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 |
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 |
20090081710 | Method for Cancer Prognosis Using Cellular Folate Vitamin Receptor Quantification - The invention relates to a method for determining a prognosis for a cancer by quantifying vitamin receptor expression on the cancer cells. The method comprises the steps of quantifying vitamin receptor expression on the cancer cells, and determining a prognosis for the cancer. The invention also relates to methods and kits for determining the presence of vitamin receptors on cancer cells to select patients that should be treated with a therapy that utilizes vitamin receptor targeting and to develop a treatment regimen for such patients. The invention further relates to kits for performing the methods. | 03-26-2009 |
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 |
20100272675 | METHOD OF ADMINISTERING CONJUGATES - The invention relates to a method of treating a host animal to eliminate pathogenic cells. The method comprises the steps of administering to the host animal a hapten-carrier conjugate, administering to the host animal a TH-I biasing adjuvant, and administering to said host animal a ligand conjugated to a hapten herein the ligand-hapten conjugate is administered during the first cycle of therapy with the hapten-carrier conjugate. The invention also relates to the same method wherein the ratio of the hapten-carrier conjugate to the TH-I biasing adjuvant on a weight to weight basis ranges from about 1:10 to about 1:1. | 10-28-2010 |
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 |
20120122893 | METHODS OF TREATING CANCER - Described are methods and compositions for treating epithelial tumors with a folate-vinca conjugate in combination with at least one other chemotherapeutic agent in which the tumors include ovarian, endometrial or non-small cell lung cancer tumors, including platinum-resistant ovarian tumors and platinum-sensitive ovarian tumors. | 05-17-2012 |
20120128587 | FOLATE-TARGETED DIAGNOSTICS AND TREATMENT - Methods of detecting and assessing functionally active folate receptors on tumors and treatment associated with those tumors are described. Also described are methods of selecting ovarian and lung cancer patients for therapy with a folate-vinca conjugate by identifying functionally active folate receptors on the tumors of the patient. Also described are methods and compositions for treating folate receptor expressing epithelial tumors with a folate-vinca conjugate in combination with doxorubicin such as pegylated liposomal doxorubicin in which the tumors include ovarian, endometrial or non-small cell lung cancer tumors, including platinum-resistant ovarian tumors and platinum sensitive ovarian tumors. Also described are methods of treating platinum-resistant ovarian cancer using a folate-targeted drug, in the absence or presence of selecting the patient by identifying functionally active folate receptors on the tumors of the patient. | 05-24-2012 |
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 |
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 |
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 |
20130330326 | METHODS OF TREATING CANCER - Described are methods and compositions for treating epithelial tumors with a folate-vinca conjugate in combination with at least one other chemotherapeutic agent in which the tumors include ovarian, endometrial or non-small cell lung cancer tumors, including platinum-resistant ovarian tumors and platinum-sensitive ovarian tumors. | 12-12-2013 |
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 |