Class / Patent application number | Description | Number of patent applications / Date published |
514210030 | Polycyclo ring system having the four-membered hetero ring as one of the cyclos | 53 |
20110166118 | NEW TRINEM ANTIBIOTICS AND INHIBITORS OF BETA-LACTAMASES - The present invention relates to a compound of Formula (I) in particular compounds of formula (Ia), the use of a therapeutically effective amount of one or more compounds of formula (I) or (Ia) as a broad-spectrum antibiotic and the use of a pharmaceutical composition comprising said compounds for the treatment of bacterial infections in humans or animals. | 07-07-2011 |
514210040 | Bicyclo ring system having the four-membered hetero ring as one of the cyclos | 52 |
20090082326 | SOLUBLE DOSAGE FORMS CONTAINING CEPHEM DERIVATIVES SUITABLE FOR PARENTERAL ADMINISTRATION - The present invention relates to new dosage forms of cephem compounds, useful for the treatment of bacterial infections. The dosage forms are stable, exhibit enhanced solubility, and are particularly well suited for, e.g., parenteral administration. | 03-26-2009 |
20100016276 | COMPOSITIONS AND METHODS FOR THE IDENTIFICATION OF A CARBAPENEMASE GENE - Compositions and methods for the rapid and sensitive detection of a carbapenemase in a sample is provided. The compositions include novel primer and probe compositions for use in detecting the presence of this enzyme in a sample, particularly using PCR methods. These primers and probe sets can be used in amplification methods (such as PCR, particularly quantitative PCR) and packaged into kits for use in amplification methods for the purpose of detecting carbapenemase in a test sample, particularly a patient sample, particularly a direct sample. Thus, in one embodiment, the present invention provides for novel oligonucleotide primers set forth in SEQ ID NOs:1, 2, 4, 5, 7, 8, 14, 15, 17, 18, and 20, and the novel oligonucleotide probe sequences set forth in SEQ ID NOs:3, 6, 9, 16, and 19. These sequences can be used in a method of detecting carbapenemase in a sample. | 01-21-2010 |
20100267686 | CARBACEPHEM BETA-LACTAM ANTIBIOTICS - Carbacephem β-lactam antibiotics having the following chemical structures (I) and (II) are disclosed: | 10-21-2010 |
20110082129 | ORGANIC COMPOUNDS - The present invention provides novel organic compounds of Formula I: methods of use, and pharmaceutical compositions thereof. | 04-07-2011 |
20110224186 | CARBACEPHEM BETA-LACTAM ANTIBIOTICS - Carbacephem β-lactam antibiotics having the following chemical structure (I) are disclosed: | 09-15-2011 |
514210050 | Plural ring hetero atoms in the bicyclo ring system | 22 |
20090042853 | PENEM PRODRUGS - Orally bioavailable prodrugs of sulopenem, e.g., | 02-12-2009 |
20090275552 | Therapy for Treating Resistant Bacterial Infections - The invention relates to an improved therapy for treating resistant bacterial infections caused by extended-spectrum β-lactamase (ESBLs)-producing strains in a warm-blooded animal, adjuvant step down therapy, and pharmaceutical compositions for such therapies. The invention also relates to a method for inhibiting bacterial resistance in ESBLs-producing strains so as to have better control over the therapy; achieve reduced hospital stay and adjuvant step down therapy so as to avoid recrudescence. In particular, the therapy includes antibacterial combination of cefepime with sulbactam via parenteral route, followed by oral third generation cephalosporin with a suitable β lactamase inhibitor. | 11-05-2009 |
20100009957 | NOVEL INHIBITORS OF BETA-LACTAMASE - A class of 7-oxo-2,6-diazabicyclo-[3.2.0]-heptane-6-sulfonic acid compounds substituted at the two position of the bicyclic ring with a heterocyclylaminocarbonyl group or a carbocyclylaminocarbonyl group are β-lactamase inhibitors. The compounds and their prodrugs and pharmaceutically acceptable salts are useful in the treatment of bacterial infections in combination with β-lactam antibiotics. In particular, the compounds are suitable for use with β-lactam antibiotics (e.g., imipenem and ceftazidime) against micro-organisms resistant to β-lactam antibiotics due to the presence of the β-lactamases. | 01-14-2010 |
20100022504 | METHODS FOR TREATING LATENT TUBERCULOSIS - A method for treating individuals affected with latent tuberculosis comprising a step of administering an effective amount of one or more carbapenem compounds to the said individuals. | 01-28-2010 |
20100125060 | FORMULATIONS COMPRISING CEFTIOFUR AND KETOPROFEN OR CEFTIOFUR AND BENZYL ALCOHOL - The present invention relates to veterinary or pharmaceutical formulations which may comprise ceftiofur, ketoprofen, benzyl alcohol, or effective combinations thereof. The formulations of the present invention may include a wetting or dispersing agent, a preservative, a flocculating agent or resuspendability enhancer, and/or a biocompatible oil vehicle. This invention also provides for, inter alia, formulations for the treating, controlling and preventing of respiratory disorders, particularly bovine respiratory disease (BRD), in warm-blooded animals, such as livestock,. This invention further provides for methods of increasing the resuspendability of an oily formulation which may comprise the addition. | 05-20-2010 |
20100261700 | BETA-LACTAMASE INHIBITORS - Broad spectrum beta-lactamase inhibitors. Certain inhibitors also exhibit potent antibiotic activity in addition to beta-lactamase inhibition. Compounds of the invention are designed such that on cleavage of the beta-lactam ring reactive moieties are generated which can inactivate beta-lactamase. Also provided are methods of making beta-lactamase inhibitors and beta-lactam antibiotics exhibiting such inhibition. Additionally provided are pharmaceutical compositions for treatment or prevention of bacterial infections and methods of treatment of such infections. | 10-14-2010 |
20110224187 | PYRROLIDINE, PIPERIDINE AND PIPERAZINE DERIVATIVES AND METHODS OF USE THEREOF - The present invention relates to novel Pyrrolidine, Piperidine and Piperazine Derivatives, pharmaceutical compositions comprising the Pyrrolidine, Piperidine and Piperazine Derivatives and the use of these compounds for treating or preventing treating allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a metabolic disorder, obesity, an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. | 09-15-2011 |
20140094447 | Pharmaceutical compositions comprising sulbactam and beta-lactamase inhibitor - Pharmaceutical compositions and methods for treating or preventing bacterial infections are disclosed. The pharmaceutical compositions typically comprise pharmaceutically effective amount of: (a) sulbactam or a pharmaceutically acceptable salt thereof, and (b) at least one beta-lactamase inhibitor or a pharmaceutically acceptable salt thereof, with the provision that the beta-lactamase inhibitor is not sulbactam. | 04-03-2014 |
20140148431 | 1,6- Diazabicyclo [3,2,1] octan-7-one derivatives and their use in the treatment of bacterial infections - Compounds of Formula (I), their preparation and use in preventing or treating bacterial infection is disclosed. | 05-29-2014 |
20140378430 | Heterocyclic Compounds and Methods of Their Use - The present invention relates to heterocyclic compounds useful for antagonising angiotensin II Type 2 (AT | 12-25-2014 |
20150031662 | USEFUL COMBINATIONS OF MONOBACTAM ANTIBIOTICS WITH BETA-LACTAMASE INHIBITORS - A pharmaceutical composition, comprising a combination of an antibiotically active compound of the formula (I): with a β-lactamase inhibitor of one of the formulae (II) to (XIII) are active against Gram-negative bacteria, in particular such bacteria which have become resistant against antibiotics such as aztreonam, carumonam and tigemonam. Optionally the compositions may comprise another β-lactamase inhibitor of one of the formulae (II) to (XIII), particularly of formula (V) or formula (VI). | 01-29-2015 |
20150031663 | PHTHALANILATE COMPOUNDS AND METHODS OF USE - The invention provides antimicrobial compounds and compositions, and methods of using them. The compounds and compositions include, for example, a compound of any one of Formulas I-X. The invention further provides methods of preparing the compounds, and useful intermediates for their preparation. The compounds can possess highly specific and selective activity, such as antibacterial activity and/or enzymatic inhibitory activity. Accordingly, the compounds and compositions can be used to treat bacterial infections, or to inhibit or kill bacteria, either in vitro or in vivo. | 01-29-2015 |
20150322087 | CEPHALOSPORIN DERIVATIVES AND METHODS OF USE - This invention provides cephalosporin derivatives for killing or inhibiting the spread of microorganisms such as non-replicating | 11-12-2015 |
20160045480 | Compositions and methods for treating bacterial infections - Pharmaceutical compositions and methods for treating bacterial infections are disclosed. | 02-18-2016 |
20220133699 | Antibacterial Compositions - Provided herein are methods of treating subjects having a bacterial infection by administering a peptide multimer and a carbapenem antibiotic. Also provided herein are methods of eliminating or inhibiting bacteria with a peptide multimer and a carbapenem antibiotic. Also provided herein are antibacterial compositions that include a peptide multimer and a carbapenem antibiotic. | 05-05-2022 |
514210060 | Ring oxygen in the bicyclo ring system | 7 |
20080318921 | Tricyclic 6-Alkylidene-Penems as Beta-Lactamase Inhibitors - The present invention provides a compound of formula I, pharmaceutical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof. | 12-25-2008 |
20090270358 | PHARMACEUTICAL FORMULATION OF CLAVULANIC ACID - The present invention generally relates to stable pharmaceutical compositions, and methods of making and administering such compositions. In one aspect, the invention features stabilized pharmaceutical compositions that include pharmaceutically active ingredients such as potassium clavulanate or Clavitesse™, preferably in an immediate-release solid dosage form or an extended-release solid dosage form. Also provided are methods for making and using such immediate-release and stabilized compositions or extended-release and stabilized compositions. | 10-29-2009 |
