Class / Patent application number | Description | Number of patent applications / Date published |
514100300 | Prodrug utilizing | 55 |
20110118172 | METASTIN DERIVATIVE AND USE THEREOF - The invention provides a stable metastin derivative having excellent biological activities (a cancer metastasis-inhibiting activity, a cancer proliferation-inhibiting activity, a gonadotropin secretion-promoting activity, a sex hormone secretion-promoting activity, etc.). By replacing the constituent amino acids of metastin with specific amino acids in the metastin derivative of the present invention, the blood stability and solubility of the metastin derivative can be more improved, the gel tendency of the metastin derivative can be reduced, the pharmacokinetics of the metastin derivative can be improved, and the metastin derivative can exhibit an excellent cancer metastasis-inhibiting activity and cancer proliferation-inhibiting activity. The metastin derivative can also exhibit a gonadotropin secretion-inhibiting activity, a sex hormone secretion-inhibiting activity, etc. | 05-19-2011 |
20110237493 | DIPEPTIDE LINKED MEDICINAL AGENTS - A non-enzymatically self cleaving dipeptide element is provided that can be linked to known medicinal agents via an amide bond. The dipeptide will spontaneously be cleaved from the medicinal agent under physiological conditions through a reaction driven by chemical instability. Accordingly, the dipeptide element provides a means of linking various compounds to known medicinal agents wherein the compounds are subsequently released from the medicinal agent after a predetermined time of exposure to physiological conditions. For example, the dipeptide can be linked to an active site of a drug to form a prodrug and/or the dipeptide may comprise a depot polymer to sequester an injectable composition comprising the complex at the point of administration. | 09-29-2011 |
20110245147 | Activation of Peptide Prodrugs by HK2 - The invention provides novel peptide prodrugs that contain cleavage sites specifically cleaved by human kallikrein 2 (hK2). These prodrugs are useful for substantially inhibiting the non-specific toxicity of a variety of therapeutic drugs. Upon cleavage of the prodrug by hK2, the therapeutic drugs are activated and exert their toxicity. Methods for treating cell proliferative disorders are also featured in the invention. | 10-06-2011 |
20110257076 | AMIDE BASED INSULIN PRODRUGS - Prodrug formulations of insulin and insulin analogs are provided wherein the insulin peptide has been modified by an amide bond linkage of a dipeptide prodrug element. The prodrugs disclosed herein have extended half lives of at least 10 hours, and more typically greater than 2 hours, 20 hours and less than 70 hours, and are converted to the active form at physiological conditions through a non-enzymatic reaction driven by chemical instability. | 10-20-2011 |
20110275554 | COMPOUNDS - The present invention relates to prodrugs of vascular disrupting agents comprising a vascular disrupting agent (VDA) associated with a MMP proteolytic cleavage site and to the use of such prodrugs in the targeted treatment of cancer. | 11-10-2011 |
20110275555 | COMPOSITIONS CONTAINING DELTA-9-THC-AMINO ACID ESTERS AND PROCESS OF PREPARATION - Compositions of the formulae (I), (II) and (III); where R1, R2 and R3 are residues of amino acids such as, but not limited to, valine, sarcosine, leucine, glutamine, tryptophan, tyrosine, alanine and 4(4-aminophenyl)butyric acid or combination thereof, and salts thereof. Methods of preparation of these compositions and methods of treating any disease condition responsive to THC comprising administration of at least one these compositions in a pharmaceutically acceptable carrier using a pharmaceutically acceptable formulation. | 11-10-2011 |
20110288003 | AMIDE BASED GLUCAGON AND SUPERFAMILY PEPTIDE PRODRUGS - Prodrug formulations of glucagon superfamily peptides are provided wherein the glucagon superfamily peptide has been modified by the linkage of a dipeptide to the glucagon superfamily through an amide bond linkage. The prodrugs disclosed herein have extended half lives and are converted to the active form at physiological conditions through a non-enzymatic reaction driven by chemical instability. | 11-24-2011 |
20110294718 | DIPEPTOID PRODRUGS AND THE USE THEREOF - The present application relates to prodrug derivatives of 2-amino-6-({[2-(4-chlorophenyl)-1,3-thiazol-4-yl]methyl}thio)-4-[4-(2-hydroxyethoxy)phenyl]pyridine-3,5-dicarbonitrile, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially of cardiovascular disorders. | 12-01-2011 |
20110294719 | DIPEPTOID PRODRUGS AND THE USE THEREOF - The present application relates to dipeptide-like prodrug derivatives of 2-amino-6-({[2-(4-chlorophenyl)-1,3-oxazol-4-yl]methyl}sulfanyl)-4-(4-{[2,3-dihydroxypropyl]oxy}phenyl)pyridine-3,5-dicarbonitrile, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially of cardiovascular disorders. | 12-01-2011 |
20120010124 | Cell Penetrating Peptide Conjugates for Delivering of Nucleic Acids into a Cell - The invention provides cell penetrating peptide-nucleic acid conjugates having the formula P-L-N, wherein P is a cell penetrating peptide, N is a nucleic acid, preferably an oligonucleotide and more preferably a siRNA, and L is a hydrophilic polymer, preferably a polyethylene glycol (PEG)-based linker linking P and N together. Compositions, methods of use and methods for producing such conjugates are also disclosed. | 01-12-2012 |
