72 results about "Nornitrogen mustard" patented technology

This invention pertains to certain enzyme (CPG2) activated self-immolative nitrogen mustard prodrugs, which are useful in enzyme prodrug therapy (EPT), such as ADEPT and GDEPT, for the treatment of proliferative conditions, such as cancer, and which have the following formula:wherein: RN is independently C1-7alkyl; X1 is independently —I, —Br, or —Cl; X2 is independently —I, —Br, or —Cl; the group —N(CH2CH2X1)(CH2CH2X2) is independently attached at the 2-position or at the 4-position; each RG is independently —H or an ester substituent; n is independently an integer from 0 to 4; each RP, if present, is independently a phenyl substituent; m is independently an integer from 0 to 4; each RM, if present, is independently a mustard substituent; and pharmaceutically acceptable salts, solvates, amides, and esters thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds; such compounds and compositions for use in methods of treatment of the human or animal body by therapy; the use of such compounds and compositions for the manufacture of medicaments for the treatment of proliferative conditions; and the like.

A therapeutic agent for myeloma comprising a combined use of a nitrogen mustard anticancer agent and anti-IL-6 receptor antibody. Thus, a therapeutic agent for myeloma comprising anti-IL-6 receptor antibody for use in combination with a nitrogen mustard anticancer agent; a therapeutic agent for myeloma comprising a nitrogen mustard anticancer agent for use in combination with anti-IL-6 receptor antibody; and a therapeutic agent for myeloma comprising a nitrogen mustard anticancer agent and anti-IL-6 receptor antibody.

The present invention relates to a novel class of anti-cancer compounds which selectively target androgen receptor (AR)-expressing cancer cells, such as prostate cancer cells and breast cancer cells. These agents comprise an androgen receptor (AR) binding moiety, which selectively targets the compounds to (AR)-expressing cancer cells, and a cytotoxic ablating moiety, such as a nitrogen mustard moiety. The inherent high density expression of the androgen receptor in certain cancers, such as prostate cancer and breast cancer, is thus used as a tool to selectively increase the intracellular concentration of cytotoxic compounds, such as alkylating agents, e.g. DNA alkylating agents, by selectively targeting the agents to the AR-expressing cancer cells. These agents, either alone or in a composition, are thus useful for treating, delaying the progression of, treating the recurrence of, suppressing, inhibiting or reducing the incidence of cancers characterized by the presence of AR-expressing cells, such as prostate cancer. Accordingly, the present invention provides a) methods of selectively killing an (AR)-expressing cancer cell; b) methods of inducing apoptosis in an (AR)-expressing cancer cell; c) methods of treating a cancer characterized by the presence of AR-expressing cells in a subject; d) methods of delaying the progression of a cancer characterized by the presence of AR-expressing cells in a subject; e) methods of treating the recurrence of a cancer characterized by the presence of AR-expressing cells in a subject; f) methods of suppressing, inhibiting or reducing the incidence of a cancer characterized by the presence of AR-expressing cells in a subject; and g) methods of treating metastasis of a cancer characterized by the presence of AR-expressing cells in a subject; by administering to the subject or by contacting the cancer cells with a compound comprising an androgen receptor ligand moiety and an alkylating moiety, such as the novel compounds described herein.

The subject invention provides a potentially economically viable method for the preparation of hydrogen peroxide (H2O2) in deep eutectic solvents (DES). H2O2 is then used for the destruction of small to large quantities of sulfur and nitrogen mustards and lewisite, their homologous / analogues, and similar chemical warfare agents at ambient conditions in DES without producing any toxic by-products. Furthermore, H2O2 has been used for the destruction of small to large quantities of halogenated hydrocarbons, their homologous / analogues, and similar hazardous chemicals at ambient conditions. H2O2 can be formed by either the electrochemical reduction of oxygen in DES in the presence of water or by dissolving Group 1 (alkali metals) or Group 2 (alkaline earth metals) superoxides, e.g. potassium superoxide, in DES in the presence of water, with / without chemicals used for the enhancement of the solubility of the metal superoxide in the DES, e.g. crown ethers.

A composition and method for treatment of cancer. The composition for treating a skin disorder, comprising: a Nitrogen Mustard or an HX salt of the Nitrogen Mustard, wherein the Nitrogen Mustard or the HX salt of the Nitrogen Mustard is in a non-aqueous vehicle or carrier that does not include petrolatum or ethanol, wherein the non-aqueous vehicle or carrier that does not include petrolatum or ethanol does not include petrolatum or ethanol. The method comprises topically applying the composition of a Nitrogen Mustard or a HX salt of the Nitrogen Mustard to the affected skin, wherein the Nitrogen Mustard or the HX salt of the Nitrogen Mustard is in a non-aqueous vehicle or carrier that does not include petrolatum or ethanol, wherein the non-aqueous vehicle or carrier does not include petrolatum or ethanol.

A process for a stereoselective preparation of novel chiral nitrogen mustard derivatives useful in synthesizing optically active 1,4-disubstituted piperazines of formula: wherein R, Ar, and Q are defined as set forth herein, and intermediate compounds therefor. The 1,4-disubstituted piperazines act as 5HT1A receptor binding agents useful in the treatment of Central Nervous System (CNS) disorders.

The invention discloses a hydrogen peroxide-responsive nitrogen mustard anti-tumor pro-drug and a preparation method thereof, and belongs to the field of pharmaceutical chemistry. The compound contains an alpha-ketoamide structure and a nitrogen mustard structure, can rapidly respond to H2O2, can be used as the nitrogen mustard anti-tumor pro-drug, has good response effect to H2O2, has high cell selectivity and small toxic and side effects, provides an effective, safe and highly selective anti-tumor drug, enriches the types of nitrogen mustard anti-tumor drugs, and has a good market prospect.

The invention discloses a thiosulfate silvering additive, a preparation method thereof and electroplate liquid containing the same. The thiosulfate silvering additive comprises 12-18 g / L of lauryl sodium sulfate, 3-5 g / L of polyethylene glycol, 10-13 g / L of nitrogen mustard, 5-10 g / L of cumin, 250-350 g / L of 1,10-phenanthroline monohydrate, 50-100 g / L of dimercaprol dimercaptopropanol, 50-100 g / Lof mercaptoethylamine, 100-150 g / L of ethylene glycol tetraacetic acid (EGTA) and the balance water. The additive provided by the invention enables the dispersity, the stability and the electroplatingperformance of the electroplate liquid to be quite remarkably improved, the pH value does not need to be adjusted repeatedly in the electroplating process, meanwhile, the performance including the smoothness, the adhesive force, the glossiness, the anti-tarish performance and the like of a silvering coating are remarkably improved, the thickness of the coating is further reduced, and phenomena such as fracturing do not exist; and the electroplate liquid provided by the invention does not contain cyanide, the mirror surface of the coating is bright, small in brittleness, good in adhesive force, flat in surface, bright, good in anti-tarish performance and high in heat resistance, application to the multiple fields of decorative electroplating, functional electroplating and the like can be achieved, preplating is not needed, and the bonding force can also be guaranteed.

Provided are stable compositions comprising alkylating agents, including nitrogen mustards, that are suitable for topical use, and methods for treating skin disorders comprising topically administering the compositions.