Entries |
Document | Title | Date |
20080242691 | Aqueous Solution Preparation Containing Camptothecins - An aqueous solution preparation containing camptothecins which does not require heating in its production, and wherein camptothecins have been solubilized in a stable manner is provided. | 10-02-2008 |
20080255175 | Anti-cancer agents, compositions and methods of treating cancers - Compounds and compositions useful in methods for treating cancer in mammals. The compounds of the invention are of the formula: | 10-16-2008 |
20080262014 | Use of Camptothecin Derivatives for the Treatment of Proliferative Diseases in a Fixed Dosing Regimen - Topoisomerase I inhibitors are administered for the treatment of proliferative diseases according to a once every three day fixed dosing regimens. Furthermore, the invention provides the use of topoisomerase inhibitors to manufacture a medicament which can be used in a fixed dose treatment regimen. | 10-23-2008 |
20080280937 | Ligand Conjugates of Vinca Alkaloids, Analogs, and Derivatives - Described herein are compounds, pharmaceutical compositions and methods for treating pathogenic cell populations in a patient. The compounds described herein include conjugates of cytotoxic drugs and vitamin receptor binding ligands. The conjugates also include a linker that is formed from one or more spacer linkers, heteroatom linkers, and releasable linkers. | 11-13-2008 |
20080312265 | Treatment of Drug-Resistant Tumors - A subclass of camptothecin derivatives is disclosed to be useful for the preparation of a medicament for the treatment of drug-resistant tumors and/or for the administration to patients who show polymorphisms in the gene coding for DNA topoisomerase I. | 12-18-2008 |
20090012111 | Crystalline polymorph of 7-ethyl-10-hydroxycamptothecin - A crystalline polymorph of 7-ethyl-10-hydroxycamptothecin exhibiting an X-ray diffraction pattern having peaks at 10.9±0.2, 13.2±0.2, 23.9±0.2, and 26.1±0.2 2-theta degree. | 01-08-2009 |
20090062323 | DEUTERIUM-ENRICHED IRINOTECAN - The present application describes deuterium-enriched irinotecan, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 03-05-2009 |
20090076054 | TEST METHOD FOR ENDOTOXIN - An object of the present invention is to provide a method capable of detecting and quantifying endotoxin in a sample in which endotoxin derived from gram-negative bacteria cannot be accurately detected or quantified by the method described in Commentary of the Japanese Pharmacopoeia Fourteenth Edition, Hirokawa Publishing Co. 2001 B-63. It has been found that the above object can be achieved by performing an endotoxin test using a lysate reagent in which the lysate reagent is added into a sample in the presence of albumin and/or globulin. | 03-19-2009 |
20090076055 | DEUTERIUM-ENRICHED VINFLUNINE - The present application describes deuterium-enriched vinflunine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 03-19-2009 |
20090076056 | DEUTERIUM-ENRICHED TOPOTECAN - The present application describes deuterium-enriched topotecan, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 03-19-2009 |
20090099224 | C7- substituted camptothecin analogs - The novel C7-modified camptothecin analogs, and pharmaceutically-acceptable salts thereof, of the present invention: (i) possess potent antitumor activity (i.e., in nanomolar or subnanomolar concentrations) for inhibiting the growth of human and animal tumor cells in vitro; (ii) are potent inhibition of Topoisomerase I; (iii) lack of susceptibility to MDR/MRP drug resistance; (iv) require no metabolic drug activation: (v) lack glucuronidation of the A-ring or B-ring; (vi) reduce drug-binding affinity to plasma proteins; (vii) maintain lactone stability; (viii) maintain drug potency; and (ix) possess a low molecular weight (e.g., MW<600). | 04-16-2009 |
20090111845 | Hydrated Crystalline Esters Of Camptothecin - Hydrated crystalline camptothecin esters, such as crystalline aliphatic ester hydrates of camptothecin, pharmaceutical compositions containing crystalline aliphatic ester hydrates of camptothecin, methods of treating a cancer or malignant tumor using the crystalline camptothecin ester hydrates and methods of making the same are described. | 04-30-2009 |
20090137619 | Method for preventing and/or treating peripheral neuropathies induced by the administration of an anticancer agent - A method for preventing and/or treating peripheral neuropathies induced by the administration of an anticancer agent of the family of platin compounds, taxanes, epothilone class, vinca alkaloids, said method comprising the administration in a co-ordinated manner to a subject suffering from said peripheral neuropathies, or expected to suffer from said peripheral neuropathies, an effective amount of acetyl L-carnitine or of a pharmaceutically acceptable salt thereof. In case of prevention, acetyl L-carnitine is administered to a subject, in view of the need of a treatment with an anticancer agent, immediately before or immediately after surgical removal of the tumor, but in any case before the administration of the anticancer agent. Acetyl L-carnitine can enhance the supportive effect of physiological NGF during chemotherapy-induced neuropathy, thus avoiding the problem of the local and general side effects of the exogenous administration of NGF which are a major problem of this neuroprotective strategy. | 05-28-2009 |
20090156629 | INDENOISOQUINOLINE-RELEASABLE POLYMER CONJUGATES - The present invention provides releasably-linked indenoisoquinoline polymer conjugates. Methods of making the conjugates and methods of treating mammals using the same are also disclosed. | 06-18-2009 |
20090192184 | Crystalline Polymorphs of Topotecan Hydrochloride and Methods for the Preparation Thereof - The invention relates to two novel crystalline form of Topotecan hydrochloride (Ia) | 07-30-2009 |
20090221622 | TOPOTECAN READY TO USE SOLUTIONS - Aqueous-based, ready to use topotecan-containing formulations for parenteral use having extended stability are disclosed. The formulations are surprisingly free of precipitated degradation products such as 10-hydroxycamptothecin (10-HCPT) after periods of up to 1 year or greater. | 09-03-2009 |