20120010125 | Methods, compounds and pharmaceutical compositions for treating anxiety and mood disorders - Compounds and pharmaceutical compositions containing such compounds having formula I are provided: | 01-12-2012 |
20120015866 | Prodrugs of Heteraromatic Compounds - The present invention relates to prodrugs of parent drug compounds containing heteroaromatic NH groups. | 01-19-2012 |
20120094892 | PRODRUGS - The present invention relates to a prodrug comprising at least one cytostatic agent, wherein said prodrug is cleavable by prostate-specific antigen (PSA), a process for preparing said prodrug and a pharmaceutical composition containing said prodrug in a pharmaceutically effective amount, for use in the treatment of cancer. | 04-19-2012 |
20120108494 | INHIBITORS OF INTRACELLULAR UROKINASE PLASMINOGEN ACTIVATOR AND METHODS OF USE THEREOF - The present invention provides compositions comprising amiloride amino acid and peptide conjugates. Efficient methods are also provided for administering the compositions for treating cancer and for delivering an amiloride conjugate into cancer cells in a subject in need thereof. | 05-03-2012 |
20120135914 | ETOPOSIDE AND DOXORUBICIN CONJUGATES FOR DRUG DELIVERY - The invention relates to improvements in the field of drug delivery. More particularly, the invention relates to polypeptides having a hydrolyzable covalent bond to a therapeutic agent that includes, etoposide, etoposide 4′-dimethylglycine or doxorubicin. These polypeptide conjugates can be used as vectors to transport the podophyllotoxin derivative across the blood brain barrier (BBB) or into particular cell types such as ovary, liver, lung, or kidney. The invention also relates to pharmaceutical compositions that include the compounds of the invention and to uses thereof in methods of treatment. | 05-31-2012 |
20120135915 | TREATMENT OF TRAUMATIC OR DEGENERATIVE NEUROLOGIC, OTOLOGIC, OR OPHTHALMOLOGIC DISEASES WITH TARGETED PROTEASE INHIBITORS - Described herein are compounds and methods for treating or preventing a neurologic, otologic, or ophthalmologic disease in a subject. Also described herein are compounds that can be used as therapeutics. | 05-31-2012 |
20120178666 | PRODRUGS OF GUANFACINE - Prodrugs of guanfacine with amino acids or short peptides, pharmaceutical compositions containing such prodrugs and a method for providing therapeutic benefit in the treatment of ADHD/ODD (attention deficient hyperactivity disorder and oppositional defiance disorder) with guanfacine prodrugs are provided herein. Additionally, methods for minimizing or avoiding the adverse gastrointestinal side effects associated with guanfacine administration, as well as improving the pharmacokinetics of guanfacine are provided herein. | 07-12-2012 |
20120270767 | Tumor Activated Prodrugs - The instant invention provides compositions comprising a prodrug, the prodrug comprising a therapeutically active drug; and a peptide selected from the group consisting of the sequences: Ser-Ser-Lys-Tyr-Gln (SEQ ID NO:1); Gly-Lys-Ser-Gln-Tyr-Gln (SEQ ID NO:2); and Gly-Ser-Ala-Lys-Tyr-Gln (SEQ ID NO:3) wherein the peptide is linked to the therapeutically active drug to inhibit the therapeutic activity of the drug, and wherein the therapeutically active drug is cleaved from the peptide upon proteolysis by an enzyme having a proteolytic activity of prostate specific antigen (PSA). The invention further provides methods of making and using the claimed compositions. | 10-25-2012 |
20120270768 | Tumor Activated Prodrugs - The instant invention provides compositions comprising a prodrug, the prodrug comprising a therapeutically active drug; and a peptide selected from the group consisting of the sequences: Ser-Ser-Lys-Tyr-Gln (SEQ ID NO:1); Gly-Lys-Ser-Gln-Tyr-Gln (SEQ ID NO:2); and Gly-Ser-Ala-Lys-Tyr-Gln (SEQ ID NO:3) wherein the peptide is linked to the therapeutically active drug to inhibit the therapeutic activity of the thug, and wherein the therapeutically active drug is cleaved from the peptide upon proteolysis by an enzyme having a proteolytic activity of prostate specific antigen (PSA). The invention further provides methods of making and using the claimed compositions. | 10-25-2012 |
20120283166 | PEPTIDE PRODRUGS - Provided herein are a novel class of oligopeptides and prodrugs that include amino acid sequences containing cleavage sites for fibroblast activation protein (FAP). Also provided herein are methods of treating FAP related disorders, including cancer. | 11-08-2012 |
20120322721 | DRY GROWTH HORMONE COMPOSITION TRANSIENTLY LINKED TO A POLYMER CARRIER - The present invention relates to dry compositions of rhGH polymer prodrug containing a lyoprotectant and, optionally, one or more than one excipient. Such compositions are stable for at least 1 year, when stored at 2-8° C. The invention further relates to methods of manufacturing said compositions, containers comprising such composition as well as a kit of parts. | 12-20-2012 |
