where the drug moiety is an N-methylalaninyl-maytansinoid. | 05-17-2012 |
20120141510 | MONOMETHYLVALINE COMPOUNDS CAPABLE OF CONJUGATION TO LIGANDS - Auristatin peptides, including MeVal-Val-Dil-Dap-Norephedrine (MMAE) and MeVal-Val-Dil-Dap-Phe (MMAF), were prepared and attached to Ligands through various linkers, including maleimidocaproyl-val-cit-PAB. The resulting ligand drug conjugates were active in vitro and in vivo. | 06-07-2012 |
20120171227 | PRO-DRUG COMPLEXES AND RELATED METHODS OF USE - The present invention provides methods, compositions and applications for efficient, site-specific drug delivery using pro-drug complexes comprising therapeutic agents and one or more functional groups (e.g., imaging agents, targeting agents, and trigger agents). In particular, the present invention relates to pro-drug complexes comprising one or more functional groups conjugated with a therapeutic agent (e.g., a chemotherapeutic agent), methods of synthesizing the same, as well as systems and methods utilizing the therapeutic and diagnostic compositions (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer) diagnosis and/or therapy, etc.)). | 07-05-2012 |
20120213804 | CALICHEAMICIN DERIVATIVE-CARRIER CONJUGATES - Methods for preparing monomeric cytotoxic drug/carrier conjugates with a drug loading significantly higher than in previously reported procedures and with decreased aggregation and low conjugate fraction (LCF) are described. Cytotoxic drug derivative/antibody conjugates, compositions comprising the conjugates and uses of the conjugates are also described. Monomeric calicheamicin derivative/anti-CD22 antibody conjugates, compositions comprising the conjugates and uses of the conjugates are also described. | 08-23-2012 |
20120244171 | CYTOTOXIC BENZODIAZEPINE DERIVATIVES - The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepine compounds of formula (I)-(VII). The invention also provides conjugates of the benzodiazepine compounds linked to a cell-binding agent. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention. | 09-27-2012 |
20120244172 | Conjudates of Pyrrolo[1,4]Benzodiazepine Dimers As Anticancer Agents - The present invention relates to pyrrolo[1,4]benzodiazepine (PBD) dimer conjugates, to the compositions comprising them and to their therapeutic application, in particular as anticancer agents. The invention also relates to the process for the preparation of the conjugates, to their application as anticancer agents and to the dimers themselves. | 09-27-2012 |
20120251558 | ANTIBODY-DRUG CONJUGATES - Disclosed are anti-5T4 antibody drug conjugates and methods for preparing and using the same. | 10-04-2012 |
20120251559 | Treatment of B-Cell Cancers With Anti-CD70 Antibody-Drug Conjugates - Disclosed are anti-CD70 antibodies and derivatives thereof conjugated to cytotoxic therapeutic agents, as well as pharmaceutical compositions and kits comprising the antibody- and antibody derivative-drug conjugates. Also disclosed are methods, for the treatment of a CD70-expressing cancer, comprising administering to a subject the disclosed pharmaceutical compositions. | 10-04-2012 |
20120282282 | Methods for Decreasing Ocular Toxicity of Antibody Drug Conjugates - The invention relates to charged or pro-charged cross-linking moieties and conjugates of cell binding agents and drugs comprising the charged or pro-charged cross-linking moieties and method of using the same to reduce ocular toxicity associated with administration of antibody drug conjugates. | 11-08-2012 |
20120288512 | Anti-CD70 Antibody-Drug Conjugates and Their Use for the Treatment of Cancer and Immune Disorders - Disclosed are anti-CD70 antibodies and derivatives thereof conjugated to cytotoxic, immunosuppressive, or other therapeutic agents, as well as pharmaceutical compositions and kits comprising the antibody- and antibody derivative-drug conjugates. Also disclosed are methods, for the treatment of CD70-expressing cancers and immunological disorders, comprising administering to a subject the disclosed pharmaceutical compositions. | 11-15-2012 |
20120301490 | IMMUNOCONJUGATES, COMPOSITIONS FOR MAKING THEM, AND METHODS OF MAKING AND USE - An immunoconjugate in which a phosphate-prodrugged DNA minor groove binding agent of formula (I), where X is a nucleophilically displaceable leaving group, is conjugated to an antibody or an antigen binding fragment of an antibody, and compounds that can be used for making such immunoconjugates, and uses of such immunoconjugates. | 11-29-2012 |
20120328634 | Immunoconjugates with an Intracellularly-Cleavable Linkage - The invention relates to therapeutic conjugates with improved ability to target various cancer cells containing a targeting moiety and a therapeutic moiety. The targeting and therapeutic moieties are linked via an acid cleavable linkage that increases therapeutic efficacy of the immunoconjugate. | 12-27-2012 |
20130011419 | CROSS-LINKERS AND THEIR USES - Charged or pro-charged cross-linking moieties and conjugates of cell binding agents and drugs comprising the charged or pro-charged cross-linking moieties and method of making the same. | 01-10-2013 |
20130022627 | Combination Therapy With Antibody-Drug Conjugates - Methods for the treatment of Hodgkin's lymphoma comprising administering both a chemotherapeutic regimen and an antibody-drug conjugate compound to a subject in need thereof are provided. | 01-24-2013 |
20130028919 | TARGETED PYRROLOBENZODIAZAPINE CONJUGATES - Provided are Conjugate comprising PBDs conjugated to a targeting agent and methods of using such PBDs. | 01-31-2013 |
20130156796 | Method of Treatment of Tumors That Are Resistant to EGFR Therapies by EGFR Antibody Cytotoxic Agent Conjugate - The present invention relates to the identification that EGFR antibody immunoconjugates are effective in inhibiting the growth of tumor cells that have developed EGFR and/or ALK resistance mechanisms. Methods of administering the EGFR antibody immunoconjugates to patients having resistant tumor cells is also disclosed. | 06-20-2013 |