20120252775 | METHOD FOR DIAGNOSING, PREVENTING, AND TREATING NEUROLOGICAL DISEASES - The invention provides for methods of treating autism associated with | 10-04-2012 |
514210070 | The other cyclo of the bicyclo ring system is six-membered | 4 |
20080287412 | THERAPEUTIC COMBINATION OF AMLODIPINE AND BENAZEPRIL/BENAZEPRILAT - The present invention especially relates to the use of a combination comprising | 11-20-2008 |
514210080 | 1-oxa-5-aza-bicyclo (4.2.0) octanes (including unsaturated) | 3 |
20080200447 | Neurotherapeutic Compositions and Method - Administration of β-Lactam compounds, including β-lactam antibiotics and β-lactamase inhibitors provides significant neurotropic effects in warm-blooded vertebrates evidence inter alia by anxiolytic and anti-aggressive behavior modification and enhanced cognition. Therapeutic methods for using such compounds and their pharmaceutical formulations are described. | 08-21-2008 |
20100249090 | NEUROTHERAPEUTIC COMPOSITION AND METHOD THEREFOR - Neurotherapeutically effective pharmaceutical compositions are described that include carboxypeptidase E inhibitors. One class of carboxypeptidase E inhibitors found to exhibit significant neurotropic activity are β-lactam compounds, particularly penam and cephem β-lactam antibiotics and non-antibiotic derivatives thereof. | 09-30-2010 |
20130102583 | CEPHEM COMPOUND HAVING CATECHOL GROUP - A compound of the formula: | 04-25-2013 |
514210090 | The other cyclo of the bicyclo ring system is five-membered | 25 |
20090029964 | Novel carbapenem compound - An orally administrable antibacterial agent which contains as an active ingredient a carbapenem compound represented by the formula [1] below, | 01-29-2009 |
20090286764 | STABLE PHARMACEUTICAL FORMULATIONS - Stable pharmaceutical formulations and methods of making same are provided. In a general embodiment, the present disclosure provides a method of making a stable pharmaceutical formulation comprising adding one or more vitrifying additives to an aqueous pharmaceutical solution to raise the glass transition temperature of the aqueous pharmaceutical solution. The aqueous pharmaceutical solution can be cooled to a temperature of about −50° C. to about −10° C. The vitrifying additive enhances the formation of a glass or amorphous solid of the aqueous pharmaceutical solution at cryogenic temperatures (−50 to −10° C.), and the pharmaceutical formulation can be thawed to liquid form and administered to a mammalian subject. | 11-19-2009 |
20100063023 | Bicyclic and Tricyclic Substituted 6-Methylidene Carbapenems as Broad Spectrum Beta-Lactamase Inhibitors - Provided is a β-lactamase antibiotic and a compound of formula I, a process of producing the compound, pharmaceutical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof. | 03-11-2010 |
20100075945 | GRAM-POSITIVE CARBAPENEM ANTIBACTERIALS AND PROCESSES FOR THEIR PREPARATION - The present invention provides β-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment. The present invention is also in the field of synthetic organic chemistry and is specifically provides an improved method of synthesis of β-methyl carbapenems which are useful as antibacterial agents. | 03-25-2010 |
20100160284 | CARBAPENEM ANTIBACTERIALS WITH GRAM-NEGATIVE ACTIVITY AND PROCESSES FOR THEIR PREPARATION - The present invention provides β-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment. The present invention is also in the field of synthetic organic chemistry and is specifically provides an improved method of synthesis of β-methyl carbapenems which are useful as antibacterial agents. | 06-24-2010 |
20110251169 | Arylethynyl derivatives - The present invention relates to ethynyl compounds of formula I | 10-13-2011 |
20130172313 | Carbapenem Antibacterials with Gram-Negative Activity - The present invention provides β-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment. | 07-04-2013 |
20130178456 | ARYLETHYNYL DERIVATIVES - The present invention relates to ethynyl compounds of formula I | 07-11-2013 |
20140057889 | BCL-2-SELECTIVE APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE DISEASES - Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein. | 02-27-2014 |
20140057890 | BCL-2-SELECTIVE APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE DISEASES - Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein. | 02-27-2014 |
20150045340 | AMIDINE SUBSTITUTED BETA-LACTAM COMPOUNDS, THEIR PREPARATION AND USE AS ANTIBACTERIAL AGENTS - The present invention relates to novel β-lactam compounds, their preparation and use. In particular, this invention relates to novel β-lactam compounds which are amidine substituted monobactam derivatives useful as antimicrobial agents and their preparation. | 02-12-2015 |
20150306071 | Carbapenem Antibacterials with Gram-Negative Activity - The present invention provides β-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment. | 10-29-2015 |
20160251356 | FLUORESCENT CARBAPENEMS | 09-01-2016 |
514210100 | Sulfur bonded directly to the five-membered cyclo of the bicyclo ring system (e.g., thienamycin, etc.) | 12 |
20100292169 | METHODS AND COMPOSITIONS FOR REGULATING HDAC6 ACTIVITY - The present invention provides methods and compositions for inhibiting Hsp90 activity in a cell, comprising contacting the cell with an inhibitor of histone deacetylase 6 (HDAC6) | 11-18-2010 |
20100298237 | USE OF HDAC INHIBITORS FOR TREATMENT OF CARDIAC RHYTHM DISORDERS - The present invention provides methods of ameliorating or reducing the extent of cardiac arrhythmia disorders, by administering an inhibitor of histone deacetylase enzyme (HDAC). | 11-25-2010 |
20110009341 | N-Alkylated Cyclic Peptide Melanocortin Agonists - A melanocortin-4 receptor agonist cyclic peptide of the formula | 01-13-2011 |
20110015137 | RECA INHIBITORS AND THEIR USES AS MICROBIAL INHIBITORS OR POTENTIATORS OF ANTIBIOTIC ACTIVITY - The present invention provides RecA inhibitors, compositions containing them, systems for identifying or characterizing them, and methods of using them. | 01-20-2011 |
20110046072 | SOLID PHARMACEUTICAL FORMULATION WITH DELAYED RELEASE - The invention relates to a solid pharmaceutical preparation with delayed release of the active ingredients which is suitable in particular for use in animals. | 02-24-2011 |
20110059903 | Formulations Comprising Linaclotide - The present invention relates to stable compositions comprising linaclotide, as well as to various methods and processes for the preparation and use of the compositions. | 03-10-2011 |
20110059904 | SERUM-BASED, DIAGNOSTIC, BIOLOGICAL ASSAY TO PREDICT PREGNANCY DISORDERS - The invention provides serum-based, diagnostic, biological assays for predicting disorders of pregnancy resulting from poor trophoblast and/or placental ischemia, including preeclampsia. Serum samples from such subjects exhibit an ability to disrupt the architecture involving fetal trophoblasts and maternal endothelial cells in a three-dimensional, dual cell co-culture system provided herein, in contrast to normal pregnancy serum samples. Based on these distinctions, the assays are employed to predict pregnancy outcomes as early as first trimester. | 03-10-2011 |
20110092445 | Amyloid peptide analogues, oligomers thereof, processes for preparing and composi-tions comprising said analogues or oligomers, and their uses - The present invention relates to an amyloid β peptide analogues comprising an amino acid sequence or a peptidomimetic thereof, wherein the sequence (i) forms a loop, (ii) has at least 66% identity to the amino acid sequence of native Aβ peptide or a portion thereof, (iii) comprises at least 6 contiguous amino acid residues and (iv) has at least 2 non-contiguous amino acid residues which are covalently linked with each other, oligomers comprising a plurality of said amyloid β peptide analogues, processes for preparing the amyloid β peptide analogues or oligomers, compositions comprising the amyloid β peptide analogues or oligomers, and uses of the amyloid β peptide analogues or oligomers such as their use for treating or preventing an amyloidosis (e.g. by active immunization), for diagnosing an amyloidosis, and for providing agents that are capable of binding to the amyloid β peptide analogues or oligomers. The subject invention also describes agents that are capable of binding to the amyloid β peptide analogues or oligomers, e.g. antibodies, compositions comprising the agents, and uses of the agents such as their use for treating or preventing an amyloidosis (e.g. by passive immunization) and for diagnosing an amyloidosis. | 04-21-2011 |
20110092446 | COMPOSITIONS AND METHODS FOR TREATMENT OF TRAUMA - The present invention features the use of a complement inhibitor, e.g., a compstatin analog for treating an individual who has suffered a severe injury. In some embodiments, the complement inhibitor may be administered within 24 hours following the injury and optionally also at later time points. The complement inhibitor may, for example, be administered prior to transporting the patient to a health care facility, during transport of the patient to a health care facility, or in the emergency department. Further provided are methods of selecting individuals for such therapy. Further provided are methods of identifying individuals at increased risk of poor outcome following trauma. In certain embodiments the methods comprise determining whether the genotype of the patient includes an allele of a polymorphism in or near a complement-related gene, wherein said allele is associated with risk of poor outcome following trauma. | 04-21-2011 |
20110092447 | USING INHIBITORS OF HISTONE DEACETYLASES FOR THE SUPPRESSION THERAPY OF INHERITED DISEASE PREDISPOSING CONDITIONS - Compounds can be used to act as inhibitors of enzymes having histone deacetylase activity for the medical therapy of conditions which predispose a person for the development of a disease, such as but not limited to cancer, inflammatory or metabolic diseases. Such conditions are linked to genetically inherited mutations of crucial genes which predispose a person with this condition to develop the disease phenotype. Thus, such compounds can be used for a suppressive therapeutic approach—the SUPPRESSION THERAPY—in order to inhibit or delay the onset or progression of the genetically predisposed disorder. Furthermore, a clinically used medicament can be manufactured for the SUPPRESSION THERAPY of such inherited predisposing conditions. | 04-21-2011 |