20130130967 | Method for Uses of Protein Precursors as Prodrugs - The present invention provides compositions useful as prodrugs and methods for making the same. The compositions include a fusion protein having a first delivery domain and a second protein precursor domain linked together via a linker sequence. The delivery domain is a protein capable of facilitating entry to a target cells via the endocytotic pathway, such as transferrin. The protein precursor is a prohormone or a profactor, such as proinsulin. Methods of this invention include the steps of selecting a protein suitable as the delivery domain, constructing a vector to encode the fusion protein, and expressing the fusion protein in a suitable expression host. Also disclosed is a method for targeted-delivery of prodrugs to livers and a method of reducing hepatic glucose production. | 05-23-2013 |
20130150281 | POLYMERIC PRODRUG WITH SELF-IMMOLATIVE LINKER - A cascade carrier linked prodrug is described comprising a biologically active moiety and a masking group having at least one nucleophile and being distinct from the carrier. | 06-13-2013 |
20130196897 | Glucosamine Pro-drug - To develop glucosamine (GlcN) pro-drugs with properties superior to the presently available GlcN products, we have synthesized derivatives with improved pharmaceutical properties. The synthesized derivatives include peptide-GlcN ester and amide conjugates where the peptide portion consists of one or more amino acids. One such compound is (5-amino-3,4,6-trihydroxyoxan-2-yl)methyl 2-(2-aminoacetamido)-3-methylbutanoate or glycine-valine-COO-GlcN (GV-GlcN).7 | 08-01-2013 |
20130203647 | DELIVERY OF HYDROPHILIC PEPTIDES - A composition comprises nanofibres for the delivery of a peptide across the blood brain barrier in a method of therapy of the human or animal body, wherein the nanofibres comprise a peptide conjugated to a lipophilic group. Further, a compound comprises a Dalargin or a derivative having one or more substituted, deleted or inserted aminoacyl units, and, conjugated to an aminoacyl group preferably via a side chain, a lipophilic group, optionally via a linker. | 08-08-2013 |
20130210702 | Vitamin E Conjugates, and Their Uses as Antioxidants and Prodrug Delivery Vehicles - Tocopherol conjugates are disclosed that are useful as antioxidants or as pro-drug delivery vehicles. The conjugates are amphiphilic, and tend to localize at the interface between water domains and lipid domains. A prototype embodiment disclosed is an alpha tocopherol-linker-carnosine conjugate that has been designated VECAR. | 08-15-2013 |
20130303435 | Smart Pro-Drugs of Serine Protease Inhibitors - The present invention relates to prodrugs of protease inhibitors, such as inhibitors of the proteosome, DPP IV, FAPα and the like. These“pro-inhibitors” are activated, i.e., cleaved, by an “activated protease” to release an active inhibitor moiety in proximity to a “target protease”. The identity of activating protease and target protease can be the same (such as pro-inhibitors being referred to as “Target-Activated Smart Protease Inhibitors” or “TASPI”) or different (e.g., “Target-Directed Smart Protease Inhibitors” or “TDSPI”). After activation of the pro-inhibitor, the active inhibitor moiety can self-inactivate by, e.g., intramolecular-cyclization or cis-trans isomerization. | 11-14-2013 |
20140051623 | Bisphosphonate-Prodrugs - The present invention relates to a prodrug, comprising a pharmaceutically and/or diagnostically active compound, and one or more bisphosphonate groups, to a process for producing such a prodrug, and to a pharmaceutical composition comprising said prodrug, to be used for the treatment of bone-related disorders such as bone cancer. | 02-20-2014 |
20140087991 | PEPTIDE PRODRUGS - Provided herein are a novel class of oligopeptides and prodrugs that include amino acid sequences containing cleavage sites for fibroblast activation protein (FAP). Also provided herein are methods of treating FAP related disorders, including cancer. | 03-27-2014 |
20140087992 | BIS(FLUOROALKYL)-1,4-BENZODIAZEPINONE COMPOUNDS AND PRODRUGS THEREOF - Disclosed are compounds of Formula (I) and/or salts thereof: | 03-27-2014 |
20140100154 | Prodrugs of Peptide Epoxy Ketone Protease Inhibitors - This disclosure features compounds that are useful as pro-drugs of epoxy ketone protease inhibitors. | 04-10-2014 |
20140121152 | Active Agent Prodrugs with Heterocyclic Linkers - The embodiments provide prodrug compounds of Formulae I-XVII. The present disclosure also provides compositions, and their methods of use, where the compositions comprise a prodrug compound of Formulae I-XVII that provides controlled release of an active agent. Such compositions can optionally provide a trypsin inhibitor that interacts with the enzyme that mediates the controlled release of an active agent from the prodrug so as to attenuate enzymatic cleavage of the prodrug. | 05-01-2014 |
