40 results about "Lyase inhibitor" patented technology

Methods and compositions for treating cancer are described herein. More particularly, the methods for treating cancer comprise administering a 17α-hydroxylase / C17,20-lyase inhibitor, such as abiraterone acetate (i.e., 3β-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 17α-hydroxylase / C17,20-lyase inhibitor, and at least one additional therapeutic agent, such as an anti-cancer agent or a steroid.

The present invention provides compounds of Formula (I) and (II), or a pharmaceutically acceptable salts thereof,where R53, R54, p, q, and n are as defined herein. The compounds of the present invention have been found to be useful as 17α-hydroxylase / C17,20-lyase inhibitors.

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 invention describes methods of treating cancer in which a therapeutically-effective amount of a 17α-hydroxylase / C17,20-lyase inhibitor is administered to a subject in need thereof, including a subject with a refractory cancer and / or a subject currently undergoing another cancer treatment, wherein the 17α-hydroxylase / C17,20-lyase inhibitor is administered in combination with a therapeutically-effective amount of at least one additional therapeutic agent, including, but not limited to, another anti-cancer agent or a steroid.

The present invention provides methods and compositions for treating cancers using a combination of a CYP 1 7 inhibitor and an additional therapeutic agent which modulates the PBK / Akt / mTOR pathway. In one aspect, the invention provides methods for the treatment of a disorder in a human subject. In some embodiments, the disorder is a neoplastic disorder. In some embodiments, the neoplastic disorder is a cancer. In some embodiments, the method comprises administering to said subject a 17a-hydroxylase / C17,20-lyase inhibitor (CYP17 inhibitor) and an additional agent, wherein the additional agent is a PBK inhibitor and / or mTOR inhibitor.

The present invention relates to a combination which comprises (a) a phosphatidylinositol 3-kinase inhibitor selected from the group consisting of a compound of formula (I) or a compound of formula (II), or pharmaceutically acceptable salt thereof, (b) a 17α-Hydroxylase / C17,20-lyase inhibitor (CYP17 inhibitor), specifically abiraterone acetate and 1-(2-Chloro-pyridin-4-yl)-3-(4-methyl-pyridin-3-yl)-imidazolidin-2-one or pharmaceutically acceptable salt thereof, for simultaneous, separate or sequential use for the treatment of a tumor disease; a pharmaceutical composition comprising such combination; use of such combination for the treatment of a tumor disease; a commercial package or product comprising such combination; and to a method of treating a patient having a tumor disease comprising administration of said combination to a patient in need thereof.

The present invention relates to a method for the prevention or treatment of certain breast cancers or ovarian cancer comprising administering to a patient in need thereof of a therapeutically effective amount of a 17,20-lyase inhibitor, wherein the breast cancer or ovarian cancer is estrogen receptor (ER) negative.

The present invention provides an industrially advantageous process for producing a steroid C17,20 lyase inhibitor represented by the general formula (I): and a Reformatsky reagent in a stable form suitable for the process. In the present invention, a compound represented by the general formula (I) is produced by reducing a specific β-hydroxy ester compound derivative or a salt thereof obtained from a specific carbonyl compound in a Reformatsky reaction in the presence of a metal hydride complex and a metal halide, and then subjecting it to a ring-closing reaction. In the above Reformatsky reaction, it is useful to use a stable solution of a compound represented by the general formula BrZnCH2COOC2H5 or a crystal of the compound which is represented by the formula (BrZnCH2COOC2H5.THF)2.

The present invention provides cancer treatment preparations of excellent targetability. The sugar chain-modified liposomes of the present invention, which contain an aromatase inhibitor, anti-androgenic agent, lyase inhibitor, GnRH agonist, GnRH antagonist, anti-angiogenic agent, tyrosine kinase inhibitor, serine-threonine kinase inhibitor, antibody having an anticancer activity, ansamitocin, capecitabine, celmoleukin, docetaxel hydrate, gemcitabine hydrochloride, oxaliplatin, prednisolone, tegafur-uracil mixtures, zinostatin stimalamer or arsenic trioxide may be used as cancer treatment preparations having an excellent targetability.