20110105414 | CYCLIC, CYSTEIN-FREE PROTEIN - A protein selected from the amino acid sequence of the region valine Val(91) to glycine Gly(l21) of the mature human tumour necrosis factor, or a portion thereof, with the proviso that the protein comprises at least the amino acid sequence of the region lysine Lys(98) to glutamic acid Glu(116), with the cysteine Cys(101) being replaced by a glycine and an amide bond being formed between the amino group of the side chain of the lysine Lys(98) and the carboxyl group of the side chain of the glutamic acid Glu(116), which activates epithelial ion channels and improves the lung function and which can be used for the manufacture of medicaments for the treatment of diseases associated with the lung function, such as oedemas. | 05-05-2011 |
20110124578 | AMINO ACID INHIBITORS OF CYTOCHROME P450 - Methods of inhibiting cytochrome P450 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450. Pharmaceutical compositions are provided that eases can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 enzymes. | 05-26-2011 |
20110124579 | SIALIC ACID TO SUPPORT SALIVATION - The present invention generally relates to the field of disorders related to an impaired salivation and compositions that can be used to treat or prevent such disorders. One embodiment of the present invention relates to a composition comprising sialic acid to treat and/or prevent disorders linked to an impaired salivation. | 05-26-2011 |
20110172167 | FORMULATIONS OF DAPTOMYCIN - Long term storage stable daptomycin-containing compositions are disclosed. The compositions include daptomycin or a pharmaceutically acceptable salt thereof at a concentration of less than or equal to about 25 mg/mL, a buffer having an acidic functional group and have a pH of from about 6.0 to about 7. The formulations are surprisingly free of degradation products such as the hydrolysis product of daptomycin and the β-isomer of daptomycin after storage periods of at least about 18 months. | 07-14-2011 |
20110195914 | MACROCYCLIC ANTIPROLIFERATION AGENTS AND METHODS OF TREATMENT - The instant invention describes macrocyclic compounds having antiproliferation activity, and methods of treating disorders such as cancer, tumors and cell proliferation related disorders. | 08-11-2011 |
20110195915 | Method of inhibiting prostate cancer cell proliferation - The present invention relates to a method of inhibiting or reducing the proliferation of prostate cancer cells, such as androgen independent prostate cancer (AIPC) cells, the method comprising administering to the cells a PLA | 08-11-2011 |
20110230426 | TEMPLATE-FIXED PEPTIDOMIMETICS - Template-fixed β-hairpin peptidomimetics of the general formula | 09-22-2011 |
20110251138 | LIPOIC ACID METABOLITE CONJUGATE: PREPARATION AND THEIR THERAPEUTIC EFFECT - The present invention is a design and synthesis of a series of therapeutic conjugates which consists of tautomers of lipoic acid metabolites, with small molecule, vitamin, carbohydrates, peptides, chemotherapeutic agent wherein or not the conjugate possesses dual binding ability. The present invention can be used to therapeutics and diagnostics in vitro for cancer and other diseases associated with altered metabolic enzymes. The invention can also be used for the controlled release of more stable form of lipoic acid in its salt form with the minerals or vitamins. | 10-13-2011 |
20110294746 | PHARMACEUTICAL MICROEMULSION FOR PREVENTING SUPRAMOLECULAR AGGREGATION OF AMPHIPHILIC MOLECULES - The present invention refers to a microemulsion formulation suitable for preventing assembly of amphiphilic drug molecules which may cause hypersensitivity reactions and other unwanted side effects. | 12-01-2011 |
20110301098 | TREATMENT FOR INTIMAL HYPERPLASIA AND RELATED CONDITIONS - The present invention provides a method of prevention or treatment of intimal hyperplasia in blood vessel walls, the method comprising the step of administering a therapeutically effective amount of an inhibitor of C5a function to a mammal. | 12-08-2011 |
20110301099 | Method for enhancing penetration of lipid insoluble medicaments through cell membranes using small S-Allyl-containing molecules with phospholipid permeability as carrier molecules - A method and composition that allows for the penetration of lipid insoluble medicaments through cell membranes using small S-Allyl-containing molecules with phospholipid permeable molecules as carrier molecules. S-Allyl-containing compounds can include alliin, allicin, | 12-08-2011 |
20110301100 | Pharmaceutical Compositions Comprising Polyethylene Glycol Having a Molecular Weight of Less Than 600 Daltons - A liquid pharmaceutical composition comprising a biodegradable polymer, polyethylene glycol having a molecular weight of less than 600 Daltons, a pharmaceutically active agent and less than 0.5% of an biologically acceptable organic solvent. | 12-08-2011 |
20110306565 | HYALURONIC ACID CONTAINING COMPOSITIONS FOR TREATMENT OF WOUNDS, SCARS, POST-SURGICAL ADHESION FORMATION - Pharmaceutical compositions are provided for enhancing the therapeutic effect of biologically active peptides, especially peptides derived from human lactoferrin. The compositions are useful for the treatment and/or prevention of wounds, scars, and post surgical adhesions. | 12-15-2011 |
20110319343 | Agonists Of Guanylate Cyclase Useful For The Treatment Of Gastrointestinal Disorders, Inflammation, Cancer And Other Disorders - The invention provides novel guanylate cyclase-C agonist peptides and their use in the treatment of human diseases including gastrointestinal disorders, inflammation or cancer (e.g., a gastrointestinal cancer). The peptides can be administered either alone or in combination with an inhibitor of cGMP-dependent phosphodiesterase. The gastrointestinal disorder may be classified as either irritable bowel syndrome, constipation, or excessive acidity etc. The gastrointestinal disease may be classified as either inflammatory bowel disease or other GI condition including Crohn's disease and ulcerative colitis, and cancer. | 12-29-2011 |
20120022004 | TREATMENT OF T-CELL MEDIATED DISEASES - The invention provides a method of treating T-cell mediated diseases and a method of inhibiting the activation of T-cells using certain diketopiperazines. The invention also provides methods of synthesizing diketopiperazines and pharmaceutical compositions comprising certain diketopiperazines. The invention further provides methods of making improved pharmaceutical compositions of proteins and peptides by either increasing or decreasing the content of diketopiperazines in the compositions and the resultant improved pharmaceutical compositions. | 01-26-2012 |
20120035116 | BILE ACIDS AND BIGUANIDES AS PROTEASE INHIBITORS FOR PRESERVING THE INTEGRITY OF PEPTIDES IN THE GUT - This invention relates to methods of preserving the integrity of peptides in the gut. In particular it concerns the use of certain compounds as inhibitors of gut proteases. Compounds identified as having gut protease inhibitory activity are biguanides, certain bile acids and pharmaceutically acceptable salts of these compounds. This activity makes these compounds useful for co-administration with prophylactic or therapeutic peptides. This invention relates to methods of inhibiting gut proteases and peptide formulations comprising these gut protease inhibitor. | 02-09-2012 |
20120040916 | MOLECULAR INHIBITORS OF THE WNT/BETA-CATENIN PATHWAY - The present invention is directed toward a method of treating a subject for a condition mediated by the Wnt/β-catenin pathway by selecting a subject with a condition mediated by the Wnt/β-catenin pathway and administering to the selected subject a compound selected from the group consisting of those set forth in Table 1, Table 2, and a pharmaceutically acceptable salt thereof. A method of similarly inhibiting the Wnt/β-catenin pathway in a subject is also disclosed. | 02-16-2012 |
20120101047 | PEPTIDOMIMETIC MACROCYCLES - The present invention provides novel peptidomimetic macrocycles and methods of using such macrocycles for the treatment of disease. | 04-26-2012 |
20120115796 | Novel Spacer Moiety for Poly(ehtylene Glycol) Modified Peptide Based Compounds - The present invention relates to a compound comprising a peptide moiety, a spacer moiety and a water-soluble polymer moiety such as a poly(ethylene glycol) moiety. The spacer moiety is between the peptide moiety and the water-soluble polymer moiety. The spacer moiety has the structure: | 05-10-2012 |
20120135942 | BETA-HAIRPIN PEPTIDOMIMETICS - β-Hairpin peptidomimetics of the general formula Cyclo(-Xaa | 05-31-2012 |
20120157392 | Epilepsy treatment employing ketogenic compounds which arrest apoptosis - Method of treating a patient suffering from apoptosis of tissue by administering to the patient a therapeutically effective amount of one or more ketogenic compounds such that a physiological ketosis is produced which arrests the apoptosis. | 06-21-2012 |
20120214748 | NOVEL PEPTIDES, PROCESS FOR PREPARATION THEREOF, AND USE THEREOF - The invention relates to peptides of the general formula (I) GX | 08-23-2012 |
20120214749 | MICROPARTICLES COMPRISING SOMATOSTATIN ANALOGUES - Disclosed are microparticles comprising a somatostatin analogue embedded in a biocompatible pharmacologically acceptable polymer matrix for a long acting release and pharmaceutical compositions comprising such microparticles. | 08-23-2012 |
20120214750 | CRYSTALLINE FORM OF LINACLOTIDE - The present invention relates to crystalline forms of linaclotide, as well as to various methods and processes for the preparation and use of the crystalline forms. | 08-23-2012 |
20120225828 | Melanocortin-1 Receptor-Specific Cyclic Peptides - Melanocortin receptor-specific cyclic peptides of the formula | 09-06-2012 |
20120225829 | METHOD OF PRODUCING FR901228 - Depsipeptides and congeners thereof are disclosed having structure (I), wherein m, n, p, q, X, R1, R2 and R3 are as defined herein. These compounds, including FR901228, have activity as, for example, immunosuppressants, as well as for the prevention or treatment of patients suffering or at risk of suffering from inflammatory, autoimmune or immune system-related diseases including graft-versus-host disease and enhancement of graft/tissue survival following transplant. Also provided are methods for inhibiting lymphocyte activation, proliferation, and/or suppression of IL-2 secretion. | 09-06-2012 |
