Patent application number | Description | Published |
20080207625 | Synthesis and Purification of Pteroic Acid and Conjugates Thereof - Methods for purifying pteroic acid, analogs of pteroic acid, and derivatives of pteroic acid are described. Methods for synthesizing and purifying conjugates of vitamins, including FITC conjugates of folic acid, folic acid analogs, and derivatives of folic acid and folic acid analogs are also described. Purified forms of pteroic acid, derivatives and analogs of pteroic acid, and conjugates thereof are also described. | 08-28-2008 |
20080248052 | Multi-Drug Ligand Conjugates - Described herein are compounds, pharmaceutical compositions and methods for treating pathogenic cell populations in a patient. The compounds described herein include conjugates of a plurality of cytotoxic drugs and vitamin receptor binding ligands. The plurality of drugs may be the same or different. Similarly, the vitamin receptor binding ligands may be the same or different. The conjugates also include a linker that is formed from one or more spacer linkers, heteroatom linkers, and releasable linkers. | 10-09-2008 |
20080280937 | Ligand Conjugates of Vinca Alkaloids, Analogs, and Derivatives - Described herein are compounds, pharmaceutical compositions and methods for treating pathogenic cell populations in a patient. The compounds described herein include conjugates of cytotoxic drugs and vitamin receptor binding ligands. The conjugates also include a linker that is formed from one or more spacer linkers, heteroatom linkers, and releasable linkers. | 11-13-2008 |
20090203889 | Bivalent linkers and conjugates thereof - Bivalent linkers derived from compounds of formulae (V), (VI), and (VII), where X | 08-13-2009 |
20100048490 | BINDING LIGAND LINKED DRUG DELIVERY CONJUGATES OF TUBULYSINS - Described herein are compounds, pharmaceutical compositions and methods for treating pathogenic cell populations. The compounds described herein include conjugates of tubulysins and vitamin receptor binding ligands. The conjugates also include a releasable bivalent linker. | 02-25-2010 |
20100104626 | METHODS AND COMPOSITIONS FOR TREATING AND DIAGNOSING KIDNEY DISEASE - The invention relates to a method for diagnosing a kidney disease state. The method comprises the steps of administering to a patient a composition comprising a conjugate or complex of the general formula V-L-D where the group V comprises a vitamin receptor binding ligand that binds to kidney proximal tubule cells and the group D comprises a diagnostic marker, and diagnosing the kidney disease state. The invention also relates to a method for treating a kidney disease state. The method comprises the steps of administering to a patient suffering from the disease state an effective amount of a composition comprising a conjugate or complex of the general formula V-L-D where the group V comprises a vitamin receptor binding ligand that binds to kidney proximal tubule cells and the group D comprises an antigen, a cytotoxin, or a cell growth inhibitor, and eliminating the disease state. | 04-29-2010 |
20100240701 | TUBULYSINS AND PROCESSES FOR PREPARING - Processes are described for the preparation of tubulysins. The processes are useful for preparing predetermined mixtures of tubulysins, preparing single tubulysins from mixtures of tubulysins, and for converting one tubulysin into a different tubulysin. The tubulysins described herein are useful in treating diseases and disease states that include pathogenic cell populations. | 09-23-2010 |
20100323973 | CONJUGATES CONTAINING HYDROPHILIC SPACER LINKERS - Described herein are compositions and methods for use in targeted drug delivery using cell receptor binding drug delivery conjugates containing hydrophilic spacer linkers for use in imaging, diagnosing, and/or treating diseases and disease states caused by pathogenic cell populations. | 12-23-2010 |
20110172254 | FOLATE RECEPTOR BINDING CONJUGATES OF ANTIFOLATES - Conjugates of antifolates, releasable linkers, and drugs, and pharmaceutical compositions containing them are described. The conjugates are useful for treating diseases arising from pathogenic cell populations. Methods for treating such diseases are also described. | 07-14-2011 |
20120022245 | FOLATE TARGETING OF NUCLEOTIDES - The present invention relates to compounds, compositions, kits, and methods of use in targeting nucleotides, such as siRNA's, to cancer cells or to immune system cells involved in inflammation. More particularly, the invention is directed to receptor binding ligand-nucleotide delivery conjugates for use in specifically targeting the conjugates to cancer cells or to immune system cells, methods of treatment with these conjugates, methods of preparation of these conjugates, and methods of reducing the expression of a gene in vitro or in vivo with the conjugates described herein. | 01-26-2012 |