20130171176 | Anthracycline-Antibody Conjugates for Cancer Therapy - The invention relates to therapeutic conjugates with the ability to target various antigens. The conjugates contain a targeting antibody or antigen binding fragment thereof and an anthracycline chemotherapeutic drug. The targeting antibody and the chemotherapeutic drug are linked via a linker comprising a hydrazide moiety. | 07-04-2013 |
20130216561 | Immunoconjugates with an Intracellularly-Cleavable Linkage - The invention relates to therapeutic conjugates with improved ability to target various cancer cells containing a targeting moiety and a therapeutic moiety. The targeting and therapeutic moieties are linked via an acid cleavable linkage that increases therapeutic efficacy of the immunoconjugate. | 08-22-2013 |
20130224229 | Novel Curcumin-Antibody Conjugates as Anti-Cancer Agents - The invention relates to curcumin derivatives having the formula I: wherein: Z represents: H | 08-29-2013 |
20130259882 | Conjugate of Folate and Antibody Preparation Method and Use Thereof - Anti-tumor conjugates, which consists of foliate or analogues thereof, linkers, an antibodies such as immunoglobulin G. The linker comprises glutathione, cysteamine or cysteine residue, and further comprises N-hydroxysuccinimide. The Conjugates target folate-receptor-positive tumor cells. Also provided are preparation methods and anti-tumor and anti-autoimmune disease uses of the conjugates. | 10-03-2013 |
20130266595 | PYRROLOBENZODIAZEPINES AND CONJUGATES THEREOF - A conjugate of formula (A): | 10-10-2013 |
20130266596 | NOVEL BENZODIAZEPINE DERIVATIVES - The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepines of formula (I) and (II), in which the diazepine ring (B) is fused with a heterocyclic ring (CD), wherein the heterocyclic ring is bicyclic or a compound of formula (III), in which the diazepine ring (B) is fused with a heterocyclic ring (C), wherein the heterocyclic ring is monocyclic. The invention provides cytotoxic dimers of these compounds. The invention also provides conjugates of the monomers and the dimers. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention. The invention further relates to methods of using the compounds or conjugates for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions. | 10-10-2013 |
20130280282 | DR5 LIGAND DRUG CONJUGATES - Ligand Drug Conjugates are provided having a DR5 binding moiety attached via linking groups and/or spacers to a therapeutic agent that are effective in treatment of various cancers. | 10-24-2013 |
20130302359 | CYTOTOXIC BENZODIAZEPINE DERIVATIVES - The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepine compounds of formula (I)-(VII). The invention also provides conjugates of the benzodiazepine compounds linked to a cell-binding agent. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention. | 11-14-2013 |
20130309257 | Thiazolidine Linker for the Conjugation of Drugs to Antibodies - In one aspect, there is provided a protein-drug conjugate compound comprising a protein covalently attached by a linker to one or more drug moieties, wherein the linker has a half-life of from 1 hour to 50 hours in phosphate buffered saline at 37° C. A carbonyl derivative of LU103793 is also described that can be used in a protein-drug conjugate compound comprising an antibody covalently attached by a linker to the drug moiety comprising, consisting or consisting essentially of the carbonyl derivative. | 11-21-2013 |
20130323268 | CYTOTOXIC AGENTS COMPRISING NEW ANSAMITOCIN DERIVATIVES - New ansamitocin derivatives bearing a linking group are disclosed. Also disclosed are methods for the synthesis of these new ansamitocin derivatives and methods for their linkage to cell-binding agents. The ansamitocin derivative-cell-binding agent conjugates are useful as therapeutic agents, which are delivered specifically to target cells and are cytotoxic. These conjugates display vastly improved therapeutic efficacy in animal tumor models compared to the previously described agents. | 12-05-2013 |
20140030279 | ANTI-CD22 ANTIBODIES AND IMMUNOCONJUGATES - The invention provides anti-CD22 antibodies and immunoconjugates and methods of using the same. | 01-30-2014 |
20140030280 | ANTI-CD79B ANTIBODIES AND IMMUNOCONJUGATES - The invention provides anti-CD79b antibodies and immunoconjugates and methods of using the same. | 01-30-2014 |
20140030281 | ANTI-CD22 ANTIBODIES AND IMMUNOCONJUGATES - The invention provides anti-CD22 antibodies and immunoconjugates and methods of using the same. | 01-30-2014 |
20140030282 | ANTI-CD79B ANTIBODIES AND IMMUNOCONJUGATES - The invention provides anti-CD79b antibodies and immunoconjugates and methods of using the same. | 01-30-2014 |
20140056926 | COMPLEX IN WHICH ANTI-COTININE ANTIBODY IS BOUND TO CONJUGATE OF COTININE AND BINDING SUBSTANCE, AND USE THEREOF - The present invention relates to a complex in which an anti-cotinine antibody is bound to a conjugate of a binding material and cotinine, and a use of the complex. The complex according to the present invention may be used as an analysis tool in an in vitro biological assay method, and may retain the specific reactivity and the biological function of the binding material, and the capabilities of inducing complement-mediated cell cytotoxicity (CDC) and antibody-dependent cell cytotoxicity (ADCC) and a prolonged in vivo half-life, which are intrinsic characteristics of an antibody. | 02-27-2014 |
20140079721 | COMPOSITIONS AND METHODS FOR THE DIAGNOSIS AND TREATMENT OF TUMOR - The present invention is directed to compositions of matter useful for the diagnosis and treatment of tumor in mammals and to methods of using those compositions of matter for the same. | 03-20-2014 |
20140079722 | EXTRACELLULAR TARGETED DRUG CONJUGATES - Antibodies targeting the dysadherin subunit of the human Na,K-ATPase signaling complex that are covalently linked via a stable linker to steroid drugs that bind the alpha subunit of that complex are useful in the treatment of cancer. | 03-20-2014 |