20140148377 | Emetine Derivatives, Prodrugs Containing Same, And Methods Of Treating Conditions Using Same - Compounds are provided herein which are emetine derivatives that can be used as prodrugs which selectively undergo activation to release emetine in specific cellular conditions. In one aspect, a blocking group is incorporated onto the emetine molecule by the derivization of the N2′-position with moieties that can be selectively removed by hydrolysis in the cancer/tumor microenvironment. Such compounds are less cytotoxic than emetine and are substantially inactive in non-cancerous cells. In one aspect, the compounds described herein can be used for the treatment of metastatic and non-metastatic cancers, including, for example, breast cancer, prostate cancer, lung cancer, and leukemia. | 05-29-2014 |
20140162935 | Compositions Comprising Enzyme-Cleavable Oxycodone Prodrug - The embodiments provide Compound KC-8, N-1-[3-(oxycodone-6-enol-carbonyl-methyl-amino)-2,2-dimethyl-propylamine]-arginine-glycine-malonic acid, or acceptable salts, solvates, and hydrates thereof. The present disclosure also provides compositions, and their methods of use, where the compositions comprise a prodrug, Compound KC-8, that provides controlled release of oxycodone. Such compositions can optionally provide a trypsin inhibitor that interacts with the enzyme that mediates the controlled release of oxycodone from the prodrug so as to attenuate enzymatic cleavage of the prodrug. | 06-12-2014 |
20140171357 | VANCOMYCIN DERIVATIVES - The invention features vancomycin class compounds modified to be suitable for oral delivery or to possess increased antimicrobial potency, formulations for the oral administration of vancomycin class compounds, and synthetic methods for making vancomycin class compounds. | 06-19-2014 |
20140179592 | Compounds - The present invention relates to compounds, and pharmaceutically acceptable salts thereof, comprising a vascular disrupting agent (VDA) associated and a MMP proteolytic cleavage site. The compounds are useful in the treatment of cancer. | 06-26-2014 |
20140213504 | Cyclodextrin-Based Polymers for Therapeutic Delivery - Described herein are CDP-therapeutic peptide conjugates, therapeutic delivery systems comprising CDP-therapeutic peptide conjugates, compositions comprising CDP-therapeutic peptide conjugates, dosage forms comprising CDP-therapeutic peptide conjugates, and kits comprising CDP-therapeutic peptide conjugates. Also disclosed are methods of using (e.g., to treat a disorder) the CDP-therapeutic peptide conjugates, therapeutic delivery systems comprising CDP-therapeutic peptide conjugates, compositions comprising CDP-therapeutic peptide conjugates, dosage forms comprising CDP-therapeutic peptide conjugates, and kits comprising CDP-therapeutic peptide conjugates. | 07-31-2014 |
20140243254 | Polymeric Hyperbranched Carrier-Linked Prodrugs - The present invention relates to water-soluble carrier-linked prodrugs of formula (I), wherein POL is a polymeric moiety, each Hyp is independently a hyperbranched moiety, each moiety SP is independently a spacer moiety, each L is independently a reversible prodrug linker moiety, m is 0 or 1, each n is independently an integer from 2 to 200 and each x is independently 0 or 1. It further relates to pharmaceutical compositions comprising said water-soluble carrier-linked prodrugs and methods of treatment. | 08-28-2014 |
20140287984 | POLYETHYLENE GLYCOL BASED PRODRUG OF ADRENOMEDULLIN AND USE THEREOF - The invention relates to novel polyethylene glycol (PEG) based prodrug of Adrenomedullin, to processes for preparation thereof, to the use thereof for treatment and/or prevention of diseases, and to the use thereof for producing medicaments for treatment and/or prevention of diseases, especially of cardiovascular, edematous and/or inflammatory disorders. | 09-25-2014 |
20140315784 | Binding Inhibitors of the Beta. Transducin Repeat-Containing Protein - The present invention relates to compounds which bind to Beta Trans-ducin repeat-containing protein (PTrCP), and modulate the activity of 13TrCP. In particular, the invention relates to compounds which demonstrate optimised binding to PTrCP. The invention also relates to pharmaceutical compositions comprising such compounds and the use of such compounds as medicaments, specifically for the treatment of disorders associated with aberrant protein degradation, such as cancer. The preferred binding inhibitors are peptides derived from the motive DSGXXS, e.g. DEGFWE, DDGFWD and Succinyl-EGFWE. | 10-23-2014 |
20150045281 | GLP-1 PRODRUGS - The invention relates to a GLP-1 prodrug of the general formula I: R1-(NHXaa1)-Xaa2-(OHis)-(GLP-1 peptide) (Formula I), wherein GLP-1 peptide is GLP-1(8-37) (SEQ ID NO: 1) or an analogue thereof having a maximum of nine amino acid changes as compared to GLP-1(8-37), R1 is lower alkyl, (NHXaa1) is an amino acid, Xaa2 is an amino acid, and (OHis) is a radical of imidazole-lactic acid; or a pharmaceutically acceptable salt, amide, or ester of the prodrug. The invention also relates to specific GLP-1 parent drugs of the general formula II: (HOHis)-(GLP-1 peptide) (Formula II), as well as specific intermediate products. The invention furthermore relates to a method of achieving release in vivo of an active and stabilised GLP-1 parent drug of the general formula II: (HOHis)-(GLP-1 peptide), by administering a GLP-1 prodrug; as well as to such GLP-1 prodrug, and such GLP-1 parent drug, respectively, for use as a medicament, in particular for use in the treatment and/or prevention of all forms of diabetes and related diseases. The prodrug may be used to alter the PK and/or absorption profile of the drug, for example to a desirable bell-shaped curve. The parent drug has a good biological activity, and is stabilised against degradation by DPP-IV. | 02-12-2015 |
