Patent application number | Description | Published |
20090062235 | Inhibitors of Dipeptidylpeptidase IV - The present invention relates to inhibitors of post-proline cleaving enzymes, such as inhibitors of dipeptidyl peptidase IV, as well as pharmaceutical compositions thereof, and methods for using such inhibitors. In particular, the inhibitors of the present invention are improved over those in the prior art by selection of particular classes of sidechains in the P1 and/or P2 position of the inhibitor that contain a carboxylic acid moiety. The compounds of the present invention can have a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the targeted protease. | 03-05-2009 |
20090124559 | Soft Protease Inhibitors and Pro-Soft Forms Thereof - The invention provides compounds and methods for inhibiting proteases. One aspect of the invention features pro-soft inhibitors which react with an activating protease to release an active inhibitor moiety in proximity to a target protease. In certain instances, compounds inhibit proteasomes and/or post-proline cleaving enzymes (PPCE), such as dipeptidyl peptidase IV. The compounds of the invention provide a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the targeted protease. | 05-14-2009 |
20090209491 | Lactams as conformationally constrained peptidomimetic inhibitors - The present invention relates to inhibitors of post-proline cleaving enzyme, such as inhibitors of dipeptidyl peptidase IV, as well as pharmaceutical compositions thereof, and methods for using such inhibitors. In particular, the inhibitors of the present invention incorporate a lactam ring in the backbone of the inhibitors. The compounds of the present invention can have a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the target protease. | 08-20-2009 |
20090209492 | Lipase Inhibitors - The present invention relates to inhibitors of lipases, such as inhibitors of endothelial lipase, as well as pharmaceutical compositions thereof, and methods for using such inhibitors. The prototype of these inhibitors has lipophilic portion and an electrophilic site. | 08-20-2009 |
20090221818 | Inhibitors of Fibroblast Activation Protein Alpha - Disclosed are peptide-based compounds that include boronic acid or cyano functionality, which efficiently and selectively inhibit fibroblast activation protein alpha. Among other therapeutic utilities, the peptide-based compounds may be useful for the treatment of cancer. | 09-03-2009 |
20090312355 | Non-Flushing Niacin Analogues, and Methods of Use Thereof - One aspect of the present invention relates to substituted pyridines and pharmaceutically acceptable salts thereof that are active against a range of mammalian maladies. Another aspect of the invention relates to a pharmaceutical composition, comprising a compound of the present invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient. The present invention also relates to methods of treating a range of mammalian maladies or conditions, including but not limited to hyperlipidemia, hypercholesterolemia, atherosclerosis, coronary artery disease, congestive heart failure, cardiovascular disease, hypertension, coronary heart disease, angina, pellagra, Hartnup's syndrome, carcinoid syndrome, arterial occlusive disease, obesity, hypothyroidism, vasoconstriction, osteoarthritis, rheumatoid arthritis, diabetes, Alzheimer's disease, lipodystrophy, or dyslipidemia, raising serum high-density lipoprotein (HDL) levels, and lowering serum low-density lipoprotein (LDL) levels. | 12-17-2009 |
20100105629 | N-Substituted Peptidomimetic Inhibitors of Dipeptidylpeptidase IV - One aspect of the present invention relates to inhibitors of post-pro line protease enzymes, such as inhibitors of dipeptidyl peptidase IV (DPIV). Other aspects of the invention relate to pharmaceutical compositions and methods of use thereof. In certain embodiments, a DPIV inhibitor comprises a carboxylic acid-containing side chain moiety at the P1 or P2 position or both. The inhibitors of the invention should possess improved specificity for the targeted protease and low toxicity. | 04-29-2010 |
20100105753 | Inhibitors of Fibroblast Activation Protein, and Methods of Use Thereof - One aspect of the present invention relates to synthetic peptide derivatives that inhibit fibroblast activation protein α (FAP) activity. Another aspect of the invention relates to methods for treating a mammal suffering from cancer by administering a therapeutically effective amount of synthetic peptides derivatives that inhibit FAP activity. | 04-29-2010 |
20100184706 | FAP-ACTIVATED CHEMOTHERAPEUTIC COMPOUNDS, AND METHODS OF USE THEREOF - One aspect of the present invention relates to compounds for delivering chemotherapeutic agents to cancerous cells to reduce discomfort and deleterious side effects associated with systemic administration of such agents. Another aspect of the invention relates to methods of treating a subject with cancer by administering a therapeutically effective amount of a chemotherapeutic agent that predominately targets cancerous cells over healthy cells. Additionally, one aspect of the present invention relates to methods of inhibiting the life-cycle of a cancerous cell, as well preparing a chemotherapeutic prodrug. | 07-22-2010 |
20110218142 | Inhibitors of Dipeptidylpeptidase IV - The present invention relates to inhibitors of post-proline cleaving enzymes, such as inhibitors of dipeptidyl peptidase IV, as well as pharmaceutical compositions thereof, and methods for using such inhibitors. In particular, the inhibitors of the present invention are improved over those in the prior art by selection of particular classes of sidechains in the P1 and/or P2 position of the inhibitor that contain a carboxylic acid moiety. The compounds of the present invention can have a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the targeted protease. | 09-08-2011 |
20110245173 | Long-Acting GLP-1 Derivatives, and Methods of Treating Cardiac Dysfunction - The present invention generally provides polypeptide analogues of GLP-‘(9-34) and GLP-1 (9-36) that have increased in vivo half-lives resulting from reduced susceptibility to proteolytic enzymes. Other aspects of the invention relate to methods of using the polypeptide analogues described herein for treating cardiac dysfunction and other heart-related maladies. Yet another aspect of the present invention relates lo formulations comprising the polypeptide analogues described herein. | 10-06-2011 |