20140093523 | Anti-Integrin Immunoconjugates, Methods and Uses - The invention relates to conjugates of anti-integrin specific antibodies with cytotoxic compounds, the synthesis, selection, and use of such conjugates for use in cancer therapy or other diseases mediated by cell proliferation, cell migration, or inflammation and which pathology involves angiogenesis or neovascularization of new tissue. In addition the invention relates to combination therapy of such diseases wherein the treatment comprises use of said conjugates in combination with one or more other treatment modalities including but not limited to: chemotherapy, surgery or radiation therapy. The preferred conjugates contain maytansinoid compounds linked to the antibody by a disulfide linkage, and preferred chemotherapeutic agents are doxorubicin, a taxane, a camptothecin, a podophyllotoxin, a nucleoside analog, or a pyrimidine analog. | 04-03-2014 |
20140105922 | Variant Target Binding Agents and Uses Thereof - The present invention provides variant target binding agents and methods relating to the use of such binding agents for the prophylaxis or treatment of cancers and immunological disorders. The variant target binding agent is conjugated to a therapeutic agent that exerts a cytotoxic, cytostatic, or immunomodulatory effect on target cells. | 04-17-2014 |
20140127239 | PYRROLOBENZODIAZEPINES AND CONJUGATES THEREOF - A compound which is either A: | 05-08-2014 |
20140127240 | Novel Binder-Drug Conjugates (ADCs) and Use of Same - The present patent application relates to novel binder-drug conjugates (ADCs) of N,N-dialkylauristatins directed against the target epidermal growth factor receptor (EGFR, gene ID 1956), effective metabolites of these ADCs, methods for producing these ADCs, use of these ADCs for treatment and or prevention of diseases as well as the use of these ADCs to produce pharmaceutical drugs for treatment and/or prevention of diseases, in particular hyperproliferative and/or angiogenic diseases such as cancer, for example. Such treatments may be administered as monotherapy or in combination with other pharmaceutical drugs or other therapeutic measures. | 05-08-2014 |
20140134193 | SPLICEOSTATIN ANALOGS AND METHODS FOR THEIR PREPARATION - The present invention is directed to novel cytotoxic spliceostatin analogs and derivatives, to antibody drug conjugates thereof, and to methods for using the same to treat medical conditions including cancer. | 05-15-2014 |
20140141025 | HYDRAZINYL-INDOLE COMPOUNDS AND METHODS FOR PRODUCING A CONJUGATE - The present disclosure provides conjugate structures (e.g., polypeptide conjugates) and hydrazinyl-indole compounds used to produce these conjugates. The disclosure also provides methods of production of such conjugates, as well as methods of using the same. | 05-22-2014 |
20140154273 | Anthracycline-Antibody Conjugates for Cancer Therapy - The invention relates to therapeutic conjugates with the ability to target various antigens. The conjugates contain a targeting antibody or antigen binding fragment thereof and an anthracycline chemotherapeutic drug. The targeting antibody and the chemotherapeutic drug are linked via a linker comprising a hydrazide moiety. | 06-05-2014 |
20140161828 | BCMA ANTIGEN BINDING PROTEINS - The present invention relates to BCMA (B-Cell Maturation Antigen) antigen binding proteins, such as antibodies, polynucleotide sequences encoding said antigen binding proteins, and compositions and methods for diagnosing and treating diseases. The present invention also relates to BCMA antibody drug conjugates. | 06-12-2014 |
20140161829 | ANTIBODY-ACTIVE AGENT CONJUGATES AND METHODS OF USE - The invention provides protein-active agent conjugates having an amino acid motif that can be recognized by an isoprenoid transferase. The invention also provides compositions containing the conjugates. The invention further provides methods for using the conjugates to deliver the active agent to a target cell, as well as methods for using the conjugates to treat a subject in need thereof (e.g., a subject in need of the active agent). | 06-12-2014 |
20140178411 | COMPOUNDS AND METHODS FOR THE TREATMENT OF CD20 POSITIVE DISEASES - Disclosed herein are anti-CD20 antibody conjugated with maytansinoid drugs for targeted delivery to disease tissues. Methods related to the preparation and uses of such antibody drug conjugates to treat CD20 positive cells in cancers are provided. | 06-26-2014 |
20140178412 | COMPOUNDS AND METHODS FOR THE TREATMENT OF EGFR POSITIVE DISEASES - Disclosed herein are anti-EGFR antibodies conjugated with maytansinoid drugs for targeted delivery to disease tissues. Methods related to the preparation and uses of such antibody drug conjugates to treat EGFR positive cells in cancers are provided. | 06-26-2014 |
20140178413 | COMPOUNDS AND METHODS FOR THE TREATMENT OF ERB B2/NEU POSITIVE DISEASES - Disclosed herein are anti-ERB B2/NEU antibodies conjugated with maytansinoid drugs for targeted delivery to disease tissues. Methods relating to the preparation and uses of such drug conjugates to treat ERB B2/NEU positive cells in cancers are provided. | 06-26-2014 |
20140178414 | MAYTANSINOID DERIVATIVES - Disclosed herein are maytansinoid drug linker derivatives which can be linked to a antigen binding unit (Abu), and maytansinoid drugs linked with an antigen binding unit (Drug-Linker-Antigen binding Unit: D-L-Abu), for targeted delivery to disease tissues. D-L-Abu, D-L-Abu derivatives, and methods relating to the use of such drug conjugates to treat antigen positive cells in cancers and immunological disorders are provided. | 06-26-2014 |
20140178415 | MAYTANSINOID DERIVATIVES - Disclosed herein are maytansinoid drug linker derivatives which can be linked to a antigen binding unit (Abu), and maytansinoid drugs linked with an antigen binding unit (Drug-Linker-Antigen binding Unit: D-L-Abu), for targeted delivery to disease tissues. D-L-Abu, D-L-Abu derivatives, and methods relating to the use of such drug conjugates to treat antigen positive cells in cancers and immunological disorders are provided. | 06-26-2014 |
20140178416 | CROSS-LINKERS AND THEIR USES - Charged or pro-charged cross-linking moieties and conjugates of cell binding agents and drugs comprising the charged or pro-charged cross-linking moieties and method of making the same. | 06-26-2014 |