20150045282 | COMPOSITIONS CONTAINING DELTA-9-THC-AMINO ACID ESTERS AND PROCESS OF PREPARATION - Suppository, hot melt and ophthalmic formulations containing amino esters of the formulae (I), (II) and (III), where R1, R2 and R3 are residues of amino acids such as, but not limited to, valine, sarcosine, leucine, glutamine, tryptophan, tyrosine, alanine and 4(4-aminophenyl)butyric acid or combination thereof, and salts thereof. | 02-12-2015 |
20150133364 | DIPEPTOID PRODRUGS AND THEIR USE - The present application relates to prodrug derivatives of 2-amino-6-({[2-(4-chlorophenyl)-1,3-thiazol-4-yl]methyl}thio)-4-[4-(2-hydroxyethoxy)phenyl]pyridine-3,5-dicarbonitrile, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially of cardiovascular disorders. | 05-14-2015 |
20150290292 | Treatment of Depression and PTSD - Depression and PTSD are treated by administration of hCG, or an hCG analog, or a prodrug or metabolite of hCG or an hCG analog, in an amount equivalent to a subcutaneous dose of 50-200 IU, preferably 120-170 IU, more preferably 140-160 IU, of hCG per day. | 10-15-2015 |
20150297735 | CONJUGATES FOR TREATING DISEASES CAUSED BY PSMA EXPRESSING CELLS - The invention described herein pertains to the diagnosis, imaging, and/or treatment of pathogenic cell populations. In particular, the invention described herein pertains to the diagnosis, imaging, and/or treatment of diseases caused by PSMA expressing cells, such as prostate cancer cells, using compounds capable of targeting PSMA expressing cells. | 10-22-2015 |
20150315226 | DISULFIDE MASKED PRODRUG COMPOSITIONS AND METHODS - The present invention relates to disulfide masked prodrug compounds, compositions and methods that are amenable to bioactivation by a reducing agent such as glutathione. Such disulfide based compounds, compositions, and methods can be useful, for example, in providing novel prodrugs for use as therapeutics. | 11-05-2015 |
20150343083 | PEPTIDE-DRUG CONJUGATES - Peptide-drug conjugates comprising p-aminobenzyl carbamoyl or p-aminobenzolyl carbonate self-immolating linkers are disclosed. The peptide-drug conjugates comprise a peptide moiety that can be cleaved by cellular proteases, bound to the self-immolating linker, which linker is bound to a cytotoxic drug moiety. Upon cleavage of the peptide moiety, the linker self-immolates, releasing the cytotoxic drug in active form. Dimeric structures of the peptide drug conjugates comprising two molecules of cytotoxic drug per conjugate are also disclosed. | 12-03-2015 |
20160002291 | Active Agent Prodrugs with Heterocyclic Linkers - The embodiments provide prodrug compounds of Formulae I-XVII. The present disclosure also provides compositions, and their methods of use, where the compositions comprise a prodrug compound of Formulae I-XVII that provides controlled release of an active agent. Such compositions can optionally provide a trypsin inhibitor that interacts with the enzyme that mediates the controlled release of an active agent from the prodrug so as to attenuate enzymatic cleavage of the prodrug. | 01-07-2016 |
20160009713 | Prodrugs of Heteraromatic Compounds | 01-14-2016 |
20160058873 | Cyclodextrin-Based Polymers for Therapeutic Delivery - Described herein are CDP-therapeutic peptide conjugates, therapeutic delivery systems comprising CDP-therapeutic peptide conjugates, compositions comprising CDP-therapeutic peptide conjugates, dosage forms comprising CDP-therapeutic peptide conjugates, and kits comprising CDP-therapeutic peptide conjugates. Also disclosed are methods of using (e.g., to treat a disorder) the CDP-therapeutic peptide conjugates, therapeutic delivery systems comprising CDP-therapeutic peptide conjugates, compositions comprising CDP-therapeutic peptide conjugates, dosage forms comprising CDP-therapeutic peptide conjugates, and kits comprising CDP-therapeutic peptide conjugates. | 03-03-2016 |
20160058881 | PRODRUGS WITH PROLONGED ACTION - A prodrug derivative of a bioactive peptide (or polypeptide) is provided that exhibits prolonged half-life in serum and prolonged action in vivo, compared to the parent peptide or polypeptide. In some embodiments, the peptide is selected from the group consisting of glucagon, exendin-4, GLP-1, GLP-2, GIP, vasoactive intestinal peptide (VIP), Pituitary adenylate cyclase-activating polypeptide 27 (PACAP-27), peptide histidine methionine (PHM), oxyntomodulin, secretin, osteocalcin, growth hormone releasing hormone, as well as analogs, derivatives and conjugates. | 03-03-2016 |
20160115147 | PRO-DRUG COMPOUNDS - The present invention provides neuronal gap junction blocking compounds according to formula (I) or a hydrate, solvate, or pharmaceutically acceptable salt thereof: | 04-28-2016 |
20160144050 | PRODRUGS ACTIVATED BY CASPASE - Described are prodrug conjugates that release a chemotherapeutic agent upon activation by caspase, and methods using such prodrug conjugates to induce apoptosis, amplify apoptosis, and treat cancer. | 05-26-2016 |
