153 results about "Anti-Carcinogenic Agents" patented technology

The present invention provides a medicinal composition having an excellent antitumor activity. That is, it provides a medicinal composition comprising a sulfonamide compound, a sulfonate compound or a salt of them, which is represented by the following formula: (wherein ring A represents an aromatic ring which may have a substituent group; ring B represents a 6-membered unsaturated hydrocarbon ring which may have a substituent group etc.; ring C represents a 5-membered hetero-ring containing one or two nitrogen atoms, and the ring C may have a substituent group; W represents a single bond or -CH=CH-; X represents -NH- etc.; and Y represents a carbon atom or a nitrogen atom; and Z represents -NH- etc.), particularly N-(3-chloro-1H-indol-7-yl)-4-sulfamoylbenzenesulfonamide or a salt thereof, combined with at least one substance selected from (1) irinotecan hydrochloride trihydrate; (2) mitomycin C; (3) 5-fluorouracil; (4) cisplatin; (5) gemcitabine hydrochloride; (6) doxorubicin; (7) taxol; (8) carboplatin; (9) oxaliplatin; (10) capecitabine; and (11) a salt of the above-mentioned (1) to (10).

The preferred embodiments are directed to small molecule inhibitors that are cellular proliferation inhibitors and thus are useful as anticancer agents. The small molecules have the general formulas that include a phenylbenzimidazole core ring.

Synthesis of a chemical compound having the formula A-B-C that may serve for applications such as drug delivery where A is a chemiluminescent, moiety, B is a photochromic moiety, and C is a biologically active moiety where A-B-C may serve as a prodrug. Novel synthetic methods of the present invention to form the prodrug comprised the steps of (1) forming a benzophenone, (2) forming a diaryl ethylene, (3) attaching a phthalimide moiety to at least one of the aryl groups of the ethylene to form a phthalimide-ethylene conjugate, (4) condensing two ethylene-phthalimide conjugates to form a phthalimide-pentadiene conjugate, (5) converting the phthalimide to the phthalhydrazide by reaction with hydrazine to form a carrier compound according to the present invention, and (6) reacting the carrier compound with an nucleophilic moiety of the drug to form the corresponding prodrug. Alternatively the carrier can be prepared by using the halo-substituted diaryl ethylene to make the corresponding cationic leuco dye-like compound with known methods. The cationic compound then is protected by reacting with a nucleophile and coupled with the aminophathalimide by palladium-catalyzed amination to form the protected phthalimide-pentadiene conjugate. The latter is refluxed with hydrazine to convert its phthalimide to the phthalhydrazide and acidified to give the carrier. An additional aspect of the present invention relates to the use of these compounds as antiviral agents for the treatment of viral infections such as HIV and as anticancer agents for the treatment of cancers such as bowel, lung, and breast cancer.

According to an aspect of the invention, urological medical devices are provided, which comprise a prostatically beneficial agent selected from alpha-adrenergic blockers, antispasmodic agents, anticholinergic / antimuscarinic agents, calcium channel blockers, anti-inflammatory agents, hormone-affecting agents, anti-cancer agents, and combinations thereof, among others. The urological medical devices are adapted for implantation or insertion into a subject's urinary tract, whereupon at least a portion of the prostatically beneficial agent is released into the subject's prostatic urethra. The release profile of the prostatically beneficial agent is effective to treat a prostatic disorder, for example, benign prostate hypertrophy, prostate cancer or prostatitis, among others. Other aspects of the invention are directed to treating prostatic disorders.

The present invention relates to a method of treating cancer by administering an IGF-1R specific antibody in combination with an anti-cancer agent exemplified by an Akt pathway inhibitor. The first and second amounts together comprise a therapeutically effective amount.

Lonidamine or a lonidamine analog is administered with one or more additional anti-cancer agents or surgery or radiation to treat cancer or is administered alone or in combination to treat cancer, optionally in a sustained release formulation, and improve patient outcome.