20120225830 | METHOD OF PRODUCING FR901228 - Depsipeptides and congeners thereof are disclosed having structure (I), wherein m, n, p, q, X, R1, R2 and R3 are as defined herein. These compounds, including FR901228, have activity as, for example, immunosuppressants, as well as for the prevention or treatment of patients suffering or at risk of suffering from inflammatory, autoimmune or immune system-related diseases including graft-versus-host disease and enhancement of graft/tissue survival following transplant. Also provided are methods for inhibiting lymphocyte activation, proliferation, and/or suppression of IL-2 secretion. | 09-06-2012 |
20120238507 | ALPHA HELICAL MIMICS, THEIR USES AND METHODS FOR THEIR PRODUCTION - Disclosed are short chain peptides that are constrained to adopt an alpha helicial conformation and their use as alpha helical scaffolds for directing amino acid side chains into positions analogous to those found in longer chain alpha helical peptides. Also disclosed is the use of these peptides for attaching peptidic or non-peptidic appendages in order to mimic side chains of longer alpha helical peptides. The peptides find use in mimicking naturally occurring peptides or proteins or in preparing new materials. | 09-20-2012 |
20120270806 | Designer Cyclic Peptides - HIV gp120 Antagonists and their Applications - The present invention is concerned with a novel composition of matter—a cyclic peptide derived from computer modeling studies that modulates the structure and function of the HIV main envelope protein gp120. The compound is capable of binding to the CD4-binding region of gp120 (this defines it as a CD4 mimic), and can be used for the purposes of: (1) controlling and preventing HIV infections, (2) detecting, isolating and purifying gp120. Contrary to examples of prior art that involved CD4 mimics being either small molecules or macromolecules, the present invention is concerned with the class of “large small molecules” that may offer a satisfactory balance between the activity and drug-like properties. Modified variants of the prototype compound that can be reasonably considered its derivatives are also claimed. | 10-25-2012 |
20120270807 | MACROCYCLIC INHIBITORS OF SERINE PROTEASE ENZYMES - The present invention relates to novel macrocyclic compounds and salts thereof that bind to and/or are inhibitors of serine protease enzymes. The present invention also relates to intermediates of these compounds, pharmaceutical compositions containing these compounds and methods of using the compounds. These compounds are useful as therapeutics for treatment and prevention of a range of disease indications including hyperproliferative disorders, in particular those characterized by tumor metastasis, inflammatory disorders, skin and tissue disorders, cardiovascular disorders, respiratory disorders and viral infections. | 10-25-2012 |
20120283196 | BETA-HAIRPIN PEPTIDOMIMETICS - β-Hairpin peptidomimetics of the general formula Cyclo(-Xaa | 11-08-2012 |
20130005666 | REPORTER SYSTEM FOR HIGH THROUGHPUT SCREENING OF COMPOUNDS AND USES THEREOF - The NF-E2-related factor 2 (Nrf2) is a key transcriptional regulator of antioxidant defense and detoxification. To directly monitor stabilization of Nrf2 we fused its Neh2 domain, responsible for the interaction with its nucleocytoplasmic regulator, Keap1, to firefly luciferase (Neh2-luciferase). It is shown herein that Neh2 domain is sufficient for recognition, ubiquitination and proteasomal degradation of Neh2-luciferase fusion protein. The novel Neh2-luc reporter system allows direct monitoring of the adaptive response to redox stress and classification of drugs based on the time-course of reporter activation. The novel reporter was used to screen a library of compounds to identify activators of Nrf2. The most robust and yet non toxic Nrf2 activators found—nordihydroguaiaretic acid, fisetin, and gedunin-induced astrocyte-dependent neuroprotection from oxidative stress via an Nrf2-dependent mechanism. | 01-03-2013 |
20130012454 | Orally Disintegrating Compositions of Linaclotide - The present invention relates to orally disintegrating or dissolving pharmaceutical compositions comprising linaclotide or pharmaceutically acceptable salts thereof, as well to various methods and processes for the preparation and use of the compositions. | 01-10-2013 |
20130040898 | METHODS OF TREATMENT OF PATIENTS AT INCREASED RISK OF DEVELOPMENT OF ISCHEMIC EVENTS AND COMPOUNDS HEREOF - The present invention relates to compounds for treatment that protects the endothelium, prevents pathologic thrombus formation in the microcirculation and preserves platelet number and function and thus may be related to treatment or prevention of ischemic events in patients with cardiovascular disease. The present invention is particularly useful for patients having or being at increased risk of development of an ischemic event such as an acute myocardial infarction and/or no-reflow phenomena and/or ischemia-reperfusion injury by administration of agent(s) modulating and/or preserving endothelial integrity. The compounds may be administered in combination with standard treatment of acute cardiovascular ischemic events such as Platelet inhibitors such as aspirin (ASA), Thienopyridins, GPIIb/IIIa inhibitors), Parenteral anticoagulants such as unfractioned heparin (UFH), bivalirudin, enoxaparin, and fondaparinux, Verapamil, Adenosine, Sodium nitroprusside, Nitroglycerin, Epinephrine, Beta-blockers and surgical methods such as percutaneous coronary intervention (PCI), PCI with thrombus aspiration, PCI with stents. | 02-14-2013 |
20130059797 | Linaclotide for the Treatment of Chronic Constipation - The invention provides methods for treating a patient with chronic constipation by administering a therapeutically effective dose of linaclotide. | 03-07-2013 |
20130065839 | TREATMENT OF T-CELL MEDIATED DISEASES - The invention provides a method of treating T-cell mediated diseases and a method of inhibiting the activation of T-cells using certain diketopiperazines. The invention also provides methods of synthesizing diketopiperazines and pharmaceutical compositions comprising certain diketopiperazines. The invention further provides methods of making improved pharmaceutical compositions of proteins and peptides by either increasing or decreasing the content of diketopiperazines in the compositions and the resultant improved pharmaceutical compositions. | 03-14-2013 |
20130072444 | ORGANIC COMPOUND FOR THE REGULATION OF VECTORIAL ION CHANNELS - A cyclic organic compound which comprises 16 amino acids or 17 amino acids and has no carboxyl group C-terminally and/or no amino group N-terminally. Optionally, one of the amino acids is a normatural amino acid. The ring closure is formed between a side chain of one amino acid and the C-terminus of another amino acid, or the ring closure is effected with the aid of a normatural amino acid. A process for producing and using the compound for regulating vectorial ion channels, for treating diseases associated with the lung function and for treating oedemas is provided. | 03-21-2013 |
20130079292 | CYCLIC PEPTIDES BINDING CXCR4 RECEPTOR AND RELATIVE MEDICAL AND DIAGNOSTIC USES - The present invention relates to the identification of new peptides and peptidomimetics which bind the CXCR4 receptor, capable of forming complexes with receptors for chemokines, in particular with CXCR4. The invention also relates to the use of these peptides for the treatment, prevention and diagnosis of diseases which involve chemokine receptors (i.e. neoplasias, metastases, HIV-1 virus infections), and also the mobilization of stem cells of hemopoietic precursors in the case of autologous transplants. Finally, the invention comprises pharmaceutical compositions and diagnostic kits comprising said peptides. | 03-28-2013 |
20130096071 | Agonists of Guanylate Cyclase Useful For the Treatment of Gastrointestinal Disorders, Inflammation, Cancer and Other Disorders - The invention provides novel guanylate cyclase-C agonist peptides and their use in the treatment of human diseases including gastrointestinal disorders, inflammation or cancer (e.g., a gastrointestinal cancer). The peptides can be administered either alone or in combination with an inhibitor of cGMP-dependent phosphodiesterase. The gastrointestinal disorder may be classified as either irritable bowel syndrome, constipation, or excessive acidity etc. The gastrointestinal disease may be classified as either inflammatory bowel disease or other GI condition including Crohn's disease and ulcerative colitis, and cancer. | 04-18-2013 |
20130109633 | CB-183,315 Compositions and Related Methods | 05-02-2013 |
20130116199 | Agonists of Guanylate Cyclase Useful For the Treatment of Gastrointestinal Disorders, Inflammation, Cancer and Other Disorders - The invention provides novel guanylate cyclase-C agonist peptides and their use in the treatment of human diseases including gastrointestinal disorders, inflammation or cancer (e.g., a gastrointestinal cancer). The peptides can be administered either alone or in combination with an inhibitor of cGMP-dependent phosphodiesterase. The gastrointestinal disorder may be classified as either irritable bowel syndrome, constipation, or excessive acidity etc. The gastrointestinal disease may be classified as either inflammatory bowel disease or other GI condition including Crohn's disease and ulcerative colitis, and cancer. | 05-09-2013 |
20130116200 | Treatment of Vascular Complications of Diabetes - A peptide consisting of 7-17 amino acids and including the adjacent hexamer TX | 05-09-2013 |
20130123196 | THIOETHER-, ETHER-, AND ALKYLAMINE-LINKED HYDROGEN BOND SURROGATE PEPTIDOMIMETICS - Provided herein are peptidomimetics and their salts having a stable, internally constrained protein secondary structure containing a thioether-, ether-, or alkylamine-linked hydrogen bond surrogate; compositions containing at least one of these, and methods of making and using these. | 05-16-2013 |
20130123197 | Crystal of Peptide Substance as well as the Preparation Method and Use Thereof - The present invention discloses a crystal of a peptide substance and the preparation method as well as the use thereof. Said crystal B possesses peaks at the following 2θ angles in the X-ray diffraction pattern (XRPD): 3.2±0.2°, 5.4±0.2°, 6.2±0.2°, and 9.3±0.2°. | 05-16-2013 |
