15 results about "Antiproliferative Agents" patented technology

Disclosed herein are novel cytotoxic compounds, and cytotoxic conjugates comprising these cytotoxic compounds and cell binding agents. More specifically, the present disclosure relates to novel camptothecin derivatives thereof, intermediates thereof, conjugates thereof, and pharmaceutically acceptable salts thereof, which are useful as medicaments, particularly as antiproliferative agents (anticancer agents).

The present invention is related with the use of 1,3,5-triaza-7-phosphaadamantane (PTA) and derivatives thereof of formula (I) as active antiproliferative agents for photodynamic therapy (PDT) and Photoactivated Chemotherapy (PACT). The invention is further related with new compounds of formula (I').

To provide therapeutic methods for treating kidney diseases.SOLUTION: There are provided therapeutic methods for treating kidney diseases, using compounds of Formula (A) in combination with a second therapeutic agent. (In the formula: each R is independently selected from a group comprising H, alkyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, halogen, -OH, CN, cycloalkyl, -O-alkyl, -O-cycloalkyl, -O-aryl, -aryl-O-aryl, -CF3, -C(H)F2, alkylene-CF3, alkylene-C(H)F2, -SO2-alkyl, -O-alkylene-O-alkyl, -heterocyclyl-L-R4, and heteroaryl-L-R4; and only one R is -heterocyclyl-L-R4 or -heteroaryl-L-R4). The second therapeutic agent is selected from an immunomodulator, a calcineurin inhibitor, a renin angiotensin aldosterone system inhibitor, an antiproliferative agent, an alkylating agent, and the like.SELECTED DRAWING: None

The present invention relates to the field of chemistry and biochemistry and in particular to the novel anticancer compounds, more particularly to antiproliferative agents and microtubule polymerization inhibitors. Even more particularly, the invention relates to novel analogs of natural antimitotic agent diazonamide A and to salts, pharmaceutical compositions, conjugates and a process of manifacture thereof and the potential use of the novel compounds for treatment of melanoma. A new series of compounds with high activity against cancer cells has been developed. The most active compounds from the series show cytotoxicity against several cancer cell lines with IC50 = 12–90 nM.

Devices, systems, and methods are provided including a structure having one or more surfaces configured for internal use within a patient's body and one or more therapeutic compositions comprising one or more active substances including a direct factor Xa inhibitor, and a direct factor IIa inhibitor disposed in or on the structure. The structure is configured to be positioned adjacent an injury site in the patient's body. The one or more active substances optionally include an anti-proliferative agent. The therapeutic composition is formulated to release the one or more active substances to the injury site to provide one or more of inhibit clot formation, promote clot dissolution, inhibit or dissolute inflammation, inhibit vessel injury, increase time before clotting, and / or inhibit cell proliferation.

A unitary product is disclosed to prevent and / or treat stenosis in a blood vessel. It is tube or wrap of appropriate dimensions to be slid over or wrap a blood vessel. The devices described herein comprise a tube or wrap comprising an effective amount of antiproliferative agent to mitigate and / or treat stenosis. They are constructed of a biocompatible, preferably biodegradable material carrying an amount of an antiproliferative drug which may be rapamycin or a rapamycin analogue with similar antiproliferative activity to effectively address the stenosis.

The invention relates to compounds according to formula (I)and pharmaceutically acceptable derivatives thereof for use as novel inhibitors of Mouse Double Minute 2 (MDM2) activity by inhibiting interactions between MDM2 and its natural negative regulator, p53. Pharmaceutical compositions containing a compound of Formula (I), or a derivative thereof, including compositions that also contain one or more additional antiproliferative agents, can be used in methods of treating proliferative diseases, including various cancers.