New derivatives of platinum (II) complex are herein provided, which are liposoluble and applicable as antimicrobial agents and anticancer agents specific to the affected parts of patients and selectively transferred to the parts if they are used in combination with a contrast medium such as lipiodol, the derivatives being represented by the following general formula:(wherein R1 and R2 may be identical or different with each other and represent an ammine optionally substituted with an organic substituent and they may be bonded together through a bivalent organic group and R3 is a saturated or unsaturated higher fatty acid, these derivatives being prepared by nitrifying a cis-dichloro-di-(substituted or unsubstituted)-ammine platinum (II) and then reacting the resulting aqua type product with a corresponding alkali metal salt of higher fatty acid.

The present invention provides supramolecular hydrogels having a three-dimensional, self-assembling, elastic, network structure comprising non-polymeric, functional molecules and a liquid medium, whereby the functional molecules are noncovalently crosslinked. The functional molecules may be, for instance, anti-inflammatory molecules, antibiotics, metal chelators, anticancer agents, small peptides, surface-modified nanoparticles, or a combination thereof. Applications of the present invention include use of the supramolecular hydrogel, for instance, as a biomaterial for wound healing, tissue engineering, drug delivery, and drug / inhibitor screening.

Chemokine receptor CCR4 and its ligands CCL1 7 and CCL22 are used as markers for the identification and / or staging of cancer. The level of CCR4, CCL17 and CCL22 are found to increase during malignant tumour progression. CCR4, CCL17 and CCL22 are used as markers for the stratification of cancer patients according to their suitability for treatment with anti-cancer agents. Information of diagnostic character is provided by measuring the level of one or more of CCR4, CCL 17 and CCL22 present in a patient sample. Methods of treatment of cancer patients which agents that modulate the activity of CCR4, CCL17 and CCL22. Methods of screening for agents which modulate the biological activities of CCR4, CCL 17 and CCL22 provide anti-cancer agents.

Novel anti-cancer agents, including, but not limited to, antibodies and immunoconjugates, that bind to EGFR are provided. Methods of using the agents, antibodies, or immunoconjugates, such as methods of inhibiting tumor growth are further provided.

α,β-Unsaturated sulfones, sulfoxides, sulfonimides, sulfinimides, acylsulfonamides and acylsulfinamides of Formula I:wherein R1, R2, M1, M2, L, E1, E2, Q1, Q2 and n are as defined herein, are useful as anti-angiogenesis agents, as agents for treatment of age related senile dementia, and as antiproliferative agents including, for example, as anticancer agents.

Methods and compositions for treating cancer are described herein. More particularly, the methods for treating cancer comprise administering a 17a-hydroxylase / C17, 20-lyase inhibitor, such as abiraterone acetate (i.e., 3beta-acetoxy-17-(3-pyridyl) androsta-5, 16-diene), in combination with at least one additional therapeutic agent such as an anti-cancer agent or a steroid. Furthermore, disclosed are compositions comprising a 17a- hydroxylase / C17, 20-lyase inhibitor, and at least one additional therapeutic agent, such as an anti-cancer agent or a steroid.

The present invention relates to processes for the production of microbial glycolipids, mannosylerythritol lipids (MEL), from lignocellulosic carbon source. These processes are characterized in that the use of lignocellulosic materials for the production of a microbial glycolipids, MEL, comprising a fermentation preferably using fungi of the genus Pseudozyma or other microorganisms such as genetically modified fungi or bacteria. The processes for production of microbial glycolipids, MEL comprise three steps: pretreatment of lignocellulosic material; enzymatic hydrolysis; and fermentation. The enzymatic hydrolysis and fermentation may take place sequentially or simultaneously with addition of exogenous enzymes or simultaneously with enzymes produced by the microorganism itself. The produced microbial glycolipids have applications as: biosurfactants; antimicrobials; anticancer agents; wound healing factors; stabilizer agents on storage and purification of proteins or vaccines; drugs and gene deliver agents; antifreeze agents.