20130157964 | Blockade Of Inflammatory Proteases With Cyclic Peptides - Drug compositions for treatment of one or more inflammatory conditions can includes at least one of a θ-defensin, analog or derivative thereof. Inventive methods include researching θ-defensins, analogs or derivatives thereof for their efficacy with respect to anti-inflammatory effects, and providing such compositions to the marketplace for the purpose of treating inflammatory conditions. Of particular interest are drug compositions effective to produce clinically relevant inhibition of tumor necrosis factor alpha (TNF-α)-converting enzyme (TACE) or other proinflammatory proteases, and/or sheddases. it is contemplated that preferred compositions can be used to treat rheumatoid arthritis, inflammatory bowel disease, and other chronic inflammatory diseases, autoimmune diseases, cancer, and Alzheimer's, osteoarthritis, inflammation-related neurodegenerative and other inflammation-related diseases. | 06-20-2013 |
20130172270 | RGD-CONTAINING CYCLIC PEPTIDES - The present invention is drawn to cyclic RGD peptides linked via a disulfide bond, where the terminal cysteines are preferably in the D configuration. These peptides target αvβ3 integrin on tumor cells and neovasculatures and function as targeting agents for tumor diagnostic imaging and therapy. Compared with the commonly used RGD ligands, compounds of the present invention have improved targeting efficacy and lower nonspecific binding to normal organs. Moreover, the compounds of the present invention can be functionalized to conjugate imaging payload without decreasing binding strength. | 07-04-2013 |
20130172271 | Pharmaceutical Spray Drying - Methods and formulations for preparing spray dried pharmaceutical products including daptomycin, azithromycin, cyclophosphamide, and voriconazole. | 07-04-2013 |
20130172272 | Novel Polypeptides That Bound to IL-23 Receptor and Inhibit Binding of IL-23 and Cell Signaling Thereof - The present invention relates to novel polypeptides that bind to IL-23 receptor and inhibit the binding of IL-23 to its corresponding receptor and cell signaling thereof. The novel polypeptides of the present invention has a core structure of WX | 07-04-2013 |
20130172273 | CYCLOTETRAPEPTIDES WITH PRO-ANGIOGENIC PROPERTIES - Cyclotetrapeptides of formula (I) or their pharmaceutically acceptable salts, cyclo[Arg-Asp-(beta-Lactam)] (I) wherein (beta-Lactam) is a biradical of the formula (II) wherein the terminal NH group of the (beta-Lactam) is attached to the α-carbonyl group of the aspartic residue (Asp), and the terminal carbonyl group of the (beta-Lactam) is attached to the α-amino group the arginine residue (Arg); processes for their preparation, and pharmaceutical compositions containing them, as well as their use in human and animal therapy. | 07-04-2013 |
20130178429 | MACROCYCLIC KINASE INHIBITORS AND USES THEREOF - The present invention provides macrocyclic compounds of Formula (I): pharmaceutically acceptable salts thereof; and pharmaceutical compositions thereof, wherein R | 07-11-2013 |
20130203681 | Macrocyclic Compounds Useful as Inhibitors of Histone Deacetylases - The present invention provides a novel macrocyclic compound of general Formula (I) having histone deacetylase (HDAC) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound. | 08-08-2013 |
20130210746 | PHARMACEUTICAL COMPOSITION - The present invention relates to pharmaceutical compositions having improved stability. | 08-15-2013 |
20130225506 | TEMPLATE-FIXED PEPTIDOMIMETICS WITH CXCR7 MODULATING ACTIVITY - Novel template-fixed β-hairpin peptidomimetics of the general formula (I), wherein the single elements T or P are α-amino acid residues connected from the carbonyl (C═O) point of attachment to the nitrogen (N) of the next element in clockwise direction and wherein said elements, depending on their positions in the chain, are defined in the description and the claims have the property to act on the receptor CXCR7. Thus, these β-hairpin peptidomimetics can be useful in the treatment or prevention of diseases or conditions in the area of dermatological disorders, metabolic diseases, inflammatory diseases, fibrotic diseases, infectious diseases, neurological diseases, cardiovascular diseases, respiratory diseases, gastro-intestinal tract disorders, urological diseases, ophthalmic diseases, stomatological diseases, haematological diseases and cancer; or the mobilisation of stem cells. | 08-29-2013 |
20130225507 | METHOD OF PRODUCING FR901228 - Depsipeptides and congeners thereof are disclosed having structure (I), wherein m, n, p, q, X, R1, R2 and R3 are as defined herein. These compounds, including FR901228, have activity as, for example, immunosuppressants, as well as for the prevention or treatment of patients suffering or at risk of suffering from inflammatory, autoimmune or immune system-related diseases including graft-versus-host disease and enhancement of graft/tissue survival following transplant. Also provided are methods for inhibiting lymphocyte activation, proliferation, and/or suppression of IL-2 secretion. | 08-29-2013 |
20130261066 | TREATMENT OF INFLAMMATORY BOWEL DISEASES USING A TRIPEPTIDE - The present invention provides peptides and peptide conjugates for treating inflammatory bowel diseases, including ulcerative colitis and Crohn's disease. The peptides are derived from annexin-1, can be acetylated or conjugated to fatty acids, may be linear or cyclic, and may comprise D amino acids. Pharmaceutical compositions and methods of use are also disclosed. | 10-03-2013 |
20130274205 | PEPTIDOMIMETIC MACROCYCLES - Provided herein are peptidomimetic macrocycles and methods of using such macrocycles for the treatment of disease. | 10-17-2013 |
20130296256 | Melanocortin-1 Receptor-Specific Cyclic Peptides - Melanocortin receptor-specific cyclic peptides of the formula | 11-07-2013 |
20130303463 | TREATMENT OF DISEASES - The invention provides (i) a method of treating metabolic syndrome in an animal, (ii) a method of suppressing the appetite of an animal, (iii) a method of treating obesity in an animal, (iv) a method of reducing the weight of an animal in need thereof, (v) a method of reducing a blood lipid level in an animal in need thereof, (vi) a method of treating non-alcoholic steatohepatitis in an animal, and (vii) a method of inhibiting adipogenesis. The methods comprise administering an effective amount of an active ingredient, wherein the active ingredient comprises a diketopiperazine, a prodrug of a diketopiperazine or a pharmaceutically-acceptable salt of either of them to the animal. The invention also provides a kit comprising a container holding a diketopiperazine, a prodrug of a diketopiperazine or a pharmaceutically-acceptable salt of either of them; and instructions for administration of the diketopiperazine, the prodrug or the pharmaceutically-acceptable salt according to a method of the invention. The diketopiperazines have the formula given in the application. | 11-14-2013 |
20130310328 | Agonists of Guanylate Cyclase Useful for the Treatment of Gastrointestinal Disorders, Inflammation, Cancer and Other Disorders - The invention provides novel guanylate cyclase-C agonist peptides and their use in the treatment of human diseases including gastrointestinal disorders, inflammation or cancer (e.g., a gastrointestinal cancer). The peptides can be administered either alone or in combination with an inhibitor of cGMP-dependent phosphodiesterase. The gastrointestinal disorder may be classified as either irritable bowel syndrome, constipation, or excessive acidity etc. The gastrointestinal disease may be classified as either inflammatory bowel disease or other GI condition including Crohn's disease and ulcerative colitis, and cancer. | 11-21-2013 |
20130324482 | COMPSTATIN ANALOGS FOR TREATMENT OF RHINOSINUSITIS AND NASAL POLYPOSIS - In some aspects, the present invention provides methods treating a subject in need of treatment for chronic rhinosinusitis or nasal polyposis, the methods comprising administering a complement inhibitor such as a compstatin analog to the subject. In some embodiments, the complement inhibitor is administered intranasally, e.g., in a nasal spray. | 12-05-2013 |
20140018307 | LINACLOTIDE COMPOSITIONS - The present invention is directed to stable linaclotide compositions and methods of treating gastrointestinal disorders in patients in need thereof by providing the stable linaclotide compositions. | 01-16-2014 |
20140024605 | Agonists of Guanylate Cyclase Useful For the Treatment of Gastrointestinal Disorders, Inflammation, Cancer and Other Disorders - The invention provides novel guanylate cyclase-C agonist peptides and their use in the treatment of human diseases including gastrointestinal disorders, inflammation or cancer (e.g., a gastrointestinal cancer). The peptides can be administered either alone or in combination with an inhibitor of cGMP-dependent phosphodiesterase. The gastrointestinal disorder may be classified as irritable bowel syndrome, constipation, or excessive acidity etc. The gastrointestinal disease may be classified as either inflammatory bowel disease or other GI condition, including Crohn's disease and ulcerative colitis, and cancer. | 01-23-2014 |
20140038907 | Coatings For Implantable Medical Devices - The present application teaches a coating having a biologically compatible compound conjugated to, or blended with, a polymer, wherein the polymer includes at least one olefin-derived unit and at least one unit derived from a vinyl alcohol, an allyl alcohol, or derivatives thereof. | 02-06-2014 |
20140045774 | METHODS FOR TREATING VIRAL DISORDERS - Disclosed are methods of treating viral disorders via the administration of an inducing agent and an anti-viral agent. In one embodiment, the inducing agent and the anti-viral agent are administered for about five days, and the anti-viral agent is subsequently administered without the inducing agent for an additional period of about sixteen days for a total cycle of about 21 days. | 02-13-2014 |