20140193437 | HYDROPHILIC SELF-IMMOLATIVE LINKERS AND CONJUGATES THEREOF - The present disclosure provides compounds with a hydrophilic self-immolative linker, which is cleavable under appropriate conditions and incorporates a hydrophilic group to provide better solubility of the compound. The compounds of the present disclosure comprise a drug moiety, a targeting moiety capable of targeting a selected cell population, and a linker which contains an acyl unit, an optional spacer unit for providing distance between the drug moiety and the targeting moiety, a peptide linker which can be cleavable under appropriate conditions, a hydrophilic self-immolative linker, and an optional second self-immolative spacer or cyclization self-elimination linker. | 07-10-2014 |
20140193438 | ENEDIYNE COMPOUNDS, CONJUGATES THEREOF, AND USES AND METHODS THEREFOR - Enediyne compounds having a structure according to formula (I), where R | 07-10-2014 |
20140220046 | Sialic Acid Derivatives For Protein Derivatisation And Conjugation - Derivatives are synthesised of starting materials, usually polysaccharides, having sialic acid at the reducing terminal end, in which the reducing terminal unit is transformed into an aldehyde group. Where the polysaccharide has a sialic acid unit at the non-reducing end it may be passivated, for instance by converting into hydroxyl-substituted moiety. The derivatives may be reacted with substrates, for instance containing amine or hydrazine groups, to form non-cross-linked polysialylated compounds. The substrates may, for instance, be therapeutically useful drugs peptides or proteins or drug delivery systems. | 08-07-2014 |
20140220047 | MONOMETHYLVALINE COMPOUNDS CAPABLE OF CONJUGATION TO LIGANDS - Auristatin peptides, including MeVal-Val-Dil-Dap-Norephedrine (MMAE) and MeVal-Val-Dil-Dap-Phe (MMAF), were prepared and attached to Ligands through various linkers, including maleimidocaproyl-val-cit-PAB. The resulting ligand drug conjugates were active in vitro and in vivo. | 08-07-2014 |
20140234345 | NOVEL ANTI-CANCER ISOCARBOSTYRIL ALKALOID CONJUGATES - The present application is directed to covalent conjugates between an isocarbostyril alkaloid and a lipophilic biomolecule, to pharmaceutical compositions comprising the conjugates and to therapeutic uses thereof, in particular for treating cancer. | 08-21-2014 |
20140234346 | PYRROLOBENZODIAZEPINES - A compound with the formula I: wherein: R | 08-21-2014 |
20140271688 | ANTIBODY DRUG CONJUGATES - The present invention relates to anti-cKIT antibodies, antibody fragments, antibody drug conjugates, and their uses for the treatment of cancer. | 09-18-2014 |
20140286969 | ANTI-EGFR ANTIBODY DRUG CONJUGATE FORMULATIONS - The invention provides a stable formulation comprising an anti-EGFR antibody drug conjugate (ADC), including an anti-EGFR antibody, e.g., antibody 1, conjugated to an auristatin, e.g., MMAF, histidine, a sugar, and a surfactant. | 09-25-2014 |
20140286970 | PYRROLOBENZODIAZEPINES AND TARGETED CONJUGATES - A compound, or a pharmaceutically acceptable salt or solvate thereof, or conjugates thereof, selected from the group consisting of formula wherein: (a) R | 09-25-2014 |
20140294867 | SITE-SPECIFIC ANTIBODY-DRUG CONJUGATION THROUGH GLYCOENGINEERING - The current disclosure provides binding polypeptides (e.g., antibodies), and effector moiety conjugates thereof (e.g., antibody-drug conjugates or ADCs), comprising a site-specifically engineered drug-glycan linkage within native or engineered glycans of the binding polypeptide. The current disclosure also provides nucleic acids encoding the antigen-binding polypeptides, recombinant expression vectors and host cells for making such antigen-binding polypeptides. Methods of using the antigen-binding polypeptides disclosed herein to treat disease are also provided. | 10-02-2014 |
20140294868 | PYRROLOBENZODIAZEPINES AND CONJUGATES THEREOF - Conjugate compounds of formula (A): | 10-02-2014 |
20140302066 | PYRROLOBENZODIAZEPINES AND TARGETED CONJUGATES - This invention relates to pyrrolobenzodiazepines (PBDs), in particular pyrrolobenzodiazepine dimers having a C2-C3 double bond and an aryl group at the C2 position in each monomer unit, and their inclusion in targeted conjugates. The differing substituent groups may offer advantages in the preparation and use of the compounds, particularly in their biological properties and the synthesis of conjugates, and the biological properties of these conjugates. | 10-09-2014 |
20140308302 | ANTI-5T4 ANTIBODIES AND USES THEREOF - Anti-5T4 antibodies, anti-5T4 antibody/drug conjugates, and methods for preparing and using the same. | 10-16-2014 |
20140314794 | COMPOSITIONS AND METHODS FOR THE DIAGNOSIS AND TREATMENT OF TUMOR - The invention is directed to antibody drug conjugate compositions of matter useful for the diagnosis and treatment of tumors in mammals and to methods of using those compositions of matter for the same. | 10-23-2014 |
20140356385 | ENZYMATIC CONJUGATION OF ANTIBODIES - The present application relates to methods for the functionalization of immunoglobulins, in particular with drugs. Also disclosed herein are linking reagents, functionalized antibodies, pharmaceutical compositions, and method of treating disease and/or conditions. | 12-04-2014 |
20140363453 | Methods for Increasing Efficacy of FOLR1 Cancer Therapy - Methods to improve the success of cancer therapies that target the human folate receptor 1 are provided. Kits comprising reagent useful in the methods are further provided. | 12-11-2014 |
20140363454 | Antibody-Drug Conjugates, Compositions and Methods of Use - Antibody-cytotoxin antibody-drug conjugates and related compounds, such as linker-cytotoxin conjugates and the linkers used to make them, tubulysin analogs, and intermediates in their synthesis; compositions; and methods, including methods of treating cancers. | 12-11-2014 |
20140363455 | DLL3 MODULATORS AND METHODS OF USE - Novel modulators, including antibodies and derivatives thereof, and methods of using such modulators to treat proliferative disorders are provided. | 12-11-2014 |
20140370037 | DLL3 MODULATORS AND METHODS OF USE - Novel modulators, including antibodies and derivatives thereof, and methods of using such modulators to treat proliferative disorders are provided. | 12-18-2014 |
20150017188 | CYSTEINE ENGINEERED ANTIBODIES AND CONJUGATES - 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: | 01-15-2015 |