20090239893 | STEREOSELECTIVE PROCESS AND CRYSTALLINE FORMS OF A CAMPTOTHECIN - A stereoselective process for preparing 7-[(E)-t-butyloxyiminomethyl]-camptothecin (also known as gimatecan) is herein disclosed. With the addition of further dissolution and precipitation steps carried out in appropriate different solvent mixtures, four new crystalline forms of gimatecan are also obtainable by using the same stereoselective process. | 09-24-2009 |
20090247563 | Novel Processes for the Production of Useful Intermediates - The present application relates to a new process for the asymmetric production of 3-(pyridin-4-yl)-3-hydroxy-pentanoic acid derivatives, which are useful intermediates in the manufacture of compounds that are known to show antiproliferative activity. | 10-01-2009 |
20090247564 | Crystalline Form of Vinflunine Ditartrate - The present invention relates to a novel crystalline form of vinflunine, to a process for preparing it, and to its uses in the therapeutic field, in particular for treating cancer. | 10-01-2009 |
20090275603 | NF- kB Inhibitors And Uses Thereof - A new class of imidazolines as 4-position esters with very potent anti-inflammatory as well as antimicrobial activity is described. The synthesis of these imidazolines includes a multicomponent reaction applicable to a combinatorial synthetic approach. The combination of these two key characteristics provides an effective therapeutic drug in the treatment of septic shock as well as many other inflammatory (arthritis and asthma) and infectious disorders. The use of this novel class of non-steroidal agents as anti-inflammatory agents (for the treatment of asthma, etc.), antibacterial agents, and antiseptic agents is described. The compounds are also useful in the treatment of tumors (such as cancers). The imidazolines are potent inhibitors of the transcription factor NF-κB as well as potent activity against the Gram (+) bacterium. The compositions are also useful for treating autoimmune diseases and for inhibiting rejection of organ and tissue transplants. | 11-05-2009 |
20090318487 | Methods for detection of promoter polymorphism in a UGT gene promoter - The present invention is directed to methods for detecting the presence of genetic polymorphisms that correlate with altered gene expression. More specifically, the present invention is directed to methods for detecting the genetic polymorphisms located in the UGT1A1 promoter. The invention also provides methods for optimizing drug dosages based upon the presence of the polymorphisms. The invention further provides methods of predicting sensitivity to xenobiotics and diagnostic kits for detecting genetic polymorphisms. | 12-24-2009 |
20090325996 | CAMPTOTHECIN DERIVATIVES AND THEIR USE - New camptothecin derivatives with the following structure of the formula (I), their use and the pharmaceutical compositions containing the same. The compounds of the present invention have good anti-tumor activities and good solubility in water, and can be used in development of medicines. | 12-31-2009 |
20100004276 | VITAMIN RECEPTOR BINDING DRUG DELIVERY CONJUGATES - The invention describes a vitamin receptor binding drug delivery conjugate, and preparations therefor. The drug delivery conjugate consists of a vitamin receptor binding moiety, a bivalent linker (L), and a drug. The vitamin receptor binding moiety includes vitamins, and vitamin receptor binding analogs and derivatives thereof, and the drug includes analogs and derivatives thereof. The vitamin receptor binding moiety is covalently linked to the bivalent linker, and the drug, or the analog or the derivative thereof, is covalently linked to the bivalent linker, wherein the bivalent linker (L) includes components such as spacer linkers, releasable linkers, and heteroatom linkers, and combinations thereof. Methods and pharmaceutical compositions for eliminating pathogenic cell populations using the drug delivery conjugate are also described. | 01-07-2010 |
20100010032 | CAMPTOTHECIN DERIVATIVES WITH ANTITUMOR ACTIVITY - Novel camptothecin derivatives having antitumor activity, the processes for the preparation thereof, the use thereof as antitumor drugs and pharmaceutical compositions containing them. | 01-14-2010 |
20100035911 | DRUG COMBINATIONS TO TREAT HYPERPROLIFERATIVE DISORDERS - A method of treating a hyperproliferative disorder, including a cancer, in a subject in need of such treatment, comprising administering to said subject a pharmaceutical combination containing a treatment effective amount of: (a) a vitamin A derivative (i.e., a retinoid), or a pharmaceutically acceptable salt thereof, and an inhibitor of microtubule structure or function; or (b) a combination containing fenretinide (i.e., N-(4-hydrophenyl) retinamide, 4-HPR) and ABT-751 (i.e., N-[2-[(4-hydroxyphenyl)amino]-3-pyridinyl]-4-methoxybenzenesulfonamide). Vitamin A derivatives that may be useful for this invention according to (a) include, but are not limited to, all-trans-retinoic acid, 13-cis-retinoic acid, and fenretinide. Microtubule inhibitors that may be useful for this invention according to (a) include, but are not limited to, inhibitors of the Vinca binding domain (e.g., vincristine, vinblastine, vinorelbine, and cryptophycin 52), inhibitors of the Taxane domain (e.g., paclitaxel, docetaxel, and epothilones), and inhibitors of the colchicine site (e.g., colchicine, ABT-751, CI-980, and combretastatin). A preferred retinoid according to (a) is fenretinide. A preferred microtubule inhibitor according to (b) is ABT-751. | 02-11-2010 |
20100048603 | BROAD-SPECTRUM ANTI-CANCER TREATMENT BASED ON IMINOCAMPTOTHECIN DERIVATIVES - A subclass of camptothecin derivatives is disclosed to be useful for the preparation of a medicament for the treatment of a cancer or tumor pathology selected from the group consisting of head and neck carcinoma, pancreas carcinoma, melanoma, bladder carcinoma, mesothelioma and epidermoid skin carcinoma. | 02-25-2010 |
20100056555 | METHOD OF TREATING RAS ASSOCIATED CANCER - New methods of treating Ras associated cancer, and especially for treating cancer that is resistant or refractory to other treatment methods, including resistant or refractory to treatment with C225 and/or CPT-11, are provided. The new methods employ PEG-conjugated 7-ethyl-10-hydroxycampothecin, alone, or in combination with other art-known anticancer agents or modalities. | 03-04-2010 |