20160193347 | MULTI-TARGETED UBENIMEX PRODRUG DERIVATIVE AND PREPARATION METHOD AND USE THEREOF | 07-07-2016 |
20170232023 | PEPTIDE-DRUG CONJUGATES | 08-17-2017 |
20100317580 | CONJUGATES OF DISORAZOLES AND THEIR DERIVATIVES WITH CELL-BINDING MOLECULES, NOVEL DISORAZOLE DERIVATIVES, PROCESSES OF MANUFACTURING AND USES THEREOF - The present invention provides conjugates of disorazoles and their derivatives with cell-binding molecules, such as peptides, proteins, hormones, blood proteins and antibodies. The present invention further provides novel disorazole derivatives and processes of manufacturing such conjugates and disorazole derivatives. These compounds can be used as medicaments for the treatment of physiological and/or pathophysiological conditions in mammals, in particular for the treatment of various tumors. | 12-16-2010 |
20100323963 | CONJUGATES OF DISORAZOLES AND THEIR DERIVATIVES WITH CELL-BINDING MOLECULES, NOVEL DISORAZOLE DERIVATIVES, PROCESSES OF MANUFACTURING AND USES THEREOF - The present invention provides conjugates of disorazoles and their derivatives with cell-binding molecules, such as peptides, proteins, hormones, blood proteins and antibodies. The present invention further provides novel disorazole derivatives and processes of manufacturing such conjugates and disorazole derivatives. These compounds can be used as medicaments for the treatment of physiological and/or pathophysiological conditions in mammals, in particular for the treatment of various tumors. | 12-23-2010 |
20110003748 | Method of treatment and compositions of D-chiro inositol and phosphates thereof - The present invention relates to the use of D-chiroinositol or a phosphate thereof in combination with folate for the reduction or prevention of congenital deformations such as anorectal malformations, neural tube defects, cleft-lip, cleft palate, and other birth defects. The invention further relates to the use of D-chiroinositol or a phosphate thereof in quieting or preventing the sensitivity of breast tissue to estrogenic, progestogenic, and or anti-androgenic insult, whether from environmental, dietary, or medicinal sources. Co-therapies as well as combination products of D-chiro-inositol (or a phosphate thereof) with at least one of (a) a folate source and (b) one or more of an estrogenic substance, a progestogenic substance, and/or an antiandrogenic substance are also claimed. | 01-06-2011 |
20110178012 | USE OF HUMAN CHORIONIC GONADOTROPIN ORALLY FOR THE TREATMENT OF OVERWEIGHT (OBESITY) ASSOCIATED WITH HIGH BLOOD TENSION, NON-INSULIN-DEPENDANT DIABETES, HYPERCHOLESTEROLEMIA, DYSLIPIDEMIAS AND LIPODYSTROPHY. - Human chorionic gonadotropin administered by intramuscular route is traditionally used for the treatment of sterility and cryptorchidism. After numerous tests performed, a compound to be administered orally—sublingual—has been developed with such drug to treat patients suffering from overweight associated with high blood tension, non-insulin-dependant diabetes, hypercholesterolemia, dyslipidemias and lipodystrophy. It was determined that hCG acts satisfactorily upon high blood tension, non-insulin-dependant diabetes, hypercholesterolemia, dyslipidemias and lipodystrophy. | 07-21-2011 |
20120058945 | NEUROPROTECTIVE IRON CHELATORS AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM - Novel iron chelators exhibiting neuroprotective and good transport properties are useful in iron chelation therapy for treatment of a disease, disorder or condition associated with iron overload and oxidative stress, e.g., a neurodegenerative or cerebrovascular disease or disorder, a neoplastic disease, hemochromatosis, thalassemia, a cardiovascular disease, diabetes, an inflammatory disorder, anthracycline cardiotoxicity, a viral infection, a protozoal infection, a yeast infection, retarding aging, and prevention and/or treatment of skin aging and skin protection against sunlight and/or UV light. The iron chelator function is provided by a 8-hydroxyquinoline, a hydroxypyridinone or a hydroxamate moiety. The neuroprotective function is imparted to the compound, e.g., by a neuroprotective peptide. A combined antiapoptotic and neuroprotective function is provided by a propargyl group. | 03-08-2012 |
20120071408 | FORMULATIONS FOR ACHIEVING WEIGHT LOSS - A formulation of human chorionic gonadotropin (HCG) for promoting weight loss comprising reconstituted HCG in an amount sufficient to promote weight loss; at least one vitamin selected from the group consisting of: vitamin B1, vitamin B2, vitamin B3, vitamin B5, vitamin B6, vitamin B7, vitamin B9, and vitamin B12; and at least one dietary supplement selected from the group consisting of: an amino acid, inositol, choline chloride, and L-carnitine. | 03-22-2012 |
20120088723 | SELECTIVE EP4 RECEPTOR AGONISTIC SUBSTANCE FOR TREATMENT OF CANCER - This invention provides a medicament for the treatment of cancer, which cause a reduction of cancer. This invention relates to use of a compound which has inhibitory activities against prostaglandin E2 receptor (EP4 receptor) and is represented by the following general formula (I), (II), (III), or (IV), or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt for the manufacture of a medicament for the treatment of cancer. The invention relates to a method for treatment of cancer comprising administering the compound or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt to humans or animals. The compound or a pharmaceutically acceptable salt thereof, or the pharmaceutical composition may be used in combination with one or more second active agents. | 04-12-2012 |