20150017189 | METHODS OF MAKING AND USING NANOSTRUCTURES - The invention provides methods for attaching drugs, dyes or radiolabels to bis-MTX. This method can be used to prepare bis-MTX analogs that can be used to deliver agents, such as nanoparticles, drugs, dyes or radiolabels, to cells. | 01-15-2015 |
20150030618 | NOVEL BINDER-DRUG CONJUGATES (ADCS) AND USE THEREOF - The present application relates to new binder-drug conjugates (ADCs) of N,N-dialkylauristatins that are directed against the target C4.4a, to active metabolites of these ADCs, to processes for preparing these ADCs, to the use of these ADCs for treating and/or preventing illnesses, and also to the use of these ADCs for producing medicaments for treating and/or preventing illnesses, more particularly hyperproliferative and/or angiogenic diseases such as, for example, cancer diseases. Such treatments may be practised as a monotherapy or else in combination with other medicaments or further therapeutic measures. | 01-29-2015 |
20150037360 | Lysosome-Cleavable Linker - The present invention relates to a linker for forming conjugates of a protein or peptide with a therapeutically active agent and which comprise a thiomaleamic acid moiety that is susceptible to cleavage under the pH conditions prevalent in the lysosome. | 02-05-2015 |
20150044238 | METHODS OF USING MONOMETHYLVALINE COMPOSITIONS HAVING PHENYLALANINE CARBOXY MODIFICATIONS AT THE C-TERMINUS - Auristatin peptide analogs of MeVal-Val-Dil-Dap-Phe (MMAF) having a carboxylic acid equivalent at the C-terminal phenylalanine were prepared and attached to ligands through various linkers, including maleimidocaproyl-val-cit-PAB. The resulting ligand-drug conjugates were active in vitro and in vivo in inhibiting cell proliferation and are represented by the general structure of | 02-12-2015 |
20150071949 | CYTOTOXIC AGENTS COMPRISING NEW MAYTANSINOIDS (DM4) - New thiol and disulfide-containing maytansinoids bearing a mono or di-alkyl substitution on the α-carbon atom bearing the sulfur atom are disclosed. Also disclosed are methods for the synthesis of these new maytansinoids and methods for the linkage of these new maytansinoids to cell-binding agents. The maytansinoid-cell-binding agent conjugates are useful as therapeutic agents, which are delivered specifically to target cells and are cytotoxic. These conjugates display vastly improved therapeutic efficacy in animal tumor models compared to the previously described agents. | 03-12-2015 |
20150071950 | C-MET TARGETING COMPOUND-BIOACTIVE MATERIAL CONJUGATE AND USE THEREOF - Disclosed is a conjugate in which a c-Met targeting compound and a bioactive material are chemically conjugated with each other, and methods of use thereof. | 03-12-2015 |
20150104469 | CARRIERS FOR IMPROVED DRUG DELIVERY - The invention provides carriers that enhance the absorption, half-life or bioavailability of therapeutic compounds. The carriers comprise targeting groups that bind the Vitamin D Binding protein (DBP), conjugation groups for coupling the targeting groups to the therapeutic compounds, and optionally scaffolding moieties. | 04-16-2015 |
20150110816 | METHODS OF TREATMENT USING ANTI-ERBB ANTIBODY-MAYTANSINOID CONJUGATES - 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. | 04-23-2015 |
20150110817 | RADIO-PHARMACEUTICAL COMPLEXES - A tissue-targeting complex comprising a tissue targeting moiety, an octadentate hydroxypyridinone-containing ligand comprising four HOPO moieties and the ion of an alpha-emitting thorium radionuclide, where at least one of the four HOPO moieties is substituted at the N-position with a hydroxyalkyl solubilising group. | 04-23-2015 |
20150290152 | AFFINITY MEDICANT CONJUGATE - In an embodiment of the invention, a composition for treating a cell population comprises an Affinity Medicant Conjugate (AMC). The medicant moiety can be a toxin including an acylfulvene or a drug moiety. The affinity moiety can be an antibody, a binding protein, a steroid, a lipid, a growth factor, a protein, a peptide or non peptidic. The affinity moiety can be covalently bound to the medicant via a linker. Novel linkers that can be directed to cysteine, arginine or lysine residues based on solution pH allow greater flexibility in preserving and/or generating specific epitopes in the AMC. | 10-15-2015 |
20150297744 | Anti-FOLR1 Immunoconjugate Dosing Regimens - Methods of administering immunoconjugates that bind to FOLR1 are provided. The methods comprise administering an anti-FOLR1 immunoconjugate to a person in need thereof, for example, a cancer patient, at a therapeutically effective dosing regimen that results in minimal adverse effects. | 10-22-2015 |
20150297747 | TRIOXACARCINS, TRIOXACARCIN-ANTIBODY CONJUGATES, AND USES THEREOF - Provided herein are trioxacarcin-antibody drug conjugates of Formula (A): and pharmaceutically acceptable salts thereof, comprising at least one instance of the group -L | 10-22-2015 |
20150297748 | ANTIBODY-DRUG CONJUGATE - As an antitumor drug which is excellent in terms of antitumor effect and safety, there is provided an antibody-drug conjugate in which an antitumor compound represented by the following formula is conjugated to an antibody via a linker having a structure represented by the following formula: | 10-22-2015 |
20150306243 | ANTIBODY-SN-38 IMMUNOCONJUGATES WITH A CL2A LINKER - The present invention concerns improved methods and compositions for preparing SN-38 conjugates of proteins or peptides, preferably immunoconjugates of antibodies or antigen-binding antibody fragments. More preferably, the SN-38 is attached to the antibody or antibody fragment using a CL2A linker, with 1-12, more preferably 6 or less, most preferably 1-5 SN-38 moieties per antibody or antibody fragment. Most preferably, the immunoconjugate is prepared in large scale batches, with various modifications to the reaction scheme to optimize yield and recovery in large scale. Other embodiments concern optimized dosages and/or schedules of administration of immunoconjugate to maximize efficacy for disease treatment and minimize side effects of administration. | 10-29-2015 |
20150315293 | ANTI-PTK7 ANTIBODY-DRUG CONJUGATES - The present invention provides anti-PTK7 antibody-drug conjugates and methods for preparing and using the same. | 11-05-2015 |
