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274 results about "Desmethyl" patented technology

Desmethyl is a term used in organic chemistry to refer to a methyl group that has been removed. Examples include desmethyltramadol and desmethylsertraline.

Methanol carbonylation system having absorber with multiple solvent options

ActiveUS20090270651A1Reduced capitalWeaken energyProductsGas treatmentMeth-Carbonylation
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.
Owner:CELANESE INT CORP

Inhibitors of histone demethylases

Compounds of the formIn which Q is selected from —CH═NR12, —W, —CH2NHR13, —CH═O and —CH(OR17)2 capable of modulating the activity of histone demethylases (HDMEs), which are useful for prevention and / or treatment of diseases in which genomic dysregulation is involved in the pathogenesis, such as e.g. cancer and formulations and methods of use of such compounds.
Owner:GILEAD SCI INC

Pyrimidine derivatives containing semicarbazide and terminal alkyne structural units, and preparation methods and applications of pyrimidine derivatives

The invention belongs to the field of medicinal chemistry, and discloses pyrimidine compounds containing semicarbazide and terminal alkyne structural units, and preparation methods and applications of the pyrimidine compounds in preparation of antitumor drugs by taking lysine specific demethylase 1 (hereafter referred to as LSD1) as a target. A pyrimidine active fragment is built by adopting a three-component one-pot method, and then the target compounds are prepared by substitution, chlorination and ammonification reaction. The general formulas of the compounds are as shown in the formula I in the specification. An in vitro anti-tumor activity experiment and an LSD1 inhibition activity experiment prove that the compounds have obvious inhibiting and killing action on a plurality of tumor cells by inhibiting the activity of the LSD1, can be used as lead compounds for further development, and are applied to preparation of the antitumor drugs.
Owner:ZHENGZHOU UNIV

Desmethyl tocopherols for preventing or slowing degenerative neurological diseases

InactiveUS20020006954A1BiocideOrganic active ingredientsDegenerative neurologic diseasesParenteral nutrition
The present invention involves the use of desmethyl tocopherols such as gamma tocopherol for the prevention of and treatment of neurological disorders. Dietary or parenteral administration of desmethyl tocopherols inhibits the undesired nitration of neurological components.
Owner:OKLAHOMA MEDICAL RES FOUND

Arylcyclopropylamine based demethylase inhibitors of lsd1 and their medical use

The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection. Thus, in one specific aspect the invention relates to formulas (II), (III), (IV), (V), (VI), (VII), (VIII), (IX).
Owner:ORYZON GENOMICS SA

Desmethyl tocopherols for protecting cardiovascular tissue

InactiveUS20010044462A1Safe deliveryAmenable to deliveryOrganic active ingredientsBiocideThrombusNitrogen
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.
Owner:OKLAHOMA MEDICAL RES FOUND

Blautia sp. AUH-JLD56 and application thereof in conversion of arctigenin

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.
Owner:HEBEI AGRICULTURAL UNIV.

2-Desmethyl ansamycin compounds

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.
Owner:KOSAN BIOSCI

Succinate salt of O-desmethyl-venlafaxine

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

Pyrazolo N-substituted dehydronorcantharidin imide derivative as well as synthesis method, activity test method and application thereof

The invention discloses a pyrazolo N-substituted dehydronorcantharidin imide derivative as well as a synthesis method, an activity test method and application thereof, belonging to the field of cantharidin derivatives. The pyrazolo N-substituted dehydronorcantharidin imide derivative has a structural general formula shown as a formula 1: in the formula 1, R1 is H, C1, F, CH3, OCH3, OH or NO2; and R2 is 2-phenyl-2H-1,2,3-triazole-4-substituent or quinoxaline-2-substituent. The novel N-substituted dehydronorcantharidin imide derivative introduces five-membered heterocyclic pyrazole rings into norcantharidin substituted arylamine and has favorable anti-tumor activity.
Owner:SHAOXING UNIVERSITY

Lysine specific demethylase-1 inhibitors and their use

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.
Owner:ORYZON GENOMICS SA

Methods for One-Pot N-Demethylation/N-Functionalization of Morphine and Tropane Alkaloids

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.
Owner:BROCK UNIVERSITY

Extended release pharmaceutical dosage form

This invention relates to novel extended release pharmaceutical dosage forms for orally delivering drugs to mammals, e.g., humans. More particularly, this invention concerns novel dosage forms of water soluble drugs such as venlafaxine, enantiomeric (R or S) forms of venlafaxine, metabolites of venlafaxine such as O-desmethyl venlafaxine (ODV) or enantiomeric (R or S) forms of said metabolites which dosage forms have an extended release profile when taken orally. This invention also provides processes for preparing such dosage forms and methods of using them.
Owner:WYETH LLC

Lysine specific demethylase-1 inhibitors and their use

The present invention relates to a compound of Formula 1, 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, haloalkoxy, aryl, arylalkoxy, alkyl, alkoxy, amido, —CH2C(=0)NH2, heteroaryl, cyano, sulfonyl, 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 a single bond, —CH2—, —CH2CH2—, —CH2CH2CH2—, and —CH2CH2CH2CH2—; and (D) is an aliphatic carbocyclic group or benzocycloalkyl, wherein said aliphatic carbocyclic group or said benzocycloalkyl has 0, 1, 2, or 3 substituents independently chosen from —NH2, —NH(C1-C6 alkyl), —N(C1-C6 alkyl)(C1-C6 alkyl), alkyl, halo, amido, cyano, alkoxy, haloalkyl, and haloalkoxy. (A′)X-(A)-(B)—(Z)-(L)-(D) formula (I) The compounds of the invention show activity for inhibiting LSD1, which makes them useful in the treatment or prevention of diseases such as cancer.
Owner:ORYZON GENOMICS SA

Method of preparing 4-R-substituted 4-demethoxydaunorubicin

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%.
Owner:SYNBIAS PHARMA

Macrocyclic and cage-like molecules based on biphenylarene and derivatives of macrocyclic and cage-like molecules as well as synthetic methods and applications of macrocyclic and cage-like molecules and derivatives

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.
Owner:TIANJIN NORMAL UNIVERSITY

Cyclopropylamine spiro(hetero)cyclic compound, and pharmaceutical composition and application thereof

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.
Owner:SHANGHAI DE NOVO PHARMA

Novel succinate salt of O-desmethyl-venlafaxine

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

Use of Oripavine as a Starting Material For Buprenorphine

ActiveUS20080312441A1Organic chemistryNorbuprenorphineMethyl group
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.
Owner:SPECGX LLC

Pyrimidine and triazole containing LSD1 inhibitor and preparation method and application thereof

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.
Owner:ZHENGZHOU UNIV

Preparation method and intermediate of minocycline

The invention discloses a preparation method and an intermediate of minocycline. A preparation method for the intermediate M-M is to subject demethylated aureomycin and dimethylamine to reactions as described in the specification in an amine solvent or amide solvent under the catalysis of a palladium complex. The preparation method for minocycline comprises the following steps: (1) subjecting demethylated aureomycin and dimethylamine to the reactions in the amine solvent or amide solvent under the catalysis of the palladium complex so as to prepare the compound M-M; and (2) subjecting the compound M-M prepared in step (1) to hydrogenation and dehydroxylation in an alcohol solvent including an acid under the catalysis of a catalyst. The preparation method provided by the invention has the advantages of easily available raw materials, low cost, simple two-step reaction operation, high product yield, good product quality, recoverability and reusability of the solvents and easy industrial production.
Owner:CHENGDU CHEMPARTNER

Methods for one-pot n-demethylation/n-acylation of morphine and tropane alkaloids

The present invention provides a method for the N-demethylation and / or N-acylation of an N-methylated heterocycle such as morphine alkaloids or tropane alkaloids. The method comprises reacting the heterocycle with an acylating agent in the presence of a metal catalyst.
Owner:BROCK UNIVERSITY

Lysine Specific Demethylase-1 inhibitors and their use

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.
Owner:ORYZON GENOMICS SA

Preparation method of compound 19-desmethyl-4-androstene-3,17 diketone

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.
Owner:ZHEJIANG XIANJU PHARMA

Prodrugs of muscarinic agonists and methods of treatment of neuropsychiatric disorders

Compounds are described that are prodrugs to active compounds that modulate a muscarinic receptor. In some cases, the compounds are prodrugs to N-desmethylclozapine. The compounds may be used to treat neuropsychiatric disorders.
Owner:ACADIA PHARMA INC
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