20100063083 | 5(S)-(2'-HYDROXYETHOXY)-20(S)-CAMPTOTHECIN AND ITS PREPARATION AND USE FOR THE TREATMENT OF CANCER - A 5(S)-(2′-hydroxyethoxy)-20(S)-camptothecin diasterisomer is described which is a better inhibitor of topoisomerase I than either the diastereoisomeric mixture 5(RS)-(2′-hydroxyethoxy)-20(S)-camptothecin, or the 5(R)-(2′-hydroxyethoxy)-20(S)-camptothecin diastereoisomer. Pharmaceutical compositions of the 5(S)-(2′-hydroxyethoxy)-20(S)-camptothecin diastereoisomer are also described as are methods of using the compound for the inhibition of topoisomerase I and for the treatment of cancer. | 03-11-2010 |
20100076008 | Pharmaceutical compositions containing plasma protein - The invention is related to water-soluble products and pharmaceutical formulations in solid or liquid form mainly for parenteral use. They consist of or comprise a therapeutically active substance (having low aqueous solubility and a substantial binding affinity to plasma proteins) and a plasma protein fraction in controlled aggregation state, whereby the said active substance and the said protein fraction are bound to each other by way of non-covalent bonds. It also covers processes for the preparation of the product and pharmaceutical formulation by dissolving the water-insoluble active substance in a water-miscible, pharmaceutically acceptable solvent, combining said solution with the aqueous solution of a plasma protein fraction in controlled aggregation state whereby a true solution is obtained containing the said active substance and the said protein fraction bound together by way of non-covalent bonds. Optionally a further pharmaceutically acceptable auxiliary additive—such as a protein aggregation controller and/or a stabilizer—may be present. The organic solvent is eliminated by dialysing, ultrafiltrating, diafiltrating and/or lyophilising. The solid products consisting of the active substance and the protein are also protected. On optional dissolution in water clear, liquid compositions are obtained suitable for direct parenteral or other administration. Method of treatment is also covered. A series of water-insoluble substances is enlisted with appropriate protein fractions to be used. | 03-25-2010 |
20100076009 | Adjuvant Chemotherapy For Anaplastic Gliomas - The present invention involves the use of 2,4-disulfonyl phenyl tert-butyl nitrone (2,4-ds-PBN) in the treatment and prevention of gliomas. The 2,4-ds-PBN may be used alone or combined with other traditional chemo- and radiotherapies and surgery, to treat or prevent glioma occurrence, recurrence, spread, growth, metastasis, or vascularization. | 03-25-2010 |
20100087473 | FREEZE-DRIED INJECTABLE PHARMACEUTICAL COMBINATION OF SEMISYNTHETIC VINCA ALKALOIDS AND CARBOHYDRATE STABLE AT ROOM TEMPERATURE - This invention relates to pharmaceutical compositions consisting of a semisynthetic derivative of vinca alkaloid, stable at room temperature, in which said derivative is present in the form of a freeze dried product obtained in the presence of at least one carbohydrate. | 04-08-2010 |
20100105716 | CAMKK(BETA) AS A TARGET FOR TREATING OBESITY - A method of treating a condition in a subject in need thereof, comprising administering a calcium/calmodulin dependency kinase kinase (CaMKK) inhibitor in a treatment-effective amount. Conditions which may be treated include obesity (particularly adult obesity), insulin resistance (including high fat diet-induced insulin resistance), hyperglycemia (including hyperglycemia accompanying obesity), diabetes, etc. | 04-29-2010 |
20100113498 | NOVEL VINBLASTINE DERIVATIVES, THEIR PREPARATION, USE AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAID DERIVATIVES - The invention provides vinblastine derivatives represented by the following formula 1 or their physiologically acceptable salts, their preparation, use and pharmaceutical compositions comprising the said derivatives. The said vinblastine derivatives show inhibiting activities against tumor cell lines and can be used as medicaments for treating malignant tumors. | 05-06-2010 |
20100120816 | CAMPTOTHECIN DERIVATIVES WITH ANTITUMOR ACTIVITY - Novel camptothecin derivatives having antitumor activity, the processes for the preparation thereof, the use thereof as antitumor drugs and pharmaceutical compositions containing them. | 05-13-2010 |
20100130525 | AQUEOUS SOLUTION PREPARATION CONTAINING CAMPTOTHECIN COMPOUNDS - An object of the invention is to provide a camptothecin compounds-containing aqueous pharmaceutical preparation which can be produced without heating and in which camptothecin compounds are dissolved in a stable state. The invention provides a camptothecin compound-containing aqueous pharmaceutical preparation, containing the following ingredients (a) to (c):
| 05-27-2010 |
20100137350 | METHODS FOR PREPARING DEHYDROCAVIDINE, DEHYDROAPOCAVIDINE OR THEIR COMPOSITION, THEIR USE AND MEDICINAL COMPOSITON CONTAINING THEM - A method for preparing dehydrocavidine, dehydroapocavidine and their respective composition is provided. The composition is first prepared by isolating and purifying the quaternary ammonium alkaloid components from the medicinal plant “Yan Huang Lian” ( | 06-03-2010 |
20100160365 | TREATMENT OF NON-HODGKIN'S LYMPHOMAS WITH MULTI-ARM POLYMERIC CONJUGATES OF 7-ETHYL-10-HYDROXYCAMPTOTHECIN - The present invention relates to methods of treatment of non-Hodgkin's lymphomas. The present invention includes administering polymeric prodrugs of 7-ethyl-10-hydroxycamptothecin to patients in need thereof. | 06-24-2010 |
20100168149 | Camptothecin Analogue Compounds, a Process for Their Preparation and Pharmaceutical Compositions Containing Them - Compound of formula (I): | 07-01-2010 |
20100168150 | Camptothecin Analogue Compounds, a Process for Their Preparation and Pharmaceutical Compositions Containing Them. - Compound of formula (I): | 07-01-2010 |
20100179180 | CRYSTALLINE IRINOTECAN HYDROCHLORIDE AND METHODS FOR ITS PREPARATION - Disclosed is a crystalline form of irinotecan hydrochloride (I) and processes for the preparation thereof from crude irinotecan hydrochloride or another polymorphic form of irinotecan. Said crystalline form is particularly suitable for industrial use, because it is easily filtered and possesses characteristics of high stability and purity. | 07-15-2010 |