20150320880 | ANTIBODY DRUG CONJUGATES - The present invention relates to anti-cKIT antibodies, antibody fragments, antibody drug conjugates, and their uses for the treatment of cancer. | 11-12-2015 |
20150320881 | COMPOUNDS AND METHODS FOR THE TREATMENT OF ERB B2/NEU POSITIVE DISEASES - Disclosed herein are anti-ERB B2/NEU antibodies conjugated with maytansinoid drugs for targeted delivery to disease tissues. Methods relating to the preparation and uses of such drug conjugates to treat ERB B2/NEU positive cells in cancers are provided. | 11-12-2015 |
20150320882 | MODIFIED ANTIBODY, ANTIBODY-CONJUGATE AND PROCESS FOR THE PREPARATION THEREOF - An antibody comprising a GlcNAc-S(A) | 11-12-2015 |
20150322155 | ACETYLENEDICARBOXYL LINKERS AND THEIR USES IN SPECIFIC CONJUGATION OF A CELL-BINDING MOLECULE - The present invention relates to novel acetylenedicarboxyl linkers used for the specific conjugation of compounds/cytotoxic agents to a cell-binding molecule, through bridge linking pairs of thiols on the cell-binding molecule. The invention also relates to methods of making such linkers, and of using such linkers in making homogeneous conjugates, as well as of application of the conjugates in treatment of cancers, infections and autoimmune disorders. | 11-12-2015 |
20150343082 | METHODS OF MAKING AND USING CHEMICALLY SELF ASSEMBLED-NANORINGS - Provided herein are compounds, conjugates and methods for making lipid-chemically self-assembled nanorings (Lipid-CSANs) and using them to treat diseases and modify cell surfaces. | 12-03-2015 |
20150352222 | HYDROPHILIC SELF-IMMOLATIVE LINKERS AND CONJUGATES THEREOF - The present disclosure provides compounds with a hydrophilic self-immolative linker, which is cleavable under appropriate conditions and incorporates a hydrophilic group to provide better solubility of the compound. The compounds of the present disclosure comprise a drug moiety, a targeting moiety capable of targeting a selected cell population, and a linker which contains an acyl unit, an optional spacer unit for providing distance between the drug moiety and the targeting moiety, a peptide linker which can be cleavable under appropriate conditions, a hydrophilic self-immolative linker, and an optional second self-immolative spacer or cyclization self-elimination linker. | 12-10-2015 |
20150352223 | CROSS-LINKERS AND THEIR USES - Charged or pro-charged cross-linking moieties and conjugates of cell binding agents and drugs comprising the charged or pro-charged cross-linking moieties and method of making the same. | 12-10-2015 |
20150352224 | ANTIBODY-DRUG CONJUGATE PRODUCED BY BINDING THROUGH LINKER HAVING HYDROPHILIC STRUCTURE - As an antitumor drug which is excellent in terms of antitumor effect and safety, there is provided an antibody-drug conjugate in which an antitumor compound represented by the following formula (I) is conjugated to an antibody via a linker having a structure represented by the following formula: -L | 12-10-2015 |
20150359903 | CONJUGATES COMPRISING CELL-BINDING AGENTS AND MAYTANSINOIDS AS CYTOTOXIC AGENTS - The invention provides linker compounds containing a disulfide group, and maytansin-derived cytotoxic compounds that are useful for forming a CBA-drug conjugates, and conjugates so formed. Such conjugates and/or cytotoxic compounds may be effective for treating a range of diseases, such as cancer, with a relatively high activity at a relatively low, non-toxic dose. | 12-17-2015 |
20150359904 | CONJUGATES COMPRISING CELL-BINDING AGENTS AND CYTOTOXIC AGENTS - The invention provides linker compounds and cytotoxic compounds that are useful for forming a CBA-drug conjugates; and conjugates so formed. Such conjugates and/or cytotoxic compounds may be effective for treating a range of diseases, such as cancer, with a relatively high activity at a relatively low, non-toxic dose. | 12-17-2015 |
20150366985 | ANTI-WALL TEICHOIC ANTIBODIES AND CONJUGATES - The invention provides anti-wall teichoic acid antibodies and antibiotic conjugates thereof, and methods of using the same. | 12-24-2015 |
20150374847 | ANTI-PMEL17 ANTIBODIES AND IMMUNOCONJUGATES - The invention provides anti-PMEL17 antibodies and immunoconjugates and methods of using the same. | 12-31-2015 |
20160015827 | ANTI-FOLATE RECEPTOR ALPHA (FRA) ANTIBODY-DRUG CONJUGATES AND METHODS OF USING THEREOF - The present disclosure provides anti-folate receptor alpha (FRA) antibody-drug conjugates comprising a hydrophilic self-immolative linker. The present disclosures further provide compositions and methods for treating cancers. | 01-21-2016 |
20160015828 | NOVEL ANTIBODY CONJUGATES AND USES THEREOF - Provided are novel antibody drug conjugates (ADCs), and methods of using such ADCs to treat proliferative disorders. | 01-21-2016 |
20160015830 | HYDROPHILIC SELF-IMMOLATIVE LINKERS AND CONJUGATES THEREOF - The present disclosure provides compounds with a hydrophilic self-immolative linker, which is cleavable under appropriate conditions and incorporates a hydrophilic group to provide better solubility of the compound. The compounds of the present disclosure comprise a drug moiety, a targeting moiety capable of targeting a selected cell population, and a linker which contains an acyl unit, an optional spacer unit for providing distance between the drug moiety and the targeting moiety, a peptide linker which can be cleavable under appropriate conditions, a hydrophilic self-immolative linker, and an optional second self-immolative spacer or cyclization self-elimination linker. | 01-21-2016 |
20160022626 | SPLICEOSTATIN ANALOGS AND METHODS FOR THEIR PREPARATION - The present invention is directed to novel cytotoxic spliceostatin analogs and derivatives, to antibody drug conjugates thereof, and to methods for using the same to treat medical conditions including cancer. | 01-28-2016 |
20160030591 | BIOLOGICALLY ACTIVE MOLECULES, CONJUGATES THEREOF, AND THERAPEUTIC USES - The present disclosure relates to linker compounds that are useful in covalently linking biologically active molecules with Ligands. The disclosed compounds also relate to biologically active molecules and Ligand conjugates, wherein the biologically active molecule is linked to the Ligand through a linker. The disclosure further provides compositions comprising biologically active molecule-ligand conjugates, methods of modifying abnormal cell growth and methods of treatment using the conjugates or the compositions. | 02-04-2016 |