20120202742 | METHODS AND DEVICES FOR THE SUSTAINED RELEASE OF MULTIPLE DRUGS - The invention relates to an drug delivery device and a method for delivering multiple drugs over a prolonged period of time. The drug delivery device has two or more unitary segments comprising a drug-permeable polymeric substance, wherein at least one of the segments further comprises a pharmaceutically active agent. The invention also relates to a method for the treatment of a benign ovarian secretory disorder in a female mammal, a method of contraception, and a method of relieving the symptoms associated with menopausal, perimenopausal and post-menopausal periods in a woman. | 08-09-2012 |
20120283187 | CONTROLLED RELEASE COMPOSITION AND METHOD OF PRODUCING THE SAME - A controlled release composition containing a physiologically active substance in high content, suppressing the initial excess release, and achieving a stable release speed over a long period of time is provided. A controlled release composition comprising (1) a physiologically active substance or salt thereof in an amount of about 14% (w/w) to about 24% (w/w) based on the total composition weight, (2) hydroxynaphthoic acid selected from the group consisting of 3-hydroxy-2-naphthoic acid and 1-hydroxy-2-naphthoic acid or salt thereof, and (3) a lactic acid polymer or salt thereof having a weight-average molecular weight of 15000 to 50000 in which the content of polymers having molecular weights of 5000 or less is about 5% by weight or less, wherein the molar ratio of said hydroxynaphthoic acid or salt thereof to said physiologically active substance or salt thereof is from 3:4 to 4:3. | 11-08-2012 |
20120295848 | SUSTAINED-RELEASE COMPOSITION AND PROCESS FOR PRODUCING THE SAME - Present invention is to provide a sustained-release composition which contains a physiologically active substance in high content even when gelatin is not included, and suppresses its initial excessive release and, thus, can achieve a stable release rate over about one month. A sustained-release composition containing a lactic acid-glycolic acid polymer having a ratio or weight average molecular weight and number average molecular weight of about 1.90 or lower, or a salt thereof, and a physiologically active substance. | 11-22-2012 |
20130012437 | LYTIC PEPTIDES HAVING ANTI-PROLIFERATIVE ACTIVITY AGAINST PROSTATE CANCER CELLS - Lytic peptides, including fusion peptides of lytic peptides conjugated with luteinizing hormone-releasing hormone or modified versions thereof to target luteinizing hormone-releasing hormone receptors, are disclosed. The lytic peptides show anti-proliferative activity against human prostate cancer cell lines, but are nontoxic to normal primary human prostate epithelial cells or to bone marrow stromal cells in co-culture. The lytic peptides have specificity for and anti-proliferative activity against prostate cancer tumor cells, and low toxicity for normal prostate cells, making the peptides useful in therapies for prostate cancer. | 01-10-2013 |
20130157951 | Pharmaceutical Composition Containing Goserelin for In-Situ Implant - The present invention provides a pharmaceutical composition capable of forming in-situ implant comprising goserelin or its pharmaceutically acceptable salts thereof, biodegradable polymer and a biocompatible organic solvent wherein the biocompatible organic solvent is miscible to dispersible in aqueous medium or body fluid. The present invention further provides a process for the preparation of pharmaceutical composition capable of forming in-situ implant. A kit containing composition for in-situ implant is provided comprising a first vial comprising a composition comprising a biodegradable polymer and a biocompatible organic solvent; wherein the biocompatible organic solvent is miscible to dispersible in aqueous medium or body fluid; and a second vial comprising goserelin acetate. | 06-20-2013 |
20130165377 | PREVENTION OF MOLECULAR WEIGHT REDUCTION OF THE POLYMER, IMPURITY FORMATION AND GELLING IN POLYMER COMPOSITIONS - Polymer and drug containing compositions and method of preparing such compositions are disclosed. The dispersed phase formulation has a polymer, a pharmaceutically or biologically active agent and a small fraction of low pKa acid additive. Stable, filter sterilizable, non-gelling solutions containing GnRH analogues at least at levels typically used in sustained release formulations and a method of increasing solubility of a high level of a GnRH analogue or a freeze-dried antgonist of GnRH in a polymer containing solution are also disclosed. The amount of the acid additive in the polymer solution is such that it is sufficient to increase the solubility of the high level of the GnRH analogue in the polymer solution without affecting the release characteristics of the microspheres prepared therefrom. | 06-27-2013 |