20100179181 | PHARMACEUTICAL FORMULATIONS OF BIODEGRADABLE BIOCOMPATIBLE CAMPTOTHECIN-POLYMER CONJUGATES - A camptothecin/polymer dual phase drug release system is described that is stable in both liquid and lyophilized states. The polymer contains acetals and/or ketals. | 07-15-2010 |
20100197718 | TREATMENT OF PEDIATRIC TUMORS - A subclass of camptothecin derivatives is disclosed to be useful for the preparation of a medicament for the treatment of pediatric tumors such as for examplerhabdomyosarcoma, primitive neuroectodermal tumors (PNET) and neuroblastoma. | 08-05-2010 |
20100204260 | Multi-Substituted Imidazolines And Method Of Use Thereof - A new class of imidazolines as 4-position acids or esters with very potent anti-inflammatory as well as antimicrobial activity is described. The synthesis of these imidazolines includes a multicomponent reaction applicable to a combinatorial synthetic approach. The combination of these two key characteristics provides an effective therapeutic drug in the treatment of septic shock as well as many other inflammatory (arthritis and asthma) and infectious disorders. The use of this novel class of non-steroidal agents as anti-inflammatory agents (for the treatment of asthma etc.), antibacterial agents and antiseptic agents is described. The compounds are also useful in the treatment of tumors (such as cancers). The imidazolines are potent inhibitors of the transcription factor NF-κB as well as potent activity against the Gram (+) bacterium | 08-12-2010 |
20100204261 | MULTI-ARM POLYMERIC CONJUGATES OF 7-ETHYL-10-HYDROXYCAMPTOTHECIN FOR TREATMENT OF BREAST, COLORECTAL, PANCREATIC, OVARIAN AND LUNG CANCERS - A four arm-polyethylene glycol-7-ethyl-10-hydroxycamptothecin conjugate, such as, | 08-12-2010 |
20100210677 | NOVEL COMPOUND, CORRESPONDING COMPOSITIONS, PREPARATION AND/OR TREATMENT METHODS - Disclosed is a novel crystalline form of topotecan monohydrochloride pentahydrate, which is a pentahydrate of 10-[(dimethylamino)methyl]-4-ethyl-4,9-dihydroxy-1H-pyrano[3′,4′:6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)dione monohydrochloride, corresponding pharmaceutical compositions, methods preparation and/or use thereof to treat anti-viral and/or cancer-related diseases. | 08-19-2010 |
20100227877 | NEW CAMPTOTHECIN DERIVATIVES AND USES THEREOF - The present invention provides two new camptothecin derivatives, which were identified as S,R- and S,S-topotecan lactates, respectively. Both compounds have anticancer activities. Pharmaceutical compositions of the new camptothecin derivatives, and cancer therapies with the new camptothecin derivatives or their pharmaceutical compositions were also provided. | 09-09-2010 |
20100267759 | INHIBITORS OF Akt ACTIVITY - Invented are novel heterocyclic carboxamide compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis. | 10-21-2010 |
20100305148 | DI-ESTER PRODRUGS OF CAMPTOTHECIN, PROCESS FOR THEIR PREPARATION AND THEIR THERAPEUTICAL APPLICATIONS - The present invention is related to 10,20-di-O ester derivatives of camptothecin and pharmaceutical formulations thereof. The compounds and pharmaceutical formulations of the present invention possess increased biological life span and bioavailability and reduced toxicity, while maintaining anti-cancer activity. | 12-02-2010 |
20100305149 | Polyal Drug Conjugates Comprising Variable Rate-Releasing Linkers - Polyal-Drug conjugates comprising a variable rate-releasing linker are described along with methods of making such conjugates. Uses for such Polyal-Drug conjugates is also described. | 12-02-2010 |
20100311783 | STEREOSELECTIVE PROCESS AND CRYSTALLINE FORMS OF A CAMPTOTHECIN - A stereoselective process for preparing 7-[(E)-t-butyloxyiminomethyl]-camptothecin (also known as gimatecan) is herein disclosed. With the addition of further dissolution and precipitation steps carried out in appropriate different solvent mixtures, four new crystalline forms of gimatecan are also obtainable by using the same stereoselective process. | 12-09-2010 |
20100311784 | STEREOSELECTIVE PROCESS AND CRYSTALLINE FORMS OF A CAMPTOTHECIN - A stereoselective process for preparing 7-[(E)-t-butyloxyiminomethyl]-camptothecin (also known as gimatecan) is herein disclosed. With the addition of further dissolution and precipitation steps carried out in appropriate different solvent mixtures, four new crystalline forms of gimatecan are also obtainable by using the same stereoselective process. | 12-09-2010 |
20110003841 | BIOACTIVE COMPOSITION FOR THE TREATMENT OF THE HIV/AIDS, METHOD FOR MANUFACTURING AND USING THE SAME - The present invention is about a bioactive composition for the treatment of HIV, particularly by the removal of the most prominent HIV antigen glycoproteins. The present invention further relates to the method for making and using such composition. | 01-06-2011 |
20110003842 | MARKER FOR DETERMINATION OF SENSITIVITY TO ANTI-CANCER AGENT - Provided are a marker for determining sensitivity to an anticancer agent capable of distinguishing a therapeutic response of an individual patient and a novel means for a cancer therapy using the marker. The marker for determining sensitivity to an anticancer agent contains a substance in a metabolic pathway in which L-phenylalanine and/or N,N-dimethyl glycine are/is involved. | 01-06-2011 |
20110015221 | PHARMACEUTICAL COMPOSITION OF VINFLUNINE WHICH IS INTENDED FOR PARENTERAL ADMINISTRATION PREPARATION METHOD THEREOF AND USE OF SAME - The invention relates to a pharmaceutical composition of vinflunine in the form of a stable sterile aqueous solution of a water-soluble salt of vinflunine with a pH of between 3 and 4. The invention also relates to the method of preparing said composition and to the use thereof as a parenterally-administered medicament for the treatment of cancer. | 01-20-2011 |
20110053972 | INHIBITORS OF AKT ACTIVITY - Invented are novel heterocyclic carboxamide compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis. | 03-03-2011 |
20110071182 | Inhibitors of AKT Activity - Invented are novel heterocyclic carboxamide compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis. | 03-24-2011 |
20110082168 | COMPOSITIONS FOR DELIVERING HIGHLY WATER SOLUBLE DRUGS - The present invention provides compositions for delivering highly water-soluble drugs (such as | 04-07-2011 |