Described herein are methods and compositions for the treatment of prostate cancer in a subject in need thereof. The prostate cancer may be a castration resistant and an androgen receptor antagonist-resistant prostate cancer. The methods may comprise administering to the subject a CYP17-lyase inhibitor of Formula II.

The invention relates to purification of an intact, non-degraded macromolecule from a biological mixture comprising the macromolecule in the presence of its lytic enzyme. The method comprises providing the biological mixture as a heterogeneous mixture comprising the lytic enzyme, at least partially, in soluble form and the macromolecule, at least partially, in non-soluble form; batch-wise contacting the heterogeneous mixture with an immobilized inhibitor of the lytic enzyme; increasing the solubility of the macromolecule in the mixture; and removing the immobilized inhibitor from the mixture.

Provided herein are compositions, systems, and methods for treating a disease, such as kidney and / or cardiovascular disease, with an agent that reduces the production of trimethylamine (TMA) or trimethylamine-n-oxide (TMAO) in a subject. In certain embodiments, the agent is: i) 3,3-dimethyl-1-butanol (DMB) or a DMB derivative or related compound, ii) acetylsalicylic acid or derivative thereof (e.g., with an enteric coating for delivery to the colon and / or cecum); iii) a flavin monooxygenase 3 (FMO3) inhibitor; iv) a gut TMA lyase inhibitor; v) an antibiotic or antimicrobial; vi) a probiotic or prebiotic; vii) an antiplatelet agent; or viii) a TMA and / or TMAO sequestering agent.

Provided herein are compositions, systems, and methods for treating a disease, such as kidney and / or cardiovascular disease, with an agent that reduces the production of trimethylamine (TMA) or trimethylamine-n-oxide (TMAO) in a subject. In certain embodiments, the agent is: i) 3,3-dimethyl-1-butanol (DMB) or a DMB derivative or related compound, ii) acetylsalicylic acid or derivative thereof (e.g., with an enteric coating for delivery to the colon and / or cecum); iii) a flavin monooxygenase 3 (FMO3) inhibitor; iv) a gut TMA lyase inhibitor; v) an antibiotic or antimicrobial; vi) a probiotic or prebiotic; vii) an antiplatelet agent; or viii) a TMA and / or TMAO sequestering agent.

The present invention provides an industrially advantageous process for producing a steroid C17,20 lyase inhibitor represented by the general formula (I):and a Reformatsky reagent in a stable form suitable for the process.In the present invention, a compound represented by the general formula (I) is produced by reducing a specific β-hydroxy ester compound derivative or a salt thereof obtained from a specific carbonyl compound in a Reformatsky reaction in the presence of a metal hydride complex and a metal halide, and then subjecting it to a ring-closing reaction. In the above Reformatsky reaction, it is useful to use a stable solution of a compound represented by the general formula BrZnCH2COOC2H5 or a crystal of the compound which is represented by the formula (BrZnCH2COOC2H5.THF)2.

Described herein are methods and compositions for the treatment of prostate cancer in a subject in need thereof. The prostate cancer may be a castration resistant and an androgen receptor antagonist-resistant prostate cancer. The methods may comprise administering to the subject a CYP17-lyase inhibitor of Formula II.

The invention relates to purification of an intact, non-degraded macromolecule from a biological mixture comprising the macromolecule in the presence of its lytic enzyme. The method comprises providing the biological mixture as a heterogeneous mixture comprising the lytic enzyme, at least partially, in soluble form and the macromolecule, at least partially, in non-soluble form; batch-wise contacting the heterogeneous mixture with an immobilized inhibitor of the lytic enzyme; increasing the solubility of the macromolecule in the mixture; and removing the immobilized inhibitor from the mixture.

A novel combination comprising a 17 α-hydroxylase / C17,20 lyase inhibitor, for example: (3β)-17-(pyridin-3-yl)androsta-5, 16-dien-3-ol or a pharmaceutically acceptable salt or ester thereof, and an AKT inhibitor, for example: N-{(1 S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide, or a pharmaceutically acceptable salt thereof, and optional additional antineoplastic agents; pharmaceutical compositions comprising the same and methods of using such combinations and compositions in the treatment of conditions in which the inhibition of 17 α-hydroxylase / C17,20 lyase and / or AKT inhibition is beneficial, e.g., cancer.