Disclosed are compounds comprising alkylating moieties, such as pyrrolobenzodiazepines (PBDs, comprising three fused 6-7-5-membered rings), C2-substituted PBDs (including C2-endo, C1 / C2-endo, and C2 / C3-endo PBDs), pyrridinobenzodiazepines (PDDs, comprising three fused 6-7-6-membered rings), indolinobenzodiazapenes (IBDs, comprising four fused 6-7-5-6 membered rings), and tetrahydroisoquinolinebenzodiazepines (QBDs, comprising four fused 6-7-6-6 membered rings), or a pharmaceutically acceptable salt thereof. In particular, the disclosed compounds, or a pharmaceutically acceptable salt thereof, may comprise a guanine alkylating moiety linked to an aromatic group. The disclosed compounds are useful as medicaments, in particular as anti-proliferative agents.

To provide therapeutically effective camptothecin derivatives that have increased solubility, potency, lactone stability, and bioavailability.SOLUTION: Disclosed herein are novel cytotoxic compounds, and cytotoxic conjugates comprising these cytotoxic compounds and cell-binding agents. More specifically, this disclosure relates to novel camptothecin derivatives thereof, intermediates thereof, conjugates thereof, and pharmaceutically acceptable salts thereof, which are useful as medicaments, in particular as anti-proliferative agents (anticancer agents). In one aspect, the invention provides a compound of Formula I, or a pharmaceutically acceptable salt thereof: Z-L1-D (Formula I), wherein: D is represented by the following structural formula (R1 is -F, -CH3, or -CF3; R2 is -H, -F or the like; -L1-Z is -H, -(C1 to C6 alkylene)-H or the like).SELECTED DRAWING: None

A method of treating a urethral stricture includes: dilating a stricture in a urethra; applying an anti-proliferative or steroidal agent to a luminal wall of the urethra near the stricture; deploying a stent or scaffold within the urethra to maintain contact between the anti-proliferative or steroidal agent and the luminal wall of the urethra near the stricture; leaving the stent or scaffolding within the urethra, thereby allowing fluid to pass through a lumen of the stent or scaffolding; and removing the stent or scaffolding after a therapeutic time period.

Subject matter of the present invention is a white crystalline polymorph A of the Ca salt of a compound according to formula I or a solvate and / or a hydrate thereof with a molar ratio of a compound according to formula I or a solvate and / or a hydrate thereof to calcium which is 2±0.3. Subject matter of the present invention is in particular a compound according to formula I or a solvate and / or a hydrate thereof which is characterized by an X-ray powder diffraction pattern having characteristic peaks expressed in degrees 2theta at ±0.2 of the values shown below: 2 theta=5.91°, 9.64°, 16.78°, 17.81°, 19.81°, 25.41° In particular the invention refers to new polymorphs of calcium salts of the Ca salt of a compound according to formula I or a solvate and / or a hydrate thereof which inhibits dihydroorotate dehydrogenase (DHODH), a process for their manufacture, pharmaceutical compositions containing them and to their use for the treatment and prevention of diseases, in particular their use in diseases where there is an advantage in inhibiting dihydroorotate dehydrogenase (DHODH).

A method of treating a urethral stricture includes: dilating a stricture in a urethra; applying an anti-proliferative or steroidal agent to a luminal wall of the urethra near the stricture; deploying a stent or scaffold within the urethra to maintain contact between the anti-proliferative or steroidal agent and the luminal wall of the urethra near the stricture; leaving the stent or scaffolding within the urethra, thereby allowing fluid to pass through a lumen of the stent or scaffolding; and removing the stent or scaffolding after a therapeutic time period.

A unitary product is disclosed to prevent and / or treat stenosis in a blood vessel. It is tube or wrap of appropriate dimensions to be slid over or wrap a blood vessel. The devices described herein comprise a tube or wrap comprising an effective amount of antiproliferative agent to mitigate and / or treat stenosis. They are constructed of a biocompatible, preferably biodegradable material carrying an amount of an antiproliferative drug which may be rapamycin or a rapamycin analogue with similar antiproliferative activity to effectively address the stenosis.