20110136850 | METHODS AND COMPOSITIONS FOR TOPOISOMERASE I MODULATED TUMOR SUPPRESSION - Disclosed herein are methods and compositions for determining the sensitivity or enhancing the sensitivity of cells to the effects of topoisomerase I inhibitors. Also disclosed are methods and compositions for inducing cell death, apoptosis and/or growth arrest which may be used for tumor suppression. | 06-09-2011 |
20110152305 | FILMS AND PARTICLES - Described herein are compounds and processes that can be used to prepare polymer-based films, particles, gels and related compositions, and processes for delivery of agents, and other uses. | 06-23-2011 |
20110184009 | CAMPTOTHECIN DERIVATIVES AS CHEMORADIOSENSITIZING AGENTS - Camptothecin-based compounds are useful for treating a neoplasm in mammalian subjects by administering such compound to the subjects in combination with radiotherapy, i.e., the treatment of tumors with radioactive substances or radiation from a source external to the subject. Camptothecin-based compounds are modified by positioning at least one electron-affinic group around the camptothecin structure to enhance their value in combination with radiotherapy. New Camptothecin-based compounds are disclosed that are useful for treating cancer by administering the novel compounds alone or in combination with radiotherapy. | 07-28-2011 |
20110195990 | TREATMENT OF RESISTANT OR REFRACTORY CANCERS WITH MULTI-ARM POLYMERIC CONJUGATES OF 7-ETHYL-10-HYDROXYCAMPTOTHECIN - A method of treating a resistant or refractory cancer in a mammal includes administering an effective amount of a compound of | 08-11-2011 |
20110201636 | USE OF 14,15-DIHYDRO-20,21-DINOREBURNAMENIN-14-OL FOR THE TREATMENT AND/OR PREVENTION OF SERIOUS DEPRESSION AND SLEEP/WAKING CYCLE DISORDERS - The invention relates to a novel therapeutic use of 14,15-dihydro-20,21-dinoreburnamenin-14-ol for the treatment of serious depression in humans, particularly for the treatment of a patients resistant to conventional anti-depressant treatments and for treatment of sleep/waking cycle disorders. | 08-18-2011 |
20110201637 | PHENANTHROINDOLIZIDINE DERIVATIVE AND NFKB INHIBITOR CONTAINING SAME AS ACTIVE INGREDIENT - A novel compound having an excellent NFκB inhibitory effect is provided. Specifically disclosed is a compound represented by the following formula (1) or a salt thereof:
| 08-18-2011 |
20110201638 | PHENANTHROINDOLIZIDINE COMPOUND AND NFkB INHIBITOR CONTAINING SAME AS ACTIVE INGREDIENT - A novel compound having an excellent NFκB inhibitory effect is provided and specifically disclosed is a compound represented by the following formula (1) or a salt thereof: | 08-18-2011 |
20110207764 | CYCLOPOLYSACCHARIDE COMPOSITIONS - The present invention is directed to a composition including: (a) an active ingredient other than bendamustine; (b) a charged cyclopolysaccharide comprising at least one charged group; and (c) a stabilizing agent comprising at least one charged group having a charge opposite to that of the cyclopolysaccharide. The composition provides unexpectedly desirable stability in reactive environments such as plasma which contain entities (such as enzymes, other proteins and the like) and/or conditions which can decompose or deactivate the active ingredient. | 08-25-2011 |
20110212986 | ANTI-FLAVIVIRUS THERAPEUTIC - The present invention relates to anti-flavivirus compounds, including lycorine and derivatives thereof, and their use in treating a subject infected by a flavivirus. The present invention also relates to the use of the anti-flavivirus compounds for the prophylaxis of flavivirus infection. The present invention further relates to a method of suppressing viral RNA synthesis of a flavivirus. Also described is a method of preparing an anti-flavivirus compound for use in the treatment or prophylaxis of flavivirus infection. | 09-01-2011 |
20110269789 | Compositions and Methods for Achieving Sustained Therapeutic Drug Concentrations in a Subject - Provided herein are compounds and methods for achieving a sustained therapeutic effect of small molecule anti-cancer agents when administered in vivo. | 11-03-2011 |
20110301188 | Synergistic Effects Between Sphingosine-1-Phosphate Receptor Antagonists and Antimicrotubule Agents - This invention is based on the discovery that the administration of a sphingosine-1-phosphate receptor antagonist (S1P) and at least one chemotherapeutic agent selected from the the group of antimicrotubule agents provides an unexpectedly superior treatment for cancer. Antimicrobial agents such as the taxane compounds are known in the art, for example, paclitaxel (available as TAXOL® from Bristol-Myers Squibb, Princeton, N.J.), docetaxel (available as TAXOTERE® from Sanofi-aventis, Bridgewater, N.J.) and the like and other compounds that act as antimicrotubule agents, such as Vincristine (ONCOVIN®, VINCASAR PFS®, VCR), Vinblastin (VELBAN®, VELSAR®) and Vinorelbine, and similar compounds. The present invention also provides methods of modulating the growth of selected cell populations, such as cancer cells, by administering a therapeutically effective amount of at least one sphingosine-1-phosphate 1 (S1P1R) receptor antagonists, and at least one antimicrotubule agent. | 12-08-2011 |
20120004255 | DUAL PHASE DRUG RELEASE SYSTEM - The present invention relates to conjugate comprising a carrier substituted with one or more occurrences of a moiety having the structure: | 01-05-2012 |
20120046310 | COMPOSITIONS FOR DELIVERING HIGHLY WATER SOLUBLE DRUGS - The present invention provides compositions for delivering highly water-soluble drugs (such as vinca alkaloids) and methods of using such compositions. | 02-23-2012 |
20120129880 | METHOD FOR DETERMINING SENSITIVITY TO IRINOTECAN AND USE THEREOF - To provide a method for determining the sensitivity of a patient to irinotecan, SN-38, and/or a salt thereof, which method can determine the therapeutic response of the patient and to provide a novel cancer therapeutic means employing the method. | 05-24-2012 |
20120129881 | COMBINATIONS OF THERAPEUTIC AGENTS FOR TREATING CANCER - A combination of an mTOR inhibitor compound with one or more pharmaceutically active agents, for simultaneous, concurrent, separate or sequential use for preventing or treating a proliferative disease. | 05-24-2012 |