The invention relates to microorganisms, in particular to a method for screening a trimethylamine lyase inhibitor by utilizing microorganisms. The method for screening the trimethylamine lyase inhibitor by utilizing microorganisms is characterized by comprising the following steps: inoculating a specific culture medium only containing cholineinoculator with Klebsiella pneumoniae ATCC 13883 servingas an indicator; adding a substance to be screened into the culture medium at a concentration lower than the minimum inhibitory concentration, and carrying out anaerobic culture for 12-48 hours at 37DEG C; and taking a culture solution, determining the content of trimethylamine, taking a culture solution without the to-be-detected substance as a contrast, and indicating that the substance can inhibit microorganisms from converting choline to generate trimethylamine and is a trimethylamine lyase inhibitor when the content of trimethylamine is lower than that of a control group; The method hasthe advantages of quickness, simplicity, convenience, easiness in operation, low reagent demand, capability of performing high-throughput screening and accurate result.

The invention provides application of a compound acting on a choline or trimethylamine oxide (TMAO) related target in preparation of a medicine for preventing and / or reversing clopidogrel resistance. The compound comprises one or more of an NOX inhibitor, an ROS scavenger, an Nrf2 inhibitor and an enteric microorganism choline TMA lyase inhibitor. The invention systematically explores the influence of choline or TMAO on the metabolic activation and antiplatelet effect of clopidogrel and various intervention mechanisms thereof, and provides a brand new treatment target and a prevention and treatment strategy for clinically and effectively overcoming clopidogrel resistance associated with choline or TMAO.

Provided are compounds and methods useful for the preparation of compounds useful as inhibitors of [beta]-site amyloid precursor protein (APP)-cleaving enzyme.

The present invention provides the application of compounds acting on choline or trimethylamine oxide (TMAO)-related targets in the preparation of drugs for preventing and / or reversing clopidogrel resistance, said compounds comprising NOX inhibitors, ROS scavengers, Nrf2 One or more of inhibitors and intestinal microbial choline TMA lyase inhibitors. The present invention systematically explores the effects of choline or TMAO on the metabolic activation and antiplatelet effects of clopidogrel and its various intervention mechanisms, and provides a new treatment for effectively overcoming clopidogrel resistance associated with choline or TMAO in clinical practice Targets and prevention strategies.

The invention provides a method of high-throughput sorting of high expression protein-producing cell, which utilizes linking a protein and a transmembrane domain with a self-processing cleavage site and regulating the secretion of the protein or expression of protein on the cell membrane by adding self-processing cleavage enzyme inhibitor. Then, the high expression cell line can be high-throughput sorted by a detection technique. The invention also provides a recombinant nucleotide sequence and a vector used in the method and a cell sorted by the method.

The invention discloses application of a natural coumarin compound in preparation of an ATP (adenosine triphosphate) citrate lyase inhibitor. The structural formula of the natural coumarin compound is as shown in formula (1). The compound fraxidin is separated from 95% ethanol extract of branches and leaves of glycosmis mollissima for the first time. Multiple pharmacological test studies show that the compound has shown ACL inhibitory activity, and can be used for preparing drugs for treating ACL-mediated diseases or used as a lead compound of the drugs.

The invention provides a method of high-throughput sorting of high expression protein-producing cell, which utilizes linking a protein and a transmembrane domain with a self-processing cleavage site and regulating the secretion of the protein or expression of protein on the cell membrane by adding self-processing cleavage enzyme inhibitor. Then, the high expression cell line can be high-throughput sorted by a detection technique. The invention also provides a recombinant nucleotide sequence and a vector used in the method and a cell sorted by the method.

The present invention mainly aims to provide a drug for the prophylaxis or treatment of androgen-independent prostate cancer, which is highly useful as a pharmaceutical agent. The present invention provides a drug for the prophylaxis or treatment of androgen-independent prostate cancer, containing a steroid C17,20 lyase inhibitor, particularly, a compound represented by the formula (I):wherein n is an integer of 1 to 3, and Ar is an aromatic ring optionally having substituent(s), or a salt thereof or a prodrug thereof.