An anti-glypican 3 antibody with modified sugar chains, more specifically, an anti-glypican 3 antibody lacking fucose is provided. The anti-glypican 3 antibody with modified sugar chains of the present invention may be produced by a process comprising introducing a nucleic acid encoding an anti-glypican 3 antibody into host cells with reduced fucose addition capability, such as YB2 / 0 cells and cells lacking a fucose transporter. The anti-glypican 3 antibody with modified sugar chains of the present invention has a high level of cytotoxic activity and therefore is useful as a cell growth inhibitor such as an anticancer agent.

Provided are methods of suppressing growth of hormone refractory breast tumors by contacting tumor cells with an ErbB3 inhibitor, preferably an anti-ErbB3 antibody. Also provided are methods for treating hormone refractory breast cancer in a patient by administering to the patient an inhibitor of heregulin binding to ErbB3 or to ErbB2 / ErbB3 heterodimer, which inhibitor is an anti-ErbB3 antibody or an anti-ErbB2 antibody. The treatment methods can further comprise selecting a patient having a hormone refractory breast cancer and then administering the inhibitor to the patient. The treatment methods may also comprise administering an estrogen receptor antagonist, or an aromatase inhibitor to the patent and may at further comprise administering to the patient at least one additional anti-cancer agent that is not an ErbB3 inhibitor, an estrogen receptor antagonist, or an aromatase inhibitor to the patient in combination with the ErbB3 inhibitor.

The current invention relates to the development and methods of use of a recombinant agonistic antibody anti-human CD137, and glycosylation variants thereof. These antibodies act as anti-cancer agents and / or immune modulators that are effective in shrinking solid tumors or other cancerous indications and preventing their recurrence. The types of cancer for which the contemplated antibody is effective in treating also include leukemia and lymphoma. In a preferred imbodiment the recombinant antibodies of the current invention were produced in and purified from the milk of transgenic animals. In another preferred embodiment of the current invention the agonistic anti-CD137 antibodies of the invention can be conjugated to radionuclides for radioimmunodetection or radioimmunotherapeutic purposes, or conjugated to a toxin for enhanced therapeutic treatment of various cancers.

Anti-cancer agents and / or transforming growth factor beta (TGF-beta or TGFβ) antagonists are disclosed, where the agents and / or antagonists include a therapeutically effective amount of a combination of therapeutically active portions of sRII and therapeutically active portions of sRIII or a fusion polypeptide or protein comprising therapeutically active portions of sRII and therapeutically active portions of sRIII. Methods for preventing, treating and / or ameliorating the symptoms of cancer are also disclosed based on administering an effective amount of a composition of this invention.

Therapeutically effective 2,4,5-trisubstituted imidazole compounds are provided. Also provided are methods -of preparing the compounds and pharmaceutical compositions comprising the compounds alone or in combination with other agents. The present invention further provides for the use of the compounds as anti-cancer agents; wherein: R1 is aryl, substituted aryl, heterocycle, substituted heterocycle, heteroaryl, substituted heteroaryl or amino; R2 and R3 are independently aryl, substituted aryl, heterocycle, heteroaryl, substituted heterocycle, or substituted heteroaryl or R2 and R3 when taken together along with the carbon atoms they are attached to, form aryl or substituted aryl, and R4 is hydrogen, halogen, hydroxyl, thiol, lower alkyl, substituted lower alkyl, lower alkenyl, substituted lower alkenyl, lower alkynyl, substituted lower alkynyl, alkylalkenyl, alkyl alkynyl, alkoxy, alkylthio, aryl, aryloxy, amino, amido, carboxyl, aryl, substituted aryl, heterocycle, heteroaryl, substituted heterocycle, heteroalkyl, cycloalkyl, substituted cycloalkyl, alkylcycloalkyl, alkylcycloheteroalkyl, nitro, cyano or —S(O)o.2R wherein R is alkyl, substituted alkyl, aryl, substituted aryl, heterocycle, heteroaryl, substituted heterocycle, or substituted heteroaryl.

Benzodiazepine dimers having a structure represented bywherein X comprises a heteroaromatic moiety and is as further defined in the application; R1 isand the other variables in formulae (I), (Ia), and (Ib) are as defined in the application. Such dimers are useful as anti-cancer agents, especially when used in an antibody-drug conjugate (ADC).