20140057857 | Cross-Linked Peptides and Proteins, Methods of Making Same, and Uses Thereof - Cross-linked proteins and peptides, and methods of making and uses of such cross-linked proteins and peptides. The cross-linked proteins and peptides have rigid, distance-matching bismethylene aryl cross-linking moieties. Compositions comprising the cross-linked proteins and peptides can be used as pharmaceutical delivery formulations. The cross-linked proteins and peptides can have improved properties, such as cell permeability, as compared to the parent protein or peptide. | 02-27-2014 |
20140113871 | Modification of Peptides via SNAr Reactions of Thiols with Fluorinated Aromatics - Disclosed are compounds and methods relating to a chemical transformation for the conjugation of unprotected peptide biomolecules via a S | 04-24-2014 |
20140113872 | NOVEL AGONISTS AND ANTAGONISTS OF THE UROTENSINERGIC SYSTEM - Novel urotensin ll receptor (UT) agonists and antagonists are described herein. More specifically, novel derivatives of urotensin ll-related peptide (URP) are described herein. | 04-24-2014 |
20140135273 | CB-183,314 COMPOSITIONS AND RELATED METHODS - The present disclosure provides novel solid CB-183,315 formulations which have improved chemical stability. The chemical stability of the solid CB-183,315 is dependent on the process by which the composition is made. Solid preparations of CB-183,315 can be prepared by the following method: (a) forming an aqueous solution of CB-183,315 and at least one sugar that (e.g., sucrose, trehalose or dextran) at a pH of 2-7, preferably pH 6 and (b) converting the aqueous solution to the solid preparation of CB-183,315 (e.g., via lyophilization or spray drying). | 05-15-2014 |
20140135274 | Agonists of Guanylate Cyclase Useful For the Treatment of Gastrointestinal Disorders, Inflammation, Cancer and Other Disorders - The invention provides novel guanylate cyclase-C agonist peptides and their use in the treatment of human diseases including gastrointestinal disorders, inflammation or cancer (e.g., a gastrointestinal cancer). The peptides can be administered either alone or in combination with an inhibitor of cGMP-dependent phosphodiesterase. The gastrointestinal disorder may be classified as either irritable bowel syndrome, constipation, or excessive acidity etc. The gastrointestinal disease may be classified as either inflammatory bowel disease or other GI condition including Crohn's disease and ulcerative colitis, and cancer. | 05-15-2014 |
20140162963 | Treatment of Constipation-Predominant Irritable Bowel Syndrome - The invention provides methods for treating a patient with constipation-predominant irritable bowel syndrome by administering a therapeutically effective dose of linaclotide. | 06-12-2014 |
20140187500 | COMPOUNDS, CONJUGATES AND COMPOSITIONS OF EPIPOLYTHIODIKETOPIPERAZINES AND POLYTHIODIKETOPIPERAZINES - The present application provides, among other things, compounds, compositions and methods for treating various diseases including cancer. | 07-03-2014 |
20140187501 | Targeted Conjugates Encapsulated in Particles and Formulations Thereof - Particles, including nanoparticles and microparticles, and pharmaceutical formulations thereof, containing conjugates of an active agent such as a therapeutic, prophylactic, or diagnostic agent attached to a targeting moiety via a linker have been designed which can provide improved temporospatial delivery of the active agent and/or improved biodistribution. Methods of making the conjugates, the particles, and the formulations thereof are provided. Methods of administering the formulations to a subject in need thereof are provided, for example, to treat or prevent cancer or infectious diseases. | 07-03-2014 |
20140194369 | CYCLIC LACTADHERIN PEPTIDE MIMETICS AND THEIR USES - Provided herein is a new class of cyclic lactadherin peptides (cLac) that mimic the natural phosphatidylserine (PS)-binding activity of the parent lactadherin protein. These cLacs are useful as small molecule indicators of early stage of apoptosis and of treatment efficacy evaluation. | 07-10-2014 |
20140200186 | SMALL MOLECULE COMPOSITE SURFACES AS INHIBITORS OF PROTEIN-PROTEIN INTERACTIONS - A method of inhibiting a binding event between a target protein and a binding protein, comprising administering to a cell in vitro an effective amount of a non-naturally occurring bifunctional inhibitor molecule including (a) protein binding moiety, and (b) an effector region, wherein the protein binding moiety binds to a blocking protein, and wherein the effector region binds to the target protein in order to bind the target protein and the blocking protein and prevent access of the binding protein to the target protein. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. | 07-17-2014 |
20140235555 | Pharmaceutical compositions comprising polyethylene glycol having a molecular weight of less than 600 daltons - A liquid pharmaceutical composition comprising a biodegradable polymer, polyethylene glycol having a molecular weight of less than 600 Dalton's, a pharmaceutically active agent and less than 0.5% of an biologically acceptable organic solvent. | 08-21-2014 |
20140235556 | COMPOSITIONS AND METHODS OF TREATING GLIOMAS - The present invention provides, inter alia, methods for treating or ameliorating the effects of a glioma. Methods of this invention include administering to a subject in need thereof an effective amount of a first active agent, such as e.g., an angiotensin receptor blocker, an antifungal agent, a bisphosphonate, an oxytocin inhibitor, an interleukin-1 (IL-1) inhibitor, a cyclooxygenase inhibitor, an α2δ voltage-dependent calcium channel (VDCC) inhibitor, a dihydroorotate dehydrogenase inhibitor, a calcium channel blocker, a renal sodium-chloride symporter inhibitor, an a2 adrenergic agonist, a phenothiazine antipsychotic, a calcineurin inhibitor, a 5-HT agonist, an angiotensin-converting enzyme (ACE) inhibitor, a direct rennin inhibitor, or combinations thereof, and a second active agent, which is a chemotherapeutic agent. Compositions for treating or ameliorating the effects of a glioma are also provided. | 08-21-2014 |
20140274914 | ACH-0142684 SODIUM SALT POLYMORPH, COMPOSITION INCLUDING THE SAME, AND METHOD OF MANUFACTURE THEREOF - The disclosure provides a crystalline sodium salt of ACH-0142684 comprising a Form A polymorph, a Form B polymorph, a Form C polymorph, a Form D polymorph, a Form E polymorph, a Form F polymorph, a Form G polymorph, a Form H polymorph, a Form I polymorph, or a combination thereof, wherein the Form A, B, C, D, E, F, G, H, and I polymorph exhibits an X-ray powder diffraction pattern having peak locations in accordance with FIGS. | 09-18-2014 |
20140296160 | STABILIZED ALPHA HELICAL PEPTIDES AND USES THEREOF - Novel polypeptides and methods of making and using the same are described herein. The polypeptides include cross-linking (“hydrocarbon stapling”) moieties to provide a tether between two amino acid moieties, which constrains the secondary structure of the polypeptide. The polypeptides described herein can be used to treat diseases characterized by excessive or inadequate cellular death. | 10-02-2014 |
20140296161 | DIDEMNIN BIOSYNTHETIC GENE CLUSTER IN TISTRELLA MOBILIS | 10-02-2014 |
20140336132 | ROMIDEPSIN SOLID FORMS AND USES THEREOF - The present disclosure provides solid forms of a compound of formula I. In some embodiments, the present disclosure provides crystalline forms of Compound I. In some embodiments, the present disclosure provides solvate forms of Compound I. In some embodiments, the present disclosure provides amorphous Compound I. | 11-13-2014 |
20140349948 | Treatment of Chronic Constipation - The invention provides methods for treating a patient with chronic constipation by administering a therapeutically effective dose of linaclotide. | 11-27-2014 |
20140349949 | HYALURONIC ACID CONTAINING COMPOSITIONS FOR TREATMENT OF WOUNDS, SCARS, POST-SURGICAL ADHESION FORMATION - The present invention relates to pharmaceutical compositions enhancing the therapeutic effect of biologically active peptides, especially peptides derived from human lactoferrin. The compositions are useful for the treatment and/or prevention of wounds, scars, and post surgical adhesions. | 11-27-2014 |
20140357575 | Melanocortin Receptor-Specific Heptapeptides - Melanocortin receptor-specific cyclic heptapeptides of the formula | 12-04-2014 |
20140364380 | LIPOPEPTIDE COMPOSITIONS AND RELATED METHODS - The present disclosure provides novel powder daptomycin formulations which have improved chemical stability and faster reconstitution times when in the solid state. Some examples of the compositions comprise daptomycin and sucrose. | 12-11-2014 |
20140378393 | Stable Formulations of Linaclotide - The present invention relates to stable pharmaceutical compositions comprising linaclotide or pharmaceutically acceptable salts thereof, as well as to various methods and processes for the preparation and use of the compositions. | 12-25-2014 |
20150011481 | Methods for Treating HCV - The present invention features interferon-free therapies for treating HCV genotype 1b, 2, 3 or 4. In one aspect, the therapies comprise administering Compound 1, ritonavir, and Compound 2 to a subject infected with HCV genotype 1b or 4, wherein the therapies do not include administration of any interferon, and the therapies last for 12 weeks. Preferably, the therapies do not include administration of any ribavirin. | 01-08-2015 |
20150031631 | PHARMACEUTICAL COMPOSITIONS AND RELATED METHODS OF DELIVERY - The pharmaceutical compositions described herein include a suspension which comprises an admixture in solid form of a therapeutically effective amount of a therapeutic agent and at least one salt of a medium chain fatty acid and a hydrophobic medium, e.g. castor oil or glyceryl tricaprylate or a mixture thereof. The pharmaceutical compositions described herein contain medium chain fatty acid salts and are substantially free of alcohols. The pharmaceutical compositions may be encapsulated in a capsule. Methods of treating or preventing diseases by administering such compositions to affected subjects are also disclosed. | 01-29-2015 |
20150031632 | Orally Disintegrating Compositions of Linaclotide - The present invention relates to orally disintegrating or dissolving pharmaceutical compositions comprising linaclotide or pharmaceutically acceptable salts thereof, as well as to various methods and processes for the preparation and use of the compositions. | 01-29-2015 |
