57 results about "Phenylpiperidine" patented technology

The present invention relates to compounds having therapeutic effects against disorders in the central nervous system, and in particular substituted phenylpiperidines of the formula 1:

wherein R is as defined herein.

The present invention relates to substituted phenylpiperidine derivatives as melanocortin-4 receptor modulators. Depending on the structure and the stereochemistry the compounds of the invention are either selective agonists or selective antagonists of the human melanocortin-4 receptor (MC-4R). The agonists can be used for the treatment of disorders and diseases such as obesity, diabetes and sexual dysfunction, whereas the antagonists are useful for the treatment of disorders and diseases such as cancer cachexia, muscle wasting, anorexia, anxiety and depression. Generally all diseases and disorders where the regulation of the MC-4R is involved can be treated with the compounds of the invention.

The present invention relates to compounds which have therapeutic effects against disorders in the central nervous system, and in particular new 4-(ortho,meta-disubstituted phenyl)-1-alkypiperidines and piperazines.

wherein R1, R2, R3 and X are as defined.

The invention belongs to the technical field of organic synthesis. The synthesis method firstly provided by the invention takes benzyl-4-oxopiperidine as a starting material, and the starting materialis subjected to Grignard reaction, elimination reaction, hydrogenation reduction reaction and chiral resolution in sequence to successfully obtain a target product (R)-3-phenylpiperidine or/ and (S)-3-phenylpiperidine. The synthesis method sencondly provided by the invention takes the same starting raw material for Grignard reaction, organic silicon reagent is used for removing a hydroxide radical, and benzyl is removed by catalytic hydrogenation reaction; finally, the chiral resolution is carried out to obtain a target product. The (S)-3-phenylpiperidine can be synthesized according to the synthesis method. (S)-3-p-aminosalicylic phenylpiperidine can be synthesized according to the third aspect; or according to the fourth aspect, (S)-3-p-bromophenyl piperidine is synthesized to serve asthe key intermediate for preparing the niraparib. According to the synthesis method for (R)-3-phenylpiperidine or/ and (S)-3-phenylpiperidine and the synthesis method for chiral intermediate of niraparib, production cost is obviously lowered, and the synthesis methods are favorable for the large-scale industrial production of a niraparib medicine.

A compound of the chemical formula (I) and its pharmaceutically acceptable salt: ##STR1## wherein Y is C.sub.2 -C.sub.4 alkylene; Z is a valence bond or C.sub.1 -C.sub.6 alkylene; R.sup.1 is substituted or unsubstituted aryl (e.g., phenyl and naphthyl) or heteroaryl (e.g., thienyl and furyl); R.sup.2 is hydrogen or C.sub.1 -C.sub.6 alkyl; R.sup.3 is hydrogen, hydroxy or the like; R.sup.4 is substituted or unsubstituted benzyl or the like. Typical examples are (2S*,