20120077779 | Inhibitors of Fibroblast Activation Protein Alpha - Disclosed are peptide-based compounds that include boronic acid or cyano functionality, which efficiently and selectively inhibit fibroblast activation protein alpha. Among other therapeutic utilities, the peptide-based compounds may be useful for the treatment of cancer. | 03-29-2012 |
20120077807 | NIACIN MIMETICS, AND METHODS OF USE THEREOF - Disclosed are 6-(morpholinoalkyl)-substituted pyridines, and pharmaceutically acceptable salts and prodrugs thereof, that are active against a range of mammalian therapeutic indications. | 03-29-2012 |
20120077808 | Niacin Mimetics, and Methods of Use Thereof - Disclosed are heterocyclylalkyl-substituted and heteroaralkyl-substituted pyridines, and pharmaceutically acceptable salts and prodrugs thereof, that are active against a range of mammalian therapeutic indications. | 03-29-2012 |
20120101062 | Lipase Inhibitors - The present invention relates to inhibitors of lipases, such as inhibitors of endothelial lipase, as well as pharmaceutical compositions thereof, and methods for using such inhibitors. The prototype of these inhibitors has lipophilic portion and an electrophilic site. | 04-26-2012 |
20120130044 | Stable Analogs of Peptide and Polypeptide Therapeutics - The present invention relates to compositions of peptide and polypeptide analogs that are resistant to proteolysis, pharmaceutical uses thereof, and methods of preparation thereof. | 05-24-2012 |
20120178677 | SOFT PROTEASE INHIBITORS, AND PRO-SOFT FORMS THEREOF - The invention provides compounds and methods for inhibiting proteases. One aspect of the invention features pro-soft inhibitors which react with an activating protease to release an active inhibitor moiety in proximity to a target protease. In certain instances, compounds inhibit proteasomes and/or post-proline cleaving enzymes (PPCE), such as dipeptidyl peptidase IV. The compounds of the invention provide a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the targeted protease. Another aspect of the invention provides for the use of the disclosed compounds for treating Type II diabetes, insulin resistance, glucose intolerance, hyperglycemia, hypoglycemia, hyperinsulinemia, obesity, hyperlipidemia, or hyperlipoproteinemia. | 07-12-2012 |
20130150292 | Soft Protease Inhibitors and Pro-Soft Forms Thereof - The invention provides compounds and methods for inhibiting proteases. One aspect of the invention features pro-soft inhibitors which react with an activating protease to release an active inhibitor moiety in proximity to a target protease. In certain instances, compounds inhibit proteasomes and/or post-proline cleaving enzymes (PPCE), such as dipeptidyl peptidase IV. The compounds of the invention provide a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the targeted protease. | 06-13-2013 |
20130217714 | Non-Flushing Niacin Analogues, and Methods of Use Thereof - One aspect of the present invention relates to substituted pyridines and pharmaceutically acceptable salts thereof that are active against a range of mammalian maladies. Another aspect of the invention relates to a pharmaceutical composition, comprising a compound of the present invention or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable excipient. The present invention also relates to methods of treating a range of mammalian maladies or conditions, including but not limited to hyperlipidemia, hypercholesterolemia, atherosclerosis, coronary artery disease, congestive heart failure, cardiovascular disease, hypertension, coronary heart disease, angina, pellagra, Hartnup's syndrome, carcinoid syndrome, arterial occlusive disease, obesity, hypothyroidism, vasoconstriction, osteoarthritis, rheumatoid arthritis, diabetes, Alzheimer's disease, lipodystrophy, or dyslipidemia, raising serum high-density lipoprotein (HDL) levels, and lowering serum low-density lipoprotein (LDL) levels. | 08-22-2013 |
20140018359 | Niacin Mimetics, and Methods of Use Thereof - Disclosed are 6-(morpholinoalkyl)-substituted pyridines, and pharmaceutically acceptable salts and prodrugs thereof, that are active against a range of mammalian therapeutic indications. | 01-16-2014 |
20140018545 | Inhibitors of Dipeptidylpeptidase IV - The present invention relates to inhibitors of post-proline cleaving enzymes, such as inhibitors of dipeptidyl peptidase IV, as well as pharmaceutical compositions thereof, and methods for using such inhibitors. In particular, the inhibitors of the present invention are improved over those in the prior art by selection of particular classes of sidechains in the P1 and/or P2 position of the inhibitor that contain a carboxylic acid moiety. The compounds of the present invention can have a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the targeted protease. | 01-16-2014 |
20140128344 | Soft Protease Inhibitors and Pro-Soft Forms Thereof - The invention provides compounds and methods for inhibiting proteases. One aspect of the invention features pro-soft inhibitors which react with an activating protease to release an active inhibitor moiety in proximity to a target protease. In certain instances, compounds inhibit proteasomes and/or post-proline cleaving enzymes (PPCE), such as dipeptidyl peptidase IV. The compounds of the invention provide a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the targeted protease. | 05-08-2014 |
20140255300 | FAP-Activated Proteasome Inhibitors for Treating Solid Tumors - Disclosed are proteasome inhibitors, fibroblast activation protein (FAP)-activated prodrugs of proteasome inhibitors, and pharmaceutically acceptable salts of the inhibitors and prodrugs. Also disclosed are related pharmaceutical compositions, and methods of using the inhibitors and prodrugs and compositions thereof, for example, in treating cancer or other cell proliferative diseases. In vitro and in vivo methods of quantifying the expression of FAP in a biopsy sample and a mammal, respectively, are also disclosed. | 09-11-2014 |