20160030594 | ANTIBODY DRUG CONJUGATES - The present invention relates to anti-cKIT antibodies, antibody fragments, antibody drug conjugates, and their uses for the treatment of cancer. | 02-04-2016 |
20160031887 | PYRROLOBENZODIAZEPINES AND CONJUGATES THEREOF - A conjugate of formula (A): | 02-04-2016 |
20160038606 | CYTOTOXIC AND ANTI-MITOTIC COMPOUNDS, AND METHODS OF USING THE SAME - Compounds having cytotoxic and/or anti-mitotic activity are disclosed. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed. Also disclosed are compositions having the structure: (T)-(L)-D), wherein (T) is a targeting moiety, (L) is an optional linker, and (D) is a compound having cytotoxic and/or anti-mitotic activity. | 02-11-2016 |
20160045615 | CYCLODEXTRIN AND ANTIBODY-DRUG CONJUGATE FORMULATIONS - Disclosed are formulations, including both liquid and lyophilized formulations, comprising a benzodiazepine anti-body-drug conjugate (ADC) and a cyclodextrin. Also disclosed are methods of purifying mixtures comprising benzodiazepine anti-body-drug conjugates and process drug-related impurities. | 02-18-2016 |
20160046711 | ANTI-CDH6 ANTIBODY DRUG CONJUGATES - The present invention relates to anti-CDH6 antibodies, antibody fragments, antibody drug conjugates, and their uses for the treatment of cancer. | 02-18-2016 |
20160052880 | Novel CC-1065 Analogs and Their Conjugates - This invention relates to novel analogs of the DNA-alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor. | 02-25-2016 |
20160058882 | CYTOTOXIC AGENTS COMPRISING NEW ANSAMITOCIN DERIVATIVES - New ansamitocin derivatives bearing a linking group are disclosed. Also disclosed are methods for the synthesis of these new ansamitocin derivatives and methods for their linkage to cell-binding agents. The ansamitocin derivative-cell-binding agent conjugates are useful as therapeutic agents, which are delivered specifically to target cells and are cytotoxic. These conjugates display vastly improved therapeutic efficacy in animal tumor models compared to the previously described agents. | 03-03-2016 |
20160058884 | METHODS FOR FORMULATING ANTIBODY DRUG CONJUGATE COMPOSITIONS - The present invention provides improved methods for formulating therapeutic compositions comprising an antibody drug conjugate (“ADC”) that reduce potency variability between batches of ADC and provide administration of such therapeutic compositions within a narrow intended range. | 03-03-2016 |
20160074527 | PYRROLOBENZODIAZEPINES AND ANTIBODY DISULFIDE CONJUGATES THEREOF - A compound of formula I: | 03-17-2016 |
20160074528 | ANTHRACYCLINE DISULFIDE INTERMEDIATES, ANTIBODY-DRUG CONJUGATES AND METHODS - The invention provides antibody-drug conjugates comprising an antibody conjugated to an anthracycline drug moiety via a disulfide linker, anthracycline disulfide intermediates, and methods of using the antibody-drug conjugates. | 03-17-2016 |
20160074529 | ANTI-WALL TEICHOIC ANTIBODIES AND CONJUGATES - The invention provides anti-wall teichoic acid antibodies and antibiotic conjugates thereof, and methods of using the same. | 03-17-2016 |
20160095938 | CONJUGATES COMPRISING CELL-BINDING AGENTS AND CYTOTOXIC AGENTS - The invention relates to novel cell-binding agent-cytotoxic agent conjugates, wherein the cell-binding agent (CBA) is covalently linked to the cytotoxic agent through an aldehyde group obtained from oxidation of a 2-hydroxyethylamine moiety on the CBA. The invention also provides methods of preparing the conjugates of the present invention. The invention further provides composition and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the conjugates of the invention. | 04-07-2016 |
20160106856 | CONJUGATES INCLUDING AN ANTIBODY MOIETY, A POLYPEPTIDE THAT TRAVERSES THE BLOOD-BRAIN BARRIER, AND A CYTOTOXIN - The present invention relates to antibody-polypeptide-cytotoxin conjugates and methods of making, packaging, and using the conjugates. The polypeptide can be a Kunitz-type protease inhibitor or a derivative thereof that facilitates transport of the conjugate across the blood-brain barrier and/or into cancer cells outside the CNS, and the antibody moiety selectively binds a target within the CNS or in peripheral tumors to direct the cytotoxic agent to that target (e.g., a tumor or cancer cell). The conjugates can be further defined by the inclusion of a linker between the antibody moiety and the polypeptide; by the number of polypeptides and cytotoxic agents conjugated thereto; by the positions at which the entities within the conjugates are bound to one another; and by the larger configuration of the conjugate. Modified polypeptides (e.g., polypeptides conjugated to cytotoxic agents but not to an antibody moiety), pharmaceutical compositions, kits (e.g., including a modified polypeptide and an as-yet unconjugated antibody), and methods of making and using the conjugates are also features of the invention. | 04-21-2016 |
20160106860 | CONJUGATES OF A GLYCOPROTEIN OR A GLYCAN WITH A TOXIC PAYLOAD - The invention relates to a glycoprotein-toxic payload molecule conjugate, a toxic payload molecule-glycan conjugate, and a pharmaceutical composition. The invention further relates to a method for preparing the glycoprotein-toxic payload molecule conjugate, the method for modulating growth of a cell population and a method of treating tumour cells. | 04-21-2016 |
20160106861 | AXL ANTIBODY-DRUG CONJUGATE AND ITS USE FOR THE TREATMENT OF CANCER - The present invention relates to an antibody-drug conjugate capable of binding to the protein Axl. From one aspect, the invention relates to an antibody-drug conjugate comprising an antibody capable of binding to Axl, said antibody being conjugated to at least one drug which is a pyrrolobenzodiazepme dimer (PBD dimer) drug. The invention also comprises method of treatment and the use of said antibody-drug conjugate for the treatment of cancer. | 04-21-2016 |