20150038434 | Melanocortin-1 Receptor-Specific Cyclic Peptides - Melanocortin receptor-specific cyclic peptides of the formula | 02-05-2015 |
20150045310 | NOVEL ENGINEERED POTENT CYTOTOXIC STAPLED BH3 PEPTIDES - Compositions comprising peptide sequences with high cytotoxicity to cancer cell lines are provided. Pharmaceutical compositions comprising peptide sequences with high cytotoxicity to cancer cell lines are provided. A method for treating cancer is provided. | 02-12-2015 |
20150057234 | HYDRATE OF CYCLOPEPTIDE COMPOUND AS WELL AS PREPARATION METHOD AND USE THEREOF - Disclosed is a hydrate of a compound as shown in Formula I. In formula I, R represents H or a cation capable of forming a pharmaceutically acceptable salt. The mass percentage of water in the hydrate is more than 8%. The hydrate has good stability. Moreover, disclosed are a preparation method and a use thereof. | 02-26-2015 |
20150057235 | AGONISTS OF GUANYLATE CYCLASE USEFUL FOR THE TREATMENT OF GASTROINTESTINAL DISORDERS, INFLAMMATION, CANCER AND OTHER DISORDERS - The invention provides novel guanylate cyclase-C agonist peptides and their use in the treatment of human diseases including gastrointestinal disorders, inflammation or cancer (e.g., a gastrointestinal cancer). The peptides can be administered either alone or in combination with an inhibitor of cGMP-dependent phosphodiesterase. The gastrointestinal disorder may be classified as either irritable bowel syndrome, constipation, or excessive acidity etc. The gastrointestinal disease may be classified as either inflammatory bowel disease or other GI condition, including Crohn's disease and ulcerative colitis, and cancer. | 02-26-2015 |
20150072939 | LISURID, TERGURIDE AND DERIVATIVES THEREOF FOR USE IN THE PROPHYLAXIS AND/OR TREATMENT OF FIBROTIC CHANGES - The present invention relates to the use of 5-HT | 03-12-2015 |
20150080319 | Inhibition Of Tace Activity With Cyclic Peptides - A method is provided for inhibiting TACE activity in a human subject, through the administration of a θ-defensin, analog, or derivative. Such a θ-defensin, analog, or derivative can be effectively administered parenterally, topically, or orally. The θ-defensin, analog, or derivative can be selected to additionally inhibit ADAM-10 activity. | 03-19-2015 |
20150094272 | Treatments for Gastrointestinal Disorders - The present invention features peptides, compositions, and related methods for treating gastrointestinal disorders and conditions, including but not limited to, irritable bowel syndrome (IBS), gastrointestinal motility disorders, functional gastrointestinal disorders, gastroesophageal reflux disease (GERD), duodenogastric reflux, Crohn's disease, ulcerative colitis, inflammatory bowel disease, functional heartburn, dyspepsia, visceral pain, gastroparesis, chronic intestinal pseudo-obstruction (or colonic pseudo-obstruction), disorders and conditions associated with constipation, and other conditions and disorders are described herein, using peptides and other agents that activate the guanylate cyclase C (GC-C) receptor. | 04-02-2015 |
20150105331 | HIGH-PURITY CYCLOPEPTIDE CRYSTAL AS WELL AS PREPARATION METHOD AND USE THEREOF - A high purity cyclopeptide crystal has a structure shown by Formula I. R represents H or a cation forming a pharmaceutically acceptable salt. Also disclosed are a preparation method and a use of the high-purity cyclopeptide crystal. | 04-16-2015 |
20150105332 | SOMATOSTATIN RECEPTOR AGONIST FORMULATIONS - The present invention relates to compositions forming a low viscosity mixture of: a) 20-50 wt. % of at least one diacyl glycerol; b) 20-54 wt. % of at least one phosphatidyl choline (PC); c) 5-15 wt. % of at least one biocompatible, organic mono-alcoholic solvent; d) 1 to 20 wt. % polar solvent e) 5 to 150 mg/ml of at least one peptide somatostatin receptor agonist comprising pasireotide; f) optionally at least one antioxidant; wherein the ratio of components a:b is in the range 40:60 to 54:46; wherein the pre-formulation forms, or is capable of forming, at least one liquid crystalline phase structure upon contact with excess aqueous fluid. The invention further relates to methods of treatment comprising administration of such compositions, and to pre-filled administration devices and kits containing the formulations. | 04-16-2015 |
20150105333 | LATENT HUMAN IMMUNODEFICIENCY VIRUS REACTIVATION - Provided herein are methods or reactivating a latent Human Immunodeficiency Virus (HIV) infection in a cell. The methods comprise modulating a level of NF-κB activity in the cell by contacting the cell with an agent that produces a transient first increase in the level of NF-κB activity without a second delayed increase in NF-κB activity. Optionally, a second agent is used to prime the reactivation. Also provided herein is an isolated | 04-16-2015 |
20150141349 | Method and Composition for Alleviating Tumor Symptoms - This invention relates to methods and compositions for treating carcinoid syndrome and other adverse symptoms associated with tumor-producing neuroendocrine tumors, said methods comprising administering a therapeutically effective amount of a vascular disrupting agent, or a pharmaceutically acceptable salt thereof, to a subject having a hormone producing neuroendocrine tumor. In preferred implementations, the vascular disrupting agent is combretastatin A-4 phosphate, combretastatin A-1 diphosphate, or a pharmaceutical acceptable salt thereof. | 05-21-2015 |
20150291662 | MODIFIED PEPTIDE, CB RECEPTOR LIGAND, KIT IN VITRO PROCESS FOR EVALUATING CB RECEPTOR BONDS, USES, PHARMACEUTICAL COMPOSITION FOR MODULATING CB RECEPTOR ACTIVITY - The present invention discloses novel non-natural and modified peptides acting as cannabinoid (CB) receptors ligands, especially CB1 and/or CB2, useful as modulators of its activity; they are also described as a kit and a process in vitro for evaluating the binding to CB receptors, uses and pharmaceutical composition for modulating the CB receptors activity. The invention covers the non-natural peptide of SeqID:1 and those having at least 70% similarity related to the same, including as achievements specialty useful of the invention the non-natural peptides of SeqID:2, SeqID:3, SeqID:4, SeqID:5, SeqID:6. | 10-15-2015 |
20150306225 | Compositions for Delivering Drugs with Low Water Solubility - The present invention provides compositions comprising polymeric micelles containing a drug with low water solubility, wherein sterol rings of pegylated sterols and the drug form a hydrophobic portion and polyethylene glycol chains of the pegylated sterols forms a hydrophilic portion. The present invention also provides methods of preparing and using such compositions for delivering drug(s) with low water solubility to a subject in need thereof. | 10-29-2015 |
20150307555 | VASOPRESSIN-2 RECEPTOR AGONISTS - Vasopressin-2 receptor agonists, pharmaceutical compositions thereof and methods for using the foregoing for treating diabetes insipidus, primary nocturnal enuresis, and nocturia. | 10-29-2015 |
20150328282 | METHODS FOR TREATING VIRAL DISORDERS - Disclosed are methods of treating viral disorders via the administration of an inducing agent and an anti-viral agent. In one embodiment, the inducing agent and the anti-viral agent are administered for about five days, and the anti-viral agent is subsequently administered without the inducing agent for an additional period of about sixteen days for a total cycle of about 21 days. | 11-19-2015 |
20150352104 | USE OF LEVOCETIRIZINE AND MONTELUKAST IN THE TREATMENT OF TRAUMATIC INJURY - The embodiments described herein include methods and formulations for treating lung and brain injury. The methods and formulations include, but are not limited to, methods and formulations for delivering effective concentrations of levocetirizine and montelukast to a patient in need. The methods and formulations can comprise conventional and/or modified-release elements, providing for drug delivery to the patient. | 12-10-2015 |
20150366935 | FORMULATIONS OF GUANYLATE CYCLASE C AGONISTS AND METHODS OF USE - The invention provides low-dose formulations of guanylate cyclase-C (“GCC”) agonist peptides and methods for their use. The formulations of the invention can be administered either alone or in combination with one or more additional therapeutic agents, preferably an inhibitor of cGMP-dependent phosphodiesterase or a laxative. | 12-24-2015 |
20150374824 | STABLE NOCATHIACIN LYOPHILIZED INJECTION AGENT - A stable and lyophilized pharmaceutical agent containing nocathiacin, which is prepared by lyophilizing a liquid formulation of nocathiacin, a stabilizer, an excipient, a pH regulator and injectable water, wherein the stabilizer is selected from polyethylene glycol, polysorbate or a mixture thereof, and the pH value of the liquid formulation is 1.0-6.0 is provided. | 12-31-2015 |
20150376164 | HYDROXYINDALPINE DERIVATIVES AND THEIR MEDICAL USE - The present invention relates to hydroxyindalpine derivatives of formula (I) as defined herein and pharmaceutical compositions comprising these compounds, as well as their medical use, particularly in the treatment or prevention of gastrointestinal diseases/disorders, such as constipation and functional dyspepsia. | 12-31-2015 |
20160017000 | RGD-CONTAINING CYCLIC PEPTIDES - The present invention is drawn to cyclic RGD peptides linked via a disulfide bond, where the terminal cysteines are preferably in the D configuration. These peptides target αvβ3 integrin on tumor cells and neovasculatures and function as targeting agents for tumor diagnostic imaging and therapy. Compared with the commonly used RGD ligands, compounds of the present invention have improved targeting efficacy and lower nonspecific binding to normal organs. Moreover, the compounds of the present invention can be functionalized to conjugate imaging payload without decreasing binding strength. | 01-21-2016 |
20160017002 | Process for Preparing Eptifibatide - The present invention provides processes for preparation of eptifibatide that involve coupling of amino acids in a (2+5), (4+3) and (3+4) sequence method. The invention further provides products produced by the described processes, novel compounds that can be used as synthetic intermediates for the preparation of eptifibatide. | 01-21-2016 |
