128 results about "Anti-Carcinogenic Agents" patented technology

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.

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.

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.

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 by

wherein X comprises a heteroaromatic moiety and is as further defined in the application; R¹ is

and 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).

Benzodiazepine dimers having a structure represented by

wherein R¹ is

wherein 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 invention discloses quinazoline derivatives serving as irreversible tyrosine kinase inhibitors, and use of the derivatives as inhibitors for human epidermal growth factor receptor (EGFR) mutant T790M and anticancer agents. The invention also relates to a preparation method for the quinazoline derivatives, and a medicinal composition containing the quinazoline derivatives.

The invention provides compounds of the formula: (I) having protein kinase B inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms extending between R¹ and NR²R³ and a maximum chain length of 4 atoms extending between E and NR²R³, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group A may optionally bear one or more substituents selected from oxo, fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom a with respect to the NR²R³ group and provided that the oxo group when present is located at a carbon atom a with respect to the NR²R³ group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; R¹ is an aryl or heteroaryl group; and R², R³, R⁴ and R⁵ are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds, methods for preparing the compounds and their use as anticancer agents.

Compounds of the general formula):

processes for the preparation of these compounds, compositions containing these compounds, and the uses of these compounds.

A single treatment catheter is provided for delivery of brachytherapy radiation in combination with intratumoral injection into tumor tissue with a single skin and tumor insertion site. The catheter also enables precise delivery of anti-cancer agents, such as immunotherapy or other medical substances, to specific locations within the tumor with radiographic confirmation of the injection delivery area and location.

There are provided compounds of the formula

wherein R₁ and R₂ are as described herein. The compounds are useful as anticancer agents.

The present invention provides, inter alia, methods, kits, and pharmaceutical compositions for treating or ameliorating the effects of a cancer in a subject in need thereof. The method includes administering to the subject an effective amount of (i) a first anti-cancer agent, which is BVD 523 or a pharmaceutically acceptable salt thereof and (ii) a second anti-cancer agent, which is a type 2 MEK inhibitor, or other MEK inhibitors, or pharmaceutically acceptable salts thereof, to treat or ameliorate the effects of the cancer. Additional methods for effecting cancer cell death are also provided.

Sulfone is an important drug and bioactive compound. Sulfone is widely used as a medicament, such as a medicament gamma-secretase inhibitor for preventing Alzheimer's disease, and is widely applied tobioactive compounds, natural products and agricultural chemicals, such as currently popular herbicide mesotrione. Sulfone is also most often used as an intermediate for organic synthesis. On the other hand, a chalcogen heterocyclic stent has biological activity, such as antitumor drugs and antiproliferative drugs. As is well-known, thiophene, furan and selenium compounds have a variety of biological activities, such as anti-inflammatory agents, anti-HIV PR inhibitors, NQO2 inhibitors, and anticancer agents. The invention develops a simple, convenient and efficient Bronsted acid, i.e., sulfuric acid and catalyzed three components react in water to synthesize aryl(chalcogen-heteroaryl)methyl sulfone, the yield is good to be very high, and the substrate range is wide. The synthesis method isenvironment-friendly and economic, and does not need metal catalysis. The sulfone product can be effectively converted into bactericide analogues and aryl heteroaryl ketones.

The invention provides compounds of the formula: (I) having protein kinase B inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms extending between Rand NR<2>R<3> and a maximum chain length of 4 atoms extending between E and NR<2>R<3>, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the inker group A may optionally bear one or more substituents selected from oxo, fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom a with respect to the NR<2>R<3> group and provided that the oxo group when present is located at a carbon atom a with respect to the NR<2>R<3> group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; R is an aryl or heteroaryl group; and R<2>, R<3>, R<4> and R<5> are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds, methods for preparing the compounds and their use as anticancer agents.