20120142721 | SMALL MOLECULE INHIBITORS OF POLYNUCLEOTIDE KINASE/PHOSPHATASE, POLY(ADP-RIBOSE) POLYMERASE AND USES THEREOF - The present invention generally relates to use of compounds and compositions as a chemosensitizers and/or radiosensitizers and/or inhibitors of PNKP phosphatase activity. The present invention provides pharmaceutical combinations and/or a pharmaceutically acceptable salt thereof, kits containing such compounds and/composition and methods of using such compounds and/or compositions. | 06-07-2012 |
20120142722 | CONJUGATES OF CYTOTOXIC DRUGS - Novel compounds and pharmaceutical compositions are provided. In one aspect of the invention the compounds may be utilized in medical practice, for example, in treatment of cancer and immune disorders. In another aspect of the invention there is provided a conjugate, comprising a cytotoxic agent and a modulating moiety, the modulating moiety serving to target apoptotic cells. | 06-07-2012 |
20120190703 | SALTS OF 13A-(S)DESOXYTYLOPHORININE, PREPARATION METHODS AND PHARMACEUTICAL COMPOSITIONS AND USES THEREOF - The present invention relates to the salts of (+)-13a-(S)-deoxytylophorinine represented by the general formula (I), the preparation method thereof, the pharmaceutical compositions containing them, and their use as medicaments for prevention and/or treatment of cancer and/or inflammation disease. | 07-26-2012 |
20120202840 | Use of Flubendazole and Vinca Alkaloids for Treatment of Hematological Diseases - Provided are methods for treating a hematological malignancy comprising administering an effective amount of flubendazole alone or in combination with a vinca alkaloid. Also provided are compositions and kits comprising an effective amount of flubendazole and/or a vinca alkaloid for use in the methods of the disclosure. | 08-09-2012 |
20120220618 | ANTICANCER AGENT SENSITIVITY-DETERMINING MARKER - To provide a marker for determining sensitivity of a patient to an anti-cancer agent, and novel cancer therapeutic means employing the marker. | 08-30-2012 |
20120270896 | Antineoplastic Combinations Containing HKI-272 and Vinorelbine - A combination of HKI-272 compound and a vinorelbine compound in the treatment of a neoplasm is provided. Regimens, kits, and methods for treatment of neoplasm, including breast cancer including metastatic breast cancer, and lung cancer, using this combination, optionally in combination with other anti-neoplastic agents, or immune modulators are also described. | 10-25-2012 |
20120283284 | MELONINE BISINDOLE COMPOUNDS, PHARMACEUTICAL COMPOSITIONS, PREPARATION METHOD AND USE THEREOF - The present invention relates to pharmaceutical technical field, to melonine bisindole compounds, pharmaceutical compositions thereof, and preparation methods thereof. Specifically, the present invention relates to melonine bisindole compounds of Formula I, pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the compounds or pharmaceutically acceptable salts thereof. The present invention further relates to method for preparing the melonine bisindole compounds of Formula I or pharmaceutically acceptable salts thereof, and the use of the melonine bisindole compounds of Formula I or pharmaceutically acceptable salts thereof in the manufacture of a medicament for the treatment or prophylaxis of cancers. | 11-08-2012 |
20120289535 | DUAL PHASE DRUG RELEASE SYSTEM - The present invention relates to conjugate comprising a carrier substituted with one or more occurrences of a moiety having the structure: | 11-15-2012 |
20120295932 | METHOD FOR THE TREATMENT OF CANCER - Provided is a method for determining the prognosis of cancer in a female patient with a solid tumor. Also provided is a method of sensitizing a cancer cell from a solid tumor from a male patient other than a prostate cancer cell to treatment with a chemotherapeutic agent comprising administering an effective amount of
| 11-22-2012 |
20120329822 | 10'-FLUORINATED VINCA ALKALOIDS PROVIDE ENHANCED BIOLOGICAL ACTIVITY AGAINST MDR CANCER CELLS - A 10′-fluoro-vinca alkaloid compound or its pharmaceutically acceptable salt is disclosed, as are methods of its preparation and use. A disclosed 10′-fluoro-vinca alkaloid compound has better cytotoxic potency against leukemia and cancer cell lines, and is about 8-times more cytotoxic to a multiple drug resistant cancer cell line than is a parental 10′-unsubstituted vinca alkaloid. | 12-27-2012 |
20130143909 | Acid Salt Forms of Polymer-Drug Conjugates and Alkoxylation Methods - Among other aspects, provided herein is a mixed-acid salt of a water-soluble polymer-drug conjugate, along with related methods of making and using the same. The mixed-salt acid salt is stably formed, and appears to be more resistant to hydrolytic degradation than the corresponding predominantly pure acid salt or free base forms of the polymer-drug conjugate. The mixed acid salt is reproducibly prepared and recovered, and provides surprising advantages over non-mixed acid salt forms of the water-soluble polymer drug conjugate. | 06-06-2013 |
20130158062 | MULTI-ARM POLYMER PRODRUGS - Provided herein are water-soluble prodrugs, compositions comprising such prodrugs, and related methods of making and administering the same. The prodrugs of the invention comprise a water-soluble polymer having three or more arms, at least three of which are typically covalently attached to an active agent, e.g., a small molecule. The conjugates of the invention provide an optimal balance of polymer size and structure for achieving improved drug loading, since the conjugates of the invention possess three or more active agents releasably attached to a multi-armed water-soluble polymer. The prodrugs of the invention are therapeutically effective, and exhibit improved properties in-vivo when compared to unmodified parent drug. | 06-20-2013 |
20130178493 | USE OF 14,15-DIHYDRO-20,21-DINOREBURNAMENIN-14-OL FOR THE TREATMENT AND/OR PREVENTION OF SERIOUS DEPRESSION AND SLEEP/WAKING CYCLE DISORDERS - The invention relates to a novel therapeutic use of 14,15-dihydro-20,21-dinoreburnamenin-14-ol for the treatment of serious depression in humans, particularly for the treatment of a patients resistant to conventional anti-depressant treatments and for treatment of sleep/waking cycle disorders. | 07-11-2013 |