20160022763 | COMPOSITIONS AND METHODS FOR INHIBITING CELLULAR ADHESION OR DIRECTING DIAGNOSTIC OR THERAPEUTIC AGENTS TO RGD BINDING SITES - Compounds comprising R-G-Cysteic Acid (i.e., R-G-NH—CH(CH | 01-28-2016 |
20160024153 | STAPLED AND STITCHED POLYPEPTIDES AND USES THEREOF - The present invention provides stapled polypeptides of the Formulae (I) and (VI): (I) (VI) and salts thereof; wherein the groups =====; R | 01-28-2016 |
20160039878 | Novel Polypeptides That Bound to IL-23 Receptor and Inhibit Binding of IL-23 and Cell Signaling Thereof - The present invention relates to novel linear and cyclic polypeptides that bind to IL-23 receptor and inhibit the binding of IL-23 to its corresponding receptor and cell signaling thereof. The novel polypeptides of the present invention has a core structure of WX | 02-11-2016 |
20160068615 | GLYCOGEN-BASED WATER SOLUBILITY ENHANCERS - The present invention relates to glycogen-based polymers and the use thereof for enhancing the solubility in water of lipophilic compounds, to complexes of the said glycogen-based polymers with lipophilic compounds and the use thereof for administering lipophilic compounds, and to pharmaceutical, nutraceutical, and cosmetic compositions comprising the said complexes. | 03-10-2016 |
20160095896 | BIS-SULFHYDRYL MACROCYCLIZATION SYSTEMS - The present invention provides novel peptidomimetic macrocycles and methods for their preparation and use, as well as amino acid analogs and macrocycle-forming linkers, and kits useful in their production. | 04-07-2016 |
20160096866 | POTENT COMPSTATIN ANALOGS - Compounds comprising peptides and peptidomimetics capable of binding C3 protein and inhibiting complement activation are disclosed. These compounds display greatly improved complement activation-inhibitory activity as compared with currently available compounds. Methods of making and using the compounds are also disclosed. | 04-07-2016 |
20160101145 | PEPTIDOMIMETIC MACROCYCLES AND FORMULATIONS THEREOF - Aqueous pharmaceutical formulations, for parenteral administration, comprising peptidomimetic macrocycle or a pharmaceutically acceptable salt thereof wherein the peptidomimetic macrocycle binds to MDM2 and/or MDMX proteins are disclosed. Also disclosed are methods of treating diseases and disorders using the aqueous pharmaceutical formulations disclosed herein. | 04-14-2016 |
20160113995 | LIPID NANOPARTICLE OF POLYMYXIN - A lipid nanoparticle that includes at least one antibiotic from the polymyxin family, a lipid fraction, and one or more surfactants. The lipid nanoparticle is useful in the prevention and/or treatment of respiratory tree infections. | 04-28-2016 |
20160120935 | Sustanined Release Formulation Comprising Octreotide and Two or More Polyactide-co-glycolide Polymers - The present invention relates to sustained release formulations comprising as active ingredient octreotide or a pharmaceutically-acceptable salt thereof and two or more different polylactide-co-glycolide polymers (PLGAs). | 05-05-2016 |
20160143266 | Pharmaceutical Composition Comprising a Cyclic peptide of formula X1-GQRETPEGAEAKPWY-X2 and use for extracorporeal lung treatment - A method of conditioning/improving lung functions extracorporeally by treatment of a lung ex vivo with a cyclized compound of the amino acid sequence of formula | 05-26-2016 |
20160159858 | URIC ACID-LOWERING AGENT - A uric acid-lowering agent containing, as an active ingredient, a tyrosine-containing cyclic dipeptide selected from the group consisting of cyclotryptophanyltyrosine, cycloseryltyrosine, cycloprolyltyrosine, cyclotyrosylglycine, cyclotyrosyltyrosine, cyclophenylalanyltyrosine, cycloleucyltyrosine, cyclolysyltyrosine, cyclohistidyltyrosine, cycloalanyltyrosine, cycloglutamyltyrosine, cyclovalyltyrosine, cycloisoleucyltyrosine, cyclothreonyltyrosine, cycloaspartyltyrosine, cycloasparaginyltyrosine, cycloglutaminyltyrosine, cycloarginyltyrosine, cyclomethionyltyrosine, and cyclotyrosylcysteine, or a salt thereof. The uric acid-lowering agent of the present invention has an excellent action of lowering a uric acid level, and the uric acid-lowering agent is useful in, for example, prevention or treatment of hyperuricemia, gout or the like. | 06-09-2016 |
20190142773 | USE OF HDAC INHIBITORS FOR TREATMENT OF CARDIAC RHYTHM DISORDERS | 05-16-2019 |
20220135623 | PEPTOID-BASED CHELATING LIGANDS FOR SELECTIVE METAL CHELATION - The present disclosure provides peptoid-based chelating ligands, corresponding cyclic peptoids, and methods of making thereof. Functional groups may be tailored for high metal binding affinity and selectivity. The side chains of a cyclic peptoid according to the present disclosure may be selected based on, for example, high affinity for actinide or other metal ions, selectivity for actinide or other metal ions, the ability to recover a metal once it is bound to the peptoid, and whether the overall peptoid should be hydrophobic or hydrophilic. Unlike siderophores, peptoid-based chelating ligands of the present disclosure are not readily hydrolyzed under physiological conditions. Therefore, peptoid-based chelating ligands may be, for example, used to treat actinide (e.g., iron and lead) poisoning in vivo. Moreover, peptoid-based chelating ligands of the present disclosure may be used for medical imaging, chelation therapy, drug delivery, and separation technologies, for example. | 05-05-2022 |
20140121192 | METHODS OF GENERATING BETA-LACTAMASE RESISTANT CARBAPENEM COMPOUNDS - The present invention includes compositions, methods of making and using novel carbapenem compounds including active agents, compounds, antibacterial agents, pharmaceutically acceptable salts of C1α-C1β di-substituted carbapenem compounds, C5α substituted carbapenem compounds, C6α-C6β di-substituted carbapenem compounds and combinations thereof. | 05-01-2014 |
20140235604 | COMPOUNDS AND METHODS OF TREATING OCULAR DISORDERS - A method of treating an ocular disorder in a subject associated with aberrant all-trans-retinal clearance in the retina, the method comprising administering to the subject a therapeutically effective amount of a primary amine compound of formula: | 08-21-2014 |
20140357611 | COMPOUNDS AND METHODS OF TREATING OCULAR DISORDERS - A method of treating an ocular disorder in a subject includes administering to the subject a therapeutically effective amount of a primary amine compound of formula: | 12-04-2014 |
20150306075 | COMPOSITIONS AND METHODS OF INHIBITING METALLO-B-LACTAMASES - A method of treating a bacterial infection in a subject in need thereof includes administering to the subject therapeutically effective amounts of at least one β-lactam antibiotic and at least one bisthiazolidine metallo-β-lactamase inihibitor. | 10-29-2015 |
514210110 | Additional hetero ring attached directly to the sulfur | 8 |
514210120 | The additional hetero ring contains ring nitrogen | 8 |
20080207586 | Novel crystal form of pyrrolidylthiocarbapenem derivative - A novel crystal of a pyrrolidylthiocarbapenem derivative having excellent stability is provided. According to the present invention, a crystal of (+)-(4R,5S,6S)-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-3[[(3S,5S)-5-(sulfamoylaminomethyl)pyrrolidin-3-yl]thio]-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid having a diffraction pattern in powder X-ray diffraction preferably having main peaks at diffraction angles (2θ)=13.04, 14.98, 15.88, 16.62, 20.62, 21.06, 22.18, 23.90, 26.08, 28.22 and 28.98 (degrees) is provided. | 08-28-2008 |
20090075969 | DEUTERIUM-ENRICHED DORIPENEM - The present application describes deuterium-enriched doripenem, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 03-19-2009 |
20110046107 | SULFONYL-SUBSTITUTED CARBAPENEM COMPOUNDS - The present invention relates to a compound of the formula (I), pharmaceutically acceptable salts, hydrolysable esters, isomers and hydrates thereof, and hydrates of the said esters or salts, wherein R | 02-24-2011 |
20110118229 | 2-ARYLMETHYLAZETIDINE-CARBAPENEM-3-CARBOXYLIC ACID ESTER DERIVATIVE OR ITS SALT, PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME - The present invention provides a 2-arylmethylazetidine-carbapenem-3-carboxylic acid ester derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The 2-arylmethylazetidine-carbapenem-3-carboxylic acid ester derivatives or their pharmaceutically acceptable salts show high oral absorption rate, and thus can be orally administered. The active metabolites thereof have a broad spectrum of antibacterial activities against Gram-positive and Gram-negative bacteria and excellent antibacterial activities against methicillin-resistant | 05-19-2011 |
20110281839 | COMBINATION THERAPY FOR THE TREATMENT OF BACTERIAL INFECTIONS - The present invention is directed to co-therapy and methods for the treatment of bacterial infections due to A. baumannii, such as pneumonia, blood stream infections, wound infections, urinary tract infection and intra-abdominal infections. | 11-17-2011 |
20130059831 | NOVEL CRYSTAL FORM OF PYRROLIDYLTHIOCARBAPENEM DERIVATIVE - Novel crystals of a pyrrolidylthiocarbapenem derivative having excellent stability is provided. According to the present invention, a crystal of (+)-(4R,5S,6S)-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-3[[(3S,5S)-5-(sulfamoylaminomethyl)pyrrolidin-3-yl]thio]-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid having a diffraction pattern in powder X-ray diffraction having main peaks at diffraction angles (2θ) of about 6.62, 13.04, 15.44, 16.58, 17.64, 20.88, 23.26, 25.02 and 25.52 (degrees) are provided. | 03-07-2013 |
20130065878 | CELL-FREE PREPARATION OF CARBAPENEMS - Provided herein are cell-free systems for generating carbapenems, e.g., a compound of the Formula (I): | 03-14-2013 |
20150031664 | NOVEL CRYSTAL FORM OF PYRROLIDYLTHIOCARBAPENEM DERIVATIVE - Novel crystals of a pyrrolidylthiocarbapenem derivative having excellent stability is provided. According to the present invention, a crystal of (+)-(4R,5S,6S)-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-3[[(3S,5S)-5-(sulfamoylaminomethyl)pyrrolidin-3-yl]thio]-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid having a diffraction pattern in powder X-ray diffraction having main peaks at diffraction angles (2θ) of about 6.62, 13.04, 15.44, 16.58, 17.64, 20.88, 23.26, 25.02 and 25.52 (degrees) are provided. | 01-29-2015 |