20130252890 | 6,7-DIHYDRO-5H-BENZO[7]ANNULENE DERIVATIVES, PROCESS FOR PREPARATION THEREOF, PHARMACEUTICAL PREPARATIONS COMPRISING THEM, AND THE USE THEREOF FOR PRODUCTION OF MEDICAMENTS - The invention relates to selective oestrogen receptor modulators (SERM) and methods of production thereof, use thereof for the treatment and/or prophylaxis of diseases and use thereof for the production of medicinal products for the treatment and/or prophylaxis of diseases, in particular of bleeding disorders, osteoporosis, endometriosis, myomata, hormone-dependent tumours, for hormone replacement therapy and for contraception. | 09-26-2013 |
20130274192 | MICROPARTICLES CONTAINING PHYSIOLOGICALLY ACTIVE PEPTIDE, METHOD FOR PREPARING THE SAME, AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME - Disclosed are microparticles containing physiologically active peptides, a method for preparing the same, and a pharmaceutical composition comprising the same. | 10-17-2013 |
20150133382 | Method of Testing for Endometriosis and Treatment Therefor - The present invention relates to novel genetic markers associated with endometriosis and risk of developing endometriosis, and methods and materials for determining whether a human subject has endometriosis or is at risk of developing endometriosis and the use of such risk information in selectively administering a treatment that at least partially prevents or compensates for an endometriosis related symptom. | 05-14-2015 |
20150297726 | SUSTAINED-RELEASE LIPID PRE-CONCENTRATE OF GNRH ANALOGUES AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME - Disclosed is a pharmaceutical composition, comprising: a) at least one sorbitan unsaturated fatty acid ester having a polar head with at least two or more —OH (hydroxyl) groups; b) at least one phospholipid; c) at least one liquid crystal hardener which is free of an ionizable group and has a triacyl group with 15 to 40 carbon atoms or a carbon ring structure in a hydrophobic moiety; and d) at least one GnRH (gonadotropin-releasing hormone) analogue as a pharmacologically active substance, wherein said lipid pre-concentrate exists as a liquid phase in absence of aqueous fluid and forms into a liquid crystal in presence of aqueous fluid. The pharmaceutical composition is configured to enhance the sustained release of the pharmacologically active substance GnRH analogue. | 10-22-2015 |
20150335714 | USE OF HUMAN CHORIONIC GONADOTROPIN TO INHIBIT DEVELOPMENT OR MINIMIZE SEVERITY OF CEREBRAL PALSY AND/OR ITS CO-MORBIDITIES - The invention described herein relates generally to the use of human chorionic gonadotropin (hCG) or a subunit or variant thereof, in neurodevelopmental disorders. In particular, the present invention relates to the use of hCG and related compounds as described herein for treating or reducing the likelihood of cerebral palsy and its co-morbidities in a patient or subject including a neonate, an infant or a child. | 11-26-2015 |
20150342958 | METHODS FOR TREATING GI TRACT DISORDERS - Provided herein are methods, compositions, and kits for the treatment of an enteric nervous system disorder. Such methods may comprise administering to a subject an effective amount of a phenothiazine compound, a peripherally restricted dopamine decarboxylase inhibitor, and/or a peripherally restricted dopamine D2 receptor antagonist that does not substantially inhibit hERG channels. | 12-03-2015 |
20160074320 | PHARMACEUTICAL COMPOSTIONS COMPRISING KISSPEPTIN OR DERIVATIVES THEREOF - The present invention relates to pharmaceutical compositions comprising a peptide that stimulates the release of gonadotropins and sexual steroids. More specifically, the present invention provides pharmaceutical compositions comprising kisspeptin, preferably in the kp-10 form, or derivatives thereof, for use in ovulation cycle inducing and/or infertility treatment programs. The formulations according to the present invention belong to two main groups: injectable solutions and implantable formulations. The injectable solutions according to the present invention can be divided into immediate release solutions and prolonged action solutions. The implantable formulations according to the present invention can be prepared using an RTV silicone elastomer, a rapid vulcanization silicone elastomer or a rapid vulcanization silicone elastomer with a release modulator. | 03-17-2016 |
20160145300 | ARTIFICIAL DECAPEPTIDE, MEDICATION AND METHOD OF INDUCING BREEDING OF CRUSTACEANS - The present invention provides an artificial decapeptide for inducing the development of gonad in crustacean, a medication including the artificial decapeptide and a method of inducing the gonad development of crustacean. The method includes administrating an effective amount of an artificial decapeptide to a crustacean, thereby promoting gonad development of crustaceans, wherein the artificial decapeptide includes a sequence set forth in SEQ ID NO: 2. | 05-26-2016 |
20160375090 | METHOD AND COMPOSITION FOR SYNCHRONIZING TIME OF INSEMINATION IN GILTS - Methods and compositions for synchronizing the time of insemination in gilts are provided. More particularly, methods and compositions for synchronizing the time of insemination in gilts using a gonadotropin-releasing hormone and a hormone for synchronizing estrus are provided. | 12-29-2016 |