Compounds useful as antiproliferative agents, including, for example, anticancer agents, are provided according to formula I: wherein: Ar, X, X1, g, R and R3 are as defined herein.

The present invention pertains to the design and application of a supramolecular hydrogel having a three-dimensional, selfassembling, elastic, network structure comprising non-polymeric, functional molecules and a liquid medium, whereby the functional molecules are noncovalently crosslinked. The functional molecules may be, for instance, anti-inflammatory molecules, antibiotics, metal chelators, anticancer agents, small peptides, surface-modified nanoparticles, or a combination thereof. The design of the hydrogel includes: 1) modifying functional molecules to convert them into hydrogelators while enhancing or maintaining their therapeutic properties and 2) triggering -the hydrogelation process by physical, chemical, or enzymatic processes, thereby resulting in the creation of a supramolecular hydrogel via formation of non-covalent crosslinks by the functional molecules. Applications of the present invention include use of the supramolecular hydrogel, for instance, as a biomaterial for wound healing, tissue engineering, drug delivery, and drug / inhibitor screening.

The present invention relates to a method of treating cancer in a subject in need thereof, by administering to a subject in need thereof a first amount of a histone deacetylase (HDAC) inhibitor such as suberoylanilide hydroxamic acid (SAHA), or a pharmaceutically acceptable salt or hydrate thereof, and a second amount of one or more anti-cancer agents, including Bortezomib. The HDAC inhibitor and the anti-cancer agent may be administered to comprise therapeutically effective amounts. In various aspects, the effect of the HDAC inhibitor and the anti-cancer agent may be additive or synergistic.

Compounds of formula I: wherein X is selected from oxygen, nitrogen and sulfur; n is 0 or 1; R1 is selected from alkyl, carboxylic acid, carboxylate, carboxamide, ester and combinations thereof; R2 is selected from alkyl, substituted alkyl, carboxylic acid, carboxylate, carboxamide, sulfonyl, sulfonamide and combinations thereof; and derivatives and metabolites thereof. Further provided are methods of using a compound of formula I to prevent and / or treat a subject having a condition characterized by unwanted cell proliferation. Also provided are pharmaceutical compounds comprising one or more compounds of formula I, or derivatives or pharmaceutically acceptable salts thereof.

Benzodiazepine dimers having a structure represented bywherein R1 iswherein the variables in formulae (I), (Ia), and (Ib) are as defined in the application. Such dimers are useful as anti-cancer agents, especially when used in an antibody-drug conjugate (ADC).

Compounds useful as antiproliferative agents, radioprotective agents and cytoprotective agents, including, for example, anticancer agents, are provided according to formula I: wherein ring A, ring B,,X, R1, R2, R3, a, and b are as defined herein.

The present invention provides a method for easily and inexpensively preparing a racemate or an optically-active 2-(1 -hydroxyethyl)-5-hydroxynaphtho[2,3-b]furan-4,9-dione in high yields, 2-acetyl-2,3-dihydro-5-hydroxynaphtho[2,3-b]furan-4,9-dione which is useful as an intermediate for preparing NFD, and an anticancer agent comprising 2-(1-hydroxyethyl)-5-hydroxynaphtho[2,3-b]furan-4,9-dione as an active ingredient.Said 2-(1-hydroxyethyl)-5-hydroxynaphtho[2,3-b]furan-4,9-dione is obtained in 4 or 5 steps by using comparatively inexpensive 5 -hydroxynaphthalene-1,4-dione (also referred to as juglone) as a starting material.

The bioavailability of an anticancer agent is enhanced when the anticancer agent is administered together with a pharmaceutical composition comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof.

The present invention provides methods for measuring the phosphorylation activity of Cdc7-ASK kinase complex by using as an indicator the level of phosphorylation at a phosphorylation site of MCM, which is a substrate of Cdc7-ASK kinase complex. The effects of test compounds on the phosphorylation activity of Cdc7-ASK kinase complex can also be evaluated based on these measurement methods. Compounds that inhibit this phosphorylation activity are useful as anti-cancer agents having superior specificity for cancer.