254 results about "Desmethyl" patented technology

A methanol carbonylation system 10 includes an absorber tower 75 adapted for receiving a vent gas stream and removing methyl iodide therefrom with a scrubber solvent, the absorber tower being coupled to first and second scrubber solvent sources 16, 56 which are capable of supplying different first and second scrubber solvents. A switching system including valves 90, 92, 94, 96, 98 alternatively provides first or second scrubber solvents to the absorber tower and returns the used solvent and sorbed material to the carbonylation system to accommodate different operating modes.

The present invention involves the use of desmethyl tocopherols such as gamma tocopherol for the protection of cardiovascular tissue from nitrative stress. While mechanisms other than scavenging of reactive nitrogen species may be involved, desmethyl tocopherols exhibit significant protection and may be utilized to treat or help prevent cardiovascular particularly arterial vascular disease. The desmethyl tocopherols may be administered dietarily or parenterally when a more direct dosage is desired. Both routes may be utilized together or separately to optimize therapeutic and prophylactic benefits. The lessening of damage induced by reactive nitrogen species leads to the lessening of arterial blockage in thrombosis.

The invention discloses a blautia sp. AUH-JLD56 and an application thereof in the conversion of arctigenin, and belongs to the technical field of bacterium. The preservation number of blautia sp. AUH-JLD56 is CGMCC No. 8032. The application of blautia sp. AUH-JLD56 comprises following steps: (1) culture of bacterium strain AUH-JLD56; (2) co-culture of a substrate, namely a coarse product of arctigenin, and a bacterium strain AUH-JLD56 and separation and purification of metabolite. The bacterium strain AUH-JLD56 can high effectively convert a coarse product of arctigenin in the traditional Chinese medicine actium lappa to 3'-demethylated-arctigenin, solves the 3'-demethylated-arctigenin resource shortage problem, and lays a foundation for researching and developing microorganism metabolite of pharmacological active substance in actium lappa.

2-Desmethyl ansamycins having a structure according to formula I, where R¹, R², R³, R⁴, R⁵ and R⁶ are as defined herein, and other 2-desmethyl ansamycins are useful as antiproliferative agents.

The invention relates to a compound of Formula (I): (A′)_x-(A)-(B)-(Z)-(L)-(D), wherein: (A) is heteroaryl or aryl; each (A′), if present, is independently chosen from aryl, arylalkoxy, arylalkyl, heterocyclyl, aryloxy, halo, alkoxy, haloalkyl, cycloalkyl, haloalkoxy, and cyano, wherein each (A′) is substituted with 0, 1, 2, or 3 substituents independently chosen from halo, haloalkyl, aryl, arylalkoxy, alkyl, alkoxy, cyano, sulfonyl, amido, and sulfinyl; X is 0, 1, 2, or 3; (B) is a cyclopropyl ring, wherein (A) and (Z) are covalently bonded to different carbon atoms of (B); (Z) is —NH—; (L) is chosen from —CH₂CH₂—, —CH₂CH₂CH₂—, and —CH₂CH₂CH₂CH₂—; and (D) is chosen from —N(—R1)—R2, —O—R3, and —S—R3, wherein: R1 and R2 are mutually linked to form a heterocyclic ring together with the nitrogen atom that R1 and R2 are attached to, wherein said heterocyclic ring has 0, 1, 2, or 3 substituents independently chosen from —NH₂, —NH(C₁-C₆ alkyl), —N(C₁-C₆ alkyl)(C₁-C₆ alkyl), alkyl, halo, cyano, alkoxy, haloalkyl, and haloalkoxy, or R1 and R2 are independently chosen from —H, alkyl, cycloalkyl, haloalkyl, and heterocyclyl, wherein the sum of substituents on R1 and R2 together is 0, 1, 2, or 3, and the substituents are independently chosen from —NH₂, —NH(C₁-C₆ alkyl), —N(C₁-C₆ alkyl)(C₁-C₆ alkyl), and fluoro; and R3 is chosen from —H, alkyl, cycloalkyl, haloalkyl, and heterocyclyl, wherein R3 has 0, 1, 2, or 3 substituents independently chosen from —NH₂, —NH(C₁-C₆ alkyl), —N(C₁-C₆ alkyl)(C₁-C₆ alkyl), and fluoro; or an enantiomer, diastereomer, or mixture thereof, or a pharmaceutically acceptable salt or solvate thereof. The compounds of the invention show inhibitory LSD1 activity, which makes them useful in the treatment or prevention of diseases such as cancer.

The present invention provides a method for the N-demethylation and N-functionalization of an N-methylated heterocycle such as a morphine alkaloid or tropane alkaloid. The method comprises reacting the heterocycle with an functionalization agent in the presence of a transition metal catalyst in air or in the presence of an oxidant.

The invention relates to desmethyldoxepin, isomers of desmethyldoxepin, and pharmaceutically acceptable salts and prodrugs of desmethyldoxepin; compositions containing the same, and the use of any of the aforementioned for the treatment of sleep disorders.

The present invention relates to production of polyketides and other natural products and to libraries of compounds and individual novel compounds. Therefore in aspect the present invention provides 17-desmethylrapamycin and analogues thereof, methods for their production, including recombinant strains, and isolation and uses of the compounds of the invention. In a further aspect the present invention provides for the use of 17-desmethylrapamycin and analogues thereof in the induction or maintenance of immunosuppression, the stimulation of neuronal regeneration or the treatment of cancer, B-cell malignancies, fungal infections, transplantation rejection, graft vs. host disease, autoimmune disorders, diseases of inflammation vascular disease and fibrotic diseases, and in the regulation of wound healing.

A method of synthesizing 4-R-substituted anthracyclines and their corresponding salts from 4-demethyldaunorubicin includes the steps of treating 4-demethyldaunorubicin with a sulfonylating agent to form 4-demethyl-4-sulfonyl-R₃-daunorubicin. 4-Demethyl-4-R₃-sulfonyl-daunorubicin is then subject to a reducing agent in the presence of a transition metal catalyst in a temperature range of about 30° C. to about 100° C. in a polar aprotic solvent in an inert atmosphere. Protected 4-demethoxy-4-R-daunomycin then undergoes hydrolysis in a basic solution to form the 4-R-substituted anthracyclines. The novel method lacks the step of forming a stereospecific glycoside bond between aglycone and aminoglycoside. The method also increases the yield of the final product up to 30 to 40%.

The invention discloses macrocyclic and cage-like molecules based on biphenylarene and derivatives of the macrocyclic and cage-like molecules as well as synthetic methods and applications of the macrocyclic and cage-like molecules and the derivatives. A series of novel macrocycles are obtained mainly by performing a reaction on bis(2,4-dialkoxyphenyl)arenes (naphthalene, anthracene, pyrene, porphyrin and the like) or tris(2,4-dialkoxyphenyl)arenes (benzene, sym-tribenzobenzene) and paraformaldehyde under the catalysis of a Lewis acid in high yield. In addition, perhydroxybiphenylarenes (quaterphenyl trimer, naphthalene dimer and the like) can be obtained by performing demethylation, a plurality of water-soluble derivatives can be obtained by performing further modification, and the derivatives show good bonding ability to guest molecules (viologen and the like); and moreover, functional groups introduced into the framework make the biphenylarene have excellent adsorption and separationability and photophysical properties. The compounds, derivatives and methods provided by the invention have the following advantages: raw materials of the biphenylarene are commercially available, the synthesis is simple and convenient, the yield is high, and the modification is convenient, so that the compounds and the derivatives have broad application prospects in gas adsorption and separation, performance improvement of light-emitting materials, and adsorption of water-soluble toxic substances.

Compounds having the structure of formula I

wherein R¹, R², R³, R⁴, R⁵, and R⁶ are as defined herein, are prokinetic agents and can be used to treat disorders of gastric motility.

The invention relates to a preparation method for a cyclopropylamine spiro(hetero)cyclic compound and a composition containing the same, and application of the compound and the composition as an inhibitor for human lysine-specific demethylase (LSD1). The inhibitor is the cyclopropylamine spiro(hetero)cyclic compound as shown in a formula (I) which is described in the specification, or a pharmaceutically acceptable salt, predrug, solvate, polymorphic crystal or stable isotope derivative thereof. The compound can be used for treating or preventing diseases related to human lysine-specific demethylase, e.g., cancers and nerve diseases.

A novel salt of O-desmethyl venlafaxine is provided, O-desmethylvenlafaxine succinate. Pharmaceutical compositions, dosage forms and methods of use are also provided.

There is provided a method for the synthesis of norbuprenorphine, and ultimately buprenorphine, utilizing oripavine as the starting material. Conventional methods of producing buprenorphine utilize thebaine as the starting material, requiring an O-demethylation step, typically a low to moderate yield transformation. The present use of oripavine as a starting material does not require an O-demethylation step, since the oripavine molecule lacks an O-3 methyl group.

The invention belongs to the field of medicinal chemistry, and discloses a pyrimidine and triazole containing compound and a preparation method and application thereof in preparation of anti-cancer medicine with lysine specific demethylase 1 (LSD1) being a target. The general formula of the compound is shown in the drawing I. In-vitro LSD1 enzyme inhibition activity experiments prove that by inhibiting LSD1 activity, the compound has obvious inhibiting and killing effects on kinds of cancer cells and can be applied to preparation of the anti-cancer medicine as a further developed lead compound.

The invention discloses a preparation method of a compound 19-desmethyl-4-androstene-3,17 diketone, comprises the following step of by taking compounds of 5alpha-chloro-3beta-hydroxy-6beta and 19beta-epoxy-androstane-17-ketone as raw materials, and carrying out oxidation reaction on the compounds of 5alpha-chloro-3beta-hydroxy-6beta and 19beta-epoxy-androstane-17-ketone as well as an intermediate compound 19-hydroxy-4-androstene-3,17-diketone with N-halogenated amide oxidant in a mixed solution of an organic solvent and an alkaline buffer solution in the presence of a catalytic amount of 2,2,6,6-tetramethylpiperidine-N-oxide (TENPO) in the mild condition. In the two steps of oxidation reaction, the catalytic amount of 2,2,6,6-tetramethylpiperidine-N-oxide and the N-halogenated amide oxidant are both adopted to replace a mixed solution of chromium trioxide, sulfuric acid and water. In the oxidation method, without using the chromium trioxide, the use of carcinogenic substances are avoided being used, limitation by environmental protection is avoided and a great amount of wastes containing heavy metals in preparation are avoided being generated and accumulated, thereby no money and labor is consumed for removing the wastes.

A novel salt of O-desmethylvenlafaxine, O-desmethylvenlafaxine formate, is provided. Pharmaceutical compositions, dosage forms and methods of use are also provided.

The present invention provides transdermal drug delivery devices (i.e., patches) comprising O-desmethylvenlafaxine (ODV), a selective serotonin and norepinephrine re-uptake inhibitor, or a pharmaceutically acceptable salt thereof, which, among other, offer the advantage of eliminating or reducing the adverse side effects associated with the oral administration of ODV. Also provided are methods of preparing and using these transdermal delivery systems for the treatment of depression, anxiety disorders, vasomotor symptoms and pain.