20160106863 | CYTOTOXIC BENZODIAZEPINE DERIVATIVES - The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepine compounds of formula (I)-(VII). The invention also provides conjugates of the benzodiazepine compounds linked to a cell-binding agent. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention. | 04-21-2016 |
20160108129 | CYTOTOXIC BENZODIAZEPINE DERIVATIVES - The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepine compounds of formula (I)-(VII). The invention also provides conjugates of the benzodiazepine compounds linked to a cell-binding agent. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention. | 04-21-2016 |
20160114052 | POTENT CONJUGATES AND HYDROPHILIC LINKERS - Linkers for binding drugs to cell binding agents are modified to hydrophilic linkers by incorporating a polyethylene glycol spacer. The potency or the efficacy of the cell-binding agent-drug conjugates is surprisingly enhanced several folds in a variety of cancer cell types, including those expressing a low number of antigens on the cell surface or cancer cells that are resistant to treatment. A method for preparing maytansinoids bearing a thioether moiety and a reactive group which allows the maytansinoid to be linked to a cell-binding agent in essentially a single step is also provided. | 04-28-2016 |
20160129013 | TARGETED PYRROLOBENZODIAZAPINE CONJUGATES - Provided are Conjugate comprising PBDs conjugated to a targeting agent and methods of using such PBDs. | 05-12-2016 |
20160129128 | ANTIBODY DRUG CONJUGATES - Drug conjugates of formula [D-(X)b-(AA)w-(L)-]n-Ab wherein: D is a drug moiety having the following formula (I) or a pharmaceutically acceptable salt, ester, solvate, tautomer or stereoisomer thereof, wherein: A is selected from (II) and (III) R | 05-12-2016 |
20160129130 | WEEKLY DOSING REGIMENS FOR ANTI-CD30 VC-PAB-MMAE ANTIBODY DRUG-CONJUGATES - Methods for the treatment of CD30-expressing cancers are provided. The methods comprise administering to a subject in need thereof a weekly dose of from about 0.8 mg/kg to about 1.8 mg/kg of an antibody-drug conjugate compound having formula (I); or a pharmaceutically acceptable salt thereof; wherein: mAb is an anti-CD30 antibody unit, S is a sulfur atom of the antibody, A- is a Stretcher unit, and p is from about 3 to about 5. | 05-12-2016 |
20160144052 | PYRROLOBENZODIAZEPINES AND CONJUGATES THEREOF - A conjugate of formula (A): | 05-26-2016 |
20160151505 | BIO-ORTHOGONAL DRUG ACTIVATION | 06-02-2016 |
20160151513 | METHODS OF DELIVERING DLL3 ANTIBODY DRUG CONJUGATES | 06-02-2016 |
20160158379 | KITS CONTAINING DLL3 ANTIBODY DRUG CONJUGATES - Novel modulators, including antibodies and derivatives thereof, and methods of using such modulators to treat proliferative disorders are provided. | 06-09-2016 |
20160175460 | ENGINEERED ANTI-DLL3 CONJUGATES AND METHODS OF USE | 06-23-2016 |
20160185791 | DERIVATIVES OF UNCIALAMYCIN, METHODS OF SYNTHESIS AND THEIR USE AS ANTITUMOR AGENTS - In one aspect, the present disclosure provides new analogs of uncialamycin of formulae (I) and (II). The present disclosure also provides novel synthetic pathways to obtaining uncialamycin and analogs thereof. Additionally, the present disclosure also describes methods of use of uncialamycin and analogs thereof. In another aspect, the present disclosure provides antibody-drug conjugates comprising the compounds of formulae (I) and (II). | 06-30-2016 |
20160193355 | Novel linker, preparation method, and application thereof | 07-07-2016 |
20160193356 | ENGINEERED POLYPEPTIDE CONJUGATES USING TRANSGLUTAMINASE | 07-07-2016 |
20160193359 | NEW BINDER-DRUG CONJUGATES (ADCS) AND USE THEREOF | 07-07-2016 |
20160199510 | HETEROARYLENE-BRIDGED BENZODIAZEPINE DIMERS, CONJUGATES THEREOF, AND METHODS OF MAKING AND USING | 07-14-2016 |
20160200742 | BENZODIAZEPINE DIMERS, CONJUGATES THEREOF, AND METHODS OF MAKING AND USING | 07-14-2016 |
20160250342 | Hydrazinyl-Indole Compounds and Methods for Producing a Conjugate | 09-01-2016 |
20160250344 | PYRROLOBENZODIAZEPINES AND CONJUGATES THEREOF | 09-01-2016 |
20160250345 | PYRROLOBENZODIAZEPINES AND CONJUGATES THEREOF | 09-01-2016 |
20160250346 | PYRROLOBENZODIAZEPINE-ANTIBODY CONJUGATES | 09-01-2016 |
20160250348 | Anti-DLL3 antibody drug conjugates | 09-01-2016 |
20160250349 | A NOVEL STABLE FORMULATION | 09-01-2016 |
20160375147 | MAYTANSINOID DERIVATIVES, CONJUGATES THEREOF, AND METHODS OF USE - Provided herein are maytansinoid derivatives, conjugates thereof, and methods of treating or preventing proliferative diseases with the same. | 12-29-2016 |
20160375148 | Compounds and Compositions for Treating EGFR Expressing Tumors - Provided are compounds for targeted immunotherapy. The compounds are useful in the treatment of EGFR expressing tumors/cancers. Also provided are compositions comprising the compounds. | 12-29-2016 |
20160376288 | MACROCYCLIC BENZODIAZEPINE DIMERS, CONJUGATES THEREOF, PREPARATION AND USES - Macrocyclic benzodiazepine dimers having a structure represented by formula I | 12-29-2016 |
20170232108 | MATERIALS AND METHODS RELATING TO LINKERS FOR USE IN PROTEIN DRUG CONJUGATES | 08-17-2017 |
20170232113 | QUATERNARY AMINE COMPOUNDS AND ANTIBODY-DRUG CONJUGATES THEREOF | 08-17-2017 |
20190142941 | BCL-XL Inhibitory Compounds Having Low Cell Permeability and Antibody Drug Conjugates Including the Same | 05-16-2019 |
20190144546 | ANTI-CD74 ANTIBODY CONJUGATES, COMPOSITIONS COMPRISING ANTI-CD74 ANTIBODY CONJUGATES AND METHODS OF USING ANTI-CD74 ANTIBODY CONJUGATES | 05-16-2019 |
20190144558 | COMPOSITIONS AND METHODS FOR THE DEPLETION OF CD117+ CELLS | 05-16-2019 |
20190144559 | ANTI-TROP2 ANTIBODY-DRUG CONJUGATE | 05-16-2019 |
20220133711 | CAMPTOTHECIN DERIVATIVES - Disclosed herein are novel cytotoxic compounds, and cytotoxic conjugates comprising these cytotoxic compounds and cell-binding agents. More specifically, this disclosure relates to novel camptothecin derivatives thereof, intermediates thereof, conjugates thereof, and pharmaceutically acceptable salts thereof, which are useful as medicaments, in particular as anti-proliferative agents (anticancer agents). | 05-05-2022 |
20220133900 | COMPOSITIONS AND METHODS OF TREATING MUSCLE ATROPHY AND MYOTONIC DYSTROPHY - Disclosed herein are polynucleic acid molecules, pharmaceutical compositions, and methods for treating muscle atrophy or myotonic dystrophy. | 05-05-2022 |