20120258905 | VITAMIN RECEPTOR DRUG DELIVERY CONJUGATES FOR TREATING INFLAMMATION - Described herein are compositions, methods, compounds, conjugates, and kits for use in targeted drug delivery using drug delivery conjugates containing hydrophilic spacer linkers for use in treating disease states caused by pathogenic cell populations, such as inflammatory cells. | 10-11-2012 |
20120270791 | Methods and Compositions for Treating and Diagnosing Kidney Disease - The invention relates to a method for diagnosing a kidney disease state. The method comprises the steps of administering to a patient a composition comprising a conjugate or complex of the general formula V-L-D where the group V comprises a vitamin receptor binding ligand that binds to kidney proximal tubule cells and the group D comprises a diagnostic marker, and diagnosing the kidney disease state. The invention also relates to a method for treating a kidney disease state. The method comprises the steps of administering to a patient suffering from the disease state an effective amount of a composition comprising a conjugate or complex of the general formula V-L-D where the group V comprises a vitamin receptor binding ligand that binds to kidney proximal tubule cells and the group D comprises an antigen, a cytotoxin, or a cell growth inhibitor, and eliminating the disease state. | 10-25-2012 |
20130065841 | PROCESS FOR A FOLATE-TARGETED AGENT - The invention described herein pertains to an improved process for preparing the folate-targeted conjugate EC 145 and to the conjugate EC 145 prepared using the improved process, as well as to a pharmaceutical composition comprising the conjugate EC 145 prepared using the improved process. | 03-14-2013 |
20130116195 | Binding ligand linked drug delivery conjugates of tubulysins - Described herein are compounds, pharmaceutical compositions, and methods for treating pathogenic cell populations. Kits including the compounds or pharmaceutical compositions are described. The compounds described herein include conjugates of tubulysins and folates. The conjugates also include a releasable bivalent linker. | 05-09-2013 |
20130137139 | PROCESSES FOR PREPARING TUBULYSINS - Tubulysins are a series of naturally occurring cytotoxic agents that are of interest as anticancer therapeutic agents. Processes and intermediates useful for preparing naturally occurring and non-naturally occurring tubulysins and analogs and derivatives thereof are described. | 05-30-2013 |
20130158271 | BIVALENT LINKERS AND CONJUGATES THEREOF - Bivalent linkers to be included in or for preparing vitamin, drug, diagnostic agent, and/or imaging agent conjugates are described. | 06-20-2013 |
20130203680 | FOLATE CONJUGATES FOR TREATING INFLAMMATION OF THE EYE - The present invention relates to methods of use of folate conjugates for treating inflammatory diseases of the eye, to folate conjugates for use in treating inflammatory diseases of the eye, and to folate conjugates for use in the manufacture of a medicament for treating inflammatory diseases of the eye. More particularly, the invention is directed to the use of folate linked to one or more anti-inflammatory agents for each of the above-described uses. | 08-08-2013 |
20140213760 | Folate Receptor Binding Conjugates of Antifolates - Conjugates of antifolates, releasable linkers, and drugs, and pharmaceutical compositions containing them are described. The conjugates are useful for treating diseases arising from pathogenic cell populations. Methods for treating such diseases are also described. | 07-31-2014 |
20150051399 | PROCESSES FOR PREPARING TUBULYSIN DERIVATIVES AND CONJUGATES THEREOF - The invention described herein pertains to processes for preparing tubulysin derivatives, conjugates of tubulysins, and intermediates therefore. In one illustrative embodiment of the invention, processes for derivatives or analogs of natural tubulysins including compounds of formula (T). In another embodiment, vitamin receptor binding conjugates of tubulysins are described. The processes include one or more steps described herein. In another embodiment, a process is described for preparing a compound of formula B, wherein R5 and R6 are as described in the various embodiments herein, such as each being independently selected from optionally substituted alkyl or optionally substituted cycloalkyl; and R8 is C1-C6 n-alkyl; wherein the process comprises the step of treating a compound of formula A with a silylating agent, such as triethylsilyl chloride, and a base, such as imidazole in an aprotic solvent. | 02-19-2015 |