20130231359 | Salt Form of a Multi-Arm Polymer-Drug Conjugate - Among other aspects, provided herein is a hydrohalide salt of a multi-arm water-soluble polyethylene glycol-drug conjugate, along with related methods of making and using the same. The hydrohalide salt is stably formed, and appears to be more resistant to hydrolytic degradation than the corresponding free base form of the conjugate. | 09-05-2013 |
20130274281 | METHODS OF TREATING METASTATIC BREAST CANCER WITH 4-IODO-3-NITROBENZAMIDE AND IRINOTECAN - Provided herein are methods, compositions and kits for the treatment of locally advanced or metastatic breast cancer or breast cancer brain metastases. The method comprises administration of 4-iodo-3-nitrobenzamide, a metabolite or salt thereof in combination with irinotecan. The method of treating locally advanced or metastatic breast cancer comprises at least one 21 day treatment cycle. | 10-17-2013 |
20130303562 | CHEMICAL AND RNAI SUPPRESSORS OF NEUROTOXICITY IN HUNTINGTON'S DISEASE - The invention relates to methods for screening and identification of compounds and compositions that are useful in the treatment of neurological disorders, for example, of polyQ tract expansion diseases, such as Huntington's Disease. The invention further relates to methods, compounds, and compositions for the treatment of a variety of neurological disorders. | 11-14-2013 |
20140011833 | CAMPTOTHECIN DERIVATIVES HAVING ANTI-TUMOR ACTIVITY - Disclosed are novel camptothecin derivatives having anti-tumor activity (the basic structure thereof is as shown in the figure) and compositions of such compounds and use thereof. The compounds according to the present invention exhibit very good water solubility and stability, show good selectivity among drugs of the same category, and have a very high therapeutic index. Such compounds are promising as therapeutic agents for treating tumors. | 01-09-2014 |
20140088133 | METHODS AND COMPOSITIONS FOR TREATING BETA-THALASSEMIA AND SICKLE CELL DISEASE - The present invention provides compounds (such as compounds of formula I-a) that induce γ globin expression and pharmaceutical compositions thereof. Such compounds may have beneficial therapeutic effects. Compounds and compositions described herein may be used to treat hemoglobinopathies such as β-thalassemia and sickle cell anemia. (I-a) | 03-27-2014 |
20140107147 | Antineoplastic Combinations Containing HKI-272 and Vinorelbine - A combination of HKI-272 compound and a vinorelbine compound in the treatment of a neoplasm is provided. Regimens, kits, and methods for treatment of neoplasm, including breast cancer including metastatic breast cancer, and lung cancer, using this combination, optionally in combination with other anti-neoplastic agents, or immune modulators are also described. | 04-17-2014 |
20140128421 | CAMPTOTHECIN COMPOUND CONTAINING STABLE 7-MEMBERED LACTONE RING, PREPARATION METHOD AND USE - Provided are a camptothecin compound containing 7-membered lactone ring, as shown in general formula I, and pharmaceutically acceptable salt thereof, as well as the preparation method and use thereof. In general formula I, R | 05-08-2014 |
20140135356 | Novel Analogs of Camptothecin - The present invention provides novel conjugates of camptothecin and camptothecin analogs with a linker and an HSA-binding moiety. The novel conjugates are prodrug forms of the camptothecin or camptothecin analogs and can be used to treat mammalian cell proliferative diseases, such as cancer. | 05-15-2014 |
20140135357 | DOSE REGIME FOR CAMPTOTHECIN DERIVATIVES - The present invention is directed to a method of inhibiting cancer cell growth, comprising administering a pharmaceutical composition to a subject in need thereof. The pharmaceutical composition comprises at least one camptothecin derivative or a pharmaceutically acceptable salt thereof; and at least one PEG phospholipid, and provides a sustained release of topotecan as an active ingredient. | 05-15-2014 |
20140194458 | DERIVATE, PREPARATION METHOD AND USE OF 10-METHOXYCAMPTOTHECINE - Provided is a 10-methoxycamptothecine derivate of formula (1), wherein R is selected from hydrogen, C | 07-10-2014 |
20140296278 | 5-NONYLOXYTRYPTAMINE AND RELATED INTRACELLULAR PH ACIDIFIERS FOR THE TREATMENT AND PREVENTION OF CANCER - Provided herein are compositions for lowering intracellular pH in a cell or population of cells from a subject comprising contacting the cell or population of cells with a therapeutically effective amount of 5-nonyloxytryptamine or a pharmaceutically acceptable salt, solvate, stereoisomer, or derivatives thereof. These compounds are useful for acidification of cells, including cancer cells, which induces apoptosis and cell necrosis. Methods of use of these compounds, including in pharmaceutical compositions in conjunction with other biologically active agents, in treatment of cancers, including glioblastoma and related neuronal cancers are also included. | 10-02-2014 |
20140323513 | Chemotherapeutic Compositions and Methods for Treating Human Gliomas - Disclosed are compound for targeting chemotherapeutic agents to mammalian mitochondria. Also disclosed are monoamine oxidase-specific compositions, and methods of using them for the selective therapy of mammalian cancers, and in particular, in the treatment of human gliomas. Also disclosed are methods employing the novel targeted chemotherapeutics with one or more conventional anti-cancer therapies, including, for example, radiotherapy, or multi-drug regimens. | 10-30-2014 |
20140323514 | MULTI-ARM POLYMER PRODRUGS - Provided herein are water-soluble prodrugs, compositions comprising such prodrugs, and related methods of making and administering the same. The prodrugs of the invention comprise a water-soluble polymer having three or more arms, at least three of which are typically covalently attached to an active agent, e.g., a small molecule. The conjugates of the invention provide an optimal balance of polymer size and structure for achieving improved drug loading, since the conjugates of the invention possess three or more active agents releasably attached to a multi-armed water-soluble polymer. The prodrugs of the invention are therapeutically effective, and exhibit improved properties in-vivo when compared to unmodified parent drug. | 10-30-2014 |
20140343088 | TROLOX DERIVATIVE-MODIFIED FAT-SOLUBLE ANTI-CANCER PHARMACEUTICAL COMPOUNDS, PREPARATIONS, PREPARING METHODS AND USE THEREOF - Disclosed is a trolox derivative-modified fat-soluble anti-cancer pharmaceutical compound having a structure as represented by formula I or II. An active moiety of the anti-cancer pharmaceutical compound, camptothecin or a camptothecin derivative, is covalently bonded to a lipophilic moiety, a trolox ester or a trolox amide, by a linking group to form the fat-soluble anti-cancer pharmaceutical compound. Also disclosed are a preparation, preparing method and use of the pharmaceutical compound. | 11-20-2014 |
20140357659 | METHOD FOR PREDICTING AND EVALUATING RESPONSIVENESS TO CANCER TREATMENT WITH DNA-DAMAGING CHEMOTHERAPEUTIC AGENTS - Provided herein are methods directed to the prediction and early assessment of the efficacy of cancer treatment regimens, in particular in patients undergoing therapy with a DNA-damaging chemotherapeutic agent, by determining expression levels of certain proteins found to be useful as biomarkers in circulating tumor cells obtained from the patient both prior to and post-treatment. | 12-04-2014 |
20140371258 | Water-Soluble Polymer Conjugates of Topotecan - Provided herein are water-soluble polymer conjugates of topotecan, along with compositions comprising the conjugates and related methods of making and using the same. | 12-18-2014 |
20150057305 | PHARMACEUTICAL COMPOSITION - Disclosed in the present invention is a pharmaceutical composition, comprising a weight ratio of 1:120 to 1:1000 of camptothecin compound of formula I and β-cyclodextrin or derivatives thereof, and an acidic buffer to adjust the pH=3.5-6.0. The composition can be used to treat solid tumours, such as melanoma, pancreatic cancer, hepatoma etc. The pharmaceutical composition of the present invention is miscible with a water-miscible co-solvent system in any proportion, and can be used as an intravenous infusion solvent, and has no obvious hemolysis or vascular stimulation; the pharmaceutical composition has a better tumour inhibiting rate than solubilisation of surfactants. | 02-26-2015 |
20150073008 | Topical Application of Vinca Alkaloids for the Treatment of Actinic Keratosis - The present invention provides pharmaceutical compositions comprising a vinca alkaloid of formula (I): | 03-12-2015 |
20150087668 | Methods for Treating Humans Having Brain Cancer - Among other things, a method of treating a human having brain cancer is, the method comprising administering via a non-continuous dosing regimen to the human having brain cancer, a therapeutically effective amount of a pharmaceutical composition comprising a prodrug or a pharmaceutically acceptable salt thereof, wherein the non-continuous dosing regimen comprises administering the pharmaceutical composition no more frequently than once every seven days for at least two dosings. | 03-26-2015 |
20150111918 | IMMUNE SYSTEM NEUROMODULATION AND ASSOCIATED SYSTEMS AND METHODS - Methods for treating a patient using therapeutic immune system neuromodulation and associated devices, systems, and methods are disclosed herein. One aspect of the present technology is directed to methods including modulating nerves proximate a vessel or duct of an immune system organ using an intravascularly or intraluminally positioned therapeutic element. One or more measurable physiological parameters corresponding to an immune system disorder, a condition associated with sympathetic activity in an immune system organ, or a condition associated with central sympathetic activity in the patient can thereby be reduced. | 04-23-2015 |
20150141453 | Trigger-Responsive Chain-Shattering Polymers - Disclosed are polymers containing a backbone comprising alternating N-protected hydroxymethylaniline units (“spacer”) and linker units. | 05-21-2015 |
20150148369 | CHEMICAL SUPPRESSORS OF NEUROTOXICITY IN SYNUCLEINOPATHIC DISEASES - The current application relates to the use of a compound selected from the group consisting of camptothecin and its analog, 10-hydroxy camptothecin, topotecan, irinotecan, 18-beta-glycyrrhetinic acid and its analog, carbinoxolone, etoposide, topoisomerase inhibitors, and combinations thereof, for the treatment of a synucleinopathy disease or disorder such as Parkinson's disease. | 05-28-2015 |
20150291610 | C20' Urea Derivatives of Vinca Alkaloids - A vinca alkaloid compound that is substituted at the 20′-position with a urea or thiourea group is disclosed. The urea's proximal nitrogen atom bonded to the 20′-position carbon atom is secondary, whereas the distal nitrogen atom can be unsubstituted only when the compound contains an optionally present 10′-fluoro substituent, and is otherwise preferably mono- or di-substituted. Methods of preparing the compounds are disclosed as are compositions for their use and methods of treatment using a compound. | 10-15-2015 |
20150344941 | RECOGNITION-RELEASE NANOPOROUS SUBSTRATE COMPRISING ACTIVE AGENTS, METHODS OF THEIR PREPARATION AND USES - The present invention relates to a porous substrate comprising at least one active agent entrapped within said pores of said substrate; wherein said pores are capped by at least one nucleic acid sequence; said agent is being released by a triggered reaction of said capping sequence with at least one analyte (biomarker) thereby allowing said capping to be cleaved from said pore. The invention further relates to methods of manufacturing said substrate, uses thereof for the controlled administration of active agents and diagnostic of conditions in a patient. | 12-03-2015 |
20160143900 | CAMPTOTHECIN DERIVATIVES AS ANTI-HIV AGENTS AND METHODS OF IDENTIFYING AGENTS THAT DISRUPT VIF SELF-ASSOCIATION - The present invention relates to the use of camptothecin derivatives as anti-HIV agents that disrupt self-association of the viral infectivity factor (Vif) found in HIV and other retroviruses. The present invention also relates to methods of identifying agents that disrupt VIf self-association and methods of using these agents, including methods of treating or preventing HIV infection. | 05-26-2016 |
20160175291 | SUPRESSION OF IGE PRODUCTION BY COMPOUNDS DERIVED FROM TRADITIONAL CHINESE MEDICINE | 06-23-2016 |
20160194274 | PHENANTHRENE DERIVATIVES FOR USE AS MEDICAMENTS | 07-07-2016 |
20170231972 | ANTINEOPLASTIC COMBINATIONS CONTAINING HKI-272 AND VINORELBINE | 08-17-2017 |