55 results about "PROPYLAMINE DERIVATIVES" patented technology

The present invention relates to phenylcyclopropylamine derivatives. In particular, pharmaceutical compositions comprising phenylcyclopropylamine derivatives are provided. The compounds of this invention can, inter alia, be used for the treatment and the prevention of cancer as well as neurodegenerative diseases or disorders.

This invention relates to the use of cyclopropylamine derivatives for the modulation, notably the inhibition of the activity of Lysine-specific demethylase 1 (LSD1). Suitably, the present invention relates to the use of cyclopropylamines in the treatment of cancer.

This invention relates to the use of cyclopropylamine derivatives for the modulation, notably the inhibition of the activity of Lysine-specific demethylase 1 (LSD1). Suitably, the present invention relates to the use of cyclopropylamines in the treatment of cancer.

The present invention relates to phenylcyclopropylamine derivatives. In particular, pharmaceutical compositions comprising phenylcyclopropylamine derivatives are provided. The compounds of this invention can, inter alia, be used for the treatment and the prevention of cancer as well as neurodegenerative diseases or disorders.

A water-based drilling fluid and method of using same are presented in this disclosure, which fluid is used in drilling wells through a formation containing a shale that swells in the presence of water. The drilling fluid comprises an aqueous based continuous phase; a weighting material; and a shale hydration inhibition agent (SHIA) selected from the group consisting of propylamine derivatives, hydrogenated poly(propyleneimine) dendrimers (HPPID), and polyamine twin dendrimers (PTD). In some embodiments, the SHIA of this disclosure is not hydrolyzed at a temperature in the range of from about 100° F. to about 500° F. The drilling fluid may further comprise a fluid loss control agent, an encapsulating agent, other additives, and combinations thereof. A method of reducing shale swelling during wellbore drilling is also described. The method comprises circulating in the subterranean well a water-based drilling fluid comprising an aqueous based continuous phase, a weighting material, and a SHIA.

A water-based drilling fluid and method of using same are presented in this disclosure, which fluid is used in drilling wells through a formation containing a shale that swells in the presence of water. The drilling fluid comprises an aqueous based continuous phase; a weighting material; and a shale hydration inhibition agent (SHIA) selected from the group consisting of propylamine derivatives, hydrogenated poly(propyleneimine) dendrimers (HPPID), and polyamine twin dendrimers (PTD). In some embodiments, the SHIA of this disclosure is not hydrolyzed at a temperature in the range of from about 100° F. to about 500° F. The drilling fluid may further comprise a fluid loss control agent, an encapsulating agent, other additives, and combinations thereof. A method of reducing shale swelling during wellbore drilling is also described. The method comprises circulating in the subterranean well a water-based drilling fluid comprising an aqueous based continuous phase, a weighting material, and a SHIA.

The invention includes processes for the synthesis of amphetamine, dexamphetamine, methamphetamine, derivatives of these, including their salts, and novel precursors and intermediates obtained thereby, by synthesizing aziridine phosphoramidate compounds in specified solvents at specified temperatures, and then converting to a novel aryl or aryl-alkyl phosphoramidate precursors using an organometallic compound such as a copper salt, where the novel aryl or aryl-alkyl phosphoramidate precursor is then easily converted to the target compounds using known reactions.

The present invention is directed to substituted propylamine derivatives of formula I: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.

The invention provides a preparation method of a chiral aryl cyclopropylamine derivative. The chiral aryl cyclopropylamine derivative is prepared by using benzene halide or benzene polyhalide as the initial raw material and subjecting the benzene halide or benzene polyhalide to Friedel-Crafts reaction, asymmetric reduction reaction, cyclization reaction, acylation reaction, hydrolysis reaction andCurtius rearrangement reaction, wherein the benzene halide or benzene polyhalide is preferably o-difluorobenzene, 2-chlorofluorobenzene or fluorobenzene. The preparation method has the advantages that carbonyl asymmetric reduction and a acylation reagent are used to build a cyclopropyl ester structure, and the use of chiral auxiliaries is avoided; the reaction route of the method is shortened ascompared with a reaction route in the prior art, and reaction yield is increased; acyl azide rearrangement is used to prepare primary amine, and the method is simple to operate, high in yield and suitable for large-scale industrial production.

The invention belongs to the technical field of benzothiazide derivatives, and discloses a synthetic method of a benzothiazide formaldehyde derivative. The synthesis method comprises the following steps: in the system of an organic solvent, an alkaline compound, a photocatalyst and an additive, carrying out a reaction on a benzenesulfonyl propargylamine derivative in an aerobic environment throughillumination to obtain a benzothiazine formaldehyde derivative, wherein the additive is more than one of diphenyl disulfide and thiophenol. According to the method, the benzothiazine compound is prepared by utilizing the carbon oxidation reaction of alkyne. The method is simple, convenient, efficient and high in regioselectivity, the used raw materials are simple and easy to obtain, no extra organic oxidizing agent needs to be added, oxygen in the air is used as an oxygen source and is environmentally friendly, cheap and easy to obtain. In addition, the whole operation process is simple and feasible, steps are simple and products are easy to purify.

The invention relates to a chemical synthesis method of a (1R, 2S)-2-aryl cyclopropylamine derivative. 3-aryl crylic acid serves as a raw material, the raw material and N,O-dimethyl hydroxy amine hydrochloride are subjected reaction to prepare a corresponding amide intermediate, cyclization reaction is conducted, 2- aryl cyclopropylamine is obtained; and finally D-mandelic acid serves as a resolving agent to obtain the (1R, 2S)-2-aryl cyclopropylamine derivative. The method has the advantages of being high in yield and high in e.e. value.

The present invention relates to a propylamine derivative and its application in preparation of tomoxetine (atomoxetine raceme). Said invention also provides its chemical structure formula, and the invented preparation method is simple, and is suitable for industrial production.

The invention relates to a chemical synthesis method of a (1R, 2S)-2-aryl cyclopropylamine derivative. 3-aryl crylic acid serves as a raw material, the raw material and N,O-dimethyl hydroxy amine hydrochloride are subjected reaction to prepare a corresponding amide intermediate, cyclization reaction is conducted, 2- aryl cyclopropylamine is obtained; and finally D-mandelic acid serves as a resolving agent to obtain the (1R, 2S)-2-aryl cyclopropylamine derivative. The method has the advantages of being high in yield and high in e.e. value.

The invention discloses a synthesis method of (+ / -)-alpha-fluoro-gamma-amino acid. The method comprises the steps of enabling 3-phenyl-1-propylamine or 3-phenyl-1-propylamine derivatives to be sequentially subjected to four reaction, i.e., amido protection, benzyl free radical fluorination, benzene ring oxidation and protecting group removal. The method avoids the use of a high-risk fluorine reagent DAST, and has the characteristics of being simple to operate, rapid in reaction, high in yield and the like.

A slowly-releasing microspherical medicine used for the injection to treat the diseases associated with the antagon of muscarinic receptor, the impulsive inoontinence and urination urgency or frequency is prepared from 3,3-diphenyl propylamine derivative, its optical enantiomer or cacemer, and the biodegradable medical high-molecular auxiliary. Its preparing process is also disclosed.

The invention provides naphthyloxy benzedrine derivatives, which are prepared by subsequently reacting naphthyloxy benzedrine with acid and alkali metals or ammonium (including ammonia) compounds or amino acid or alkamine or directly reacting with acid salt; when the acid or acid salt is a sulfate radical, a naphthyloxy benzedrine sulfate complex salt is obtained; and when the acid or the acid salt is a phosphate radical, a naphthyloxy benzedrine phosphate complex salt is obtained. The method has the advantages of rational design, stable process and high production feasibility. The naphthyloxy benzedrine derivatives provided by the method have the remarkable advantages of high bioavailability, high purity, small side effect and the like. The naphthyloxy benzedrine derivatives can be prepared into a preparation, and has rapid absorption and quick response after oral administration by feeding the naphthyloxy benzedrine into blood, so that the curative effect of treating premature ejaculation and erectile dysfunction of men is better achieved. The naphthyloxy benzedrine derivatives have the structural formula shown in the description.

The invention belongs to the technical field of organic synthesis and belongs to the method for synthesizing a propargylamine derivative with different substituent groups at the alkyne terminal. Mutual transformation of different propargylamine is realized through carbon-carbon single-bond activation, specifically, a compound terminal alkyne and propargyl substitute secondary amine to serve as raw materials under the catalysis system of rare earth, and the propargylamine derivative with various substituent groups at the alkyne terminal is prepared. According to the method, sources of raw materials are wide, the preparation is easy, the operation is simple and convenient, the selectivity is controllable, and the yield is high.

Disclosed are naphthalimide derivatives and in particular e.g. N-aryl-substituted naphthalimidopropylamine derivatives (i.e. 2-[3-(amino)propyl]-1H-benz[de]isoquinoline-1,3(2H)-dione derivatives) such as e.g. such as e.g. (Formula I) or (Formula III) as anti-parasitic agents for the treatment of Leishmaniasis. The compounds could also be useful to treat viral, bacterial and / or neoplastic diseases. The description discloses exemplary synthesis as well as biological tests against Leishmania infantum parasites (e.g. pages 54 to 58; examples 1 to 7). Exemplary compounds are: (example 3)(example 4) 2-(3-((5-amino naphthalene-1-yl)amino)propyl)-1H-benzo[de]isoquinoline-1, 3(2H)-dione (example 5) 2-(3-((5-amino naphthalene-1-yl)amino)propyl)-1H-benzo[de]isoquinoline-1,3(2H)-dione (example 6).

New 3-phenoxy-3-phenylpropanamine derivatives, compositions thereof and their use as a medicament in the treatment of nervous system disorders associated with cognitive deficits and behavioural dysfunctions, in particular fragile X syndrome and Rett syndrome.

The present invention provides a process for preparing a N-methyl-N-hydroxyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine compound. The present invention also provides a process for preparing (S)-(+)-N-methyl-3-methyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine with higher yield and low treatment cost, which includes the preparation of the N-methyl-N-hydroxyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine compound.

A process for the preparation on N-methyl-aryloxy-propanamine derivatives of the formula I and salts thereof. The invention also relates to the preparation and use novel intermediate of the formula XII. The invention also relates to the process of further conversion of novel intermediate into N-methyl-aryloxy propanamine derivatives and salts thereof.Wherein Q and P independently represents substituted or unsubstituted aryl group such as phenyl, naphthyl, pyridine, furanyl, pyranyl thienyl, and the like optionally substituted aryl by a halogen, a straight chain or branched alkyl group containing 1 to 6 carbon atoms, —O-alkyl group containing straight chain or branched C1-C6 alkyl group, an alkoxy group containing a straight chain or branched alkyl group having 1 to 6 carbon atoms, which comprises demethylation of N,N-dimethyl analogues of compound of formula IA.

The present invention provides a process for preparing a N-methyl-N-hydroxyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine compound. The present invention also provides a process for preparing (S)-(+)-N-methyl-3-methyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine with higher yield and low treatment cost, which includes the preparation of the N-methyl-N-hydroxyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine compound.

The invention provides a preparation method of an acylamino-containing 3, 4-dihydroisoquinoline-1 (2H)-ketone derivative, and belongs to the technical field of heterocyclic compounds. The preparation method comprises the following steps: adding a palladium catalyst, a ligand, alkali, 1, 3, 5-triformic acid phenol ester, a propargylamine derivative and amine into an organic solvent, reacting at 90-110 DEG C for 22-26 hours, and performing post-treatment to obtain the amido-containing 3, 4-dihydroisoquinoline-1 (2H)-ketone derivative. The preparation method is simple and convenient to operate, the initial raw materials are cheap and easy to obtain, the reaction efficiency is high, the substrate compatibility is good, and the amido-containing 3, 4-dihydroisoquinoline-1 (2H)-ketone derivative can be efficiently and rapidly synthesized in one step.

The present invention relates to new compounds of formula (I) that show great affinity and activity towards the subunit α2δ of voltage-gated calcium channels (VGCC), especially the α2δ-1 subunit of voltage-gated calcium channels or dual activity towards the subunit α2δ of voltage-gated calcium channels (VGCC), especially the α2δ-1 subunit of voltage-gated calcium channels, and the noradrenaline transporter (NET). The invention is also related to the process for the preparation of said compounds as well as to compositions comprising them, and to their use as medicaments.

The invention provides naphthyloxy benzedrine derivatives, which are prepared by subsequently reacting naphthyloxy benzedrine with acid and alkali metals or ammonium (including ammonia) compounds or amino acid or alkamine or directly reacting with acid salt; when the acid or acid salt is a sulfate radical, a naphthyloxy benzedrine sulfate complex salt is obtained; and when the acid or the acid salt is a phosphate radical, a naphthyloxy benzedrine phosphate complex salt is obtained. The method has the advantages of rational design, stable process and high production feasibility. The naphthyloxy benzedrine derivatives provided by the method have the remarkable advantages of high bioavailability, high purity, small side effect and the like. The naphthyloxy benzedrine derivatives can be prepared into a preparation, and has rapid absorption and quick response after oral administration by feeding the naphthyloxy benzedrine into blood, so that the curative effect of treating premature ejaculation and erectile dysfunction of men is better achieved. The naphthyloxy benzedrine derivatives have the structural formula shown in the description.

The invention discloses a novel synthesis method of 2-methyl-1-substituted phenyl-2-propylamine compounds, and belongs to the field of material synthesis. The method comprises steps as follows: substituted benzyl halide is taken as a raw material and subjected to a reaction with isobutyronitrile under the action of alkali, obtained 2-methyl-1-substituted phenyl-2-butyronitrile is hydrolyzed and subjected to reactions of Curtius rearrangement and the like, and 2-methyl-1-substituted phenyl-2-propylamine is produced. On the basis of an original method, reaction steps are shortened, the total yield is obviously increased, and meanwhile, the novel method is provided for synthesis of substituted phenyl-2-propylamine derivatives containing bromine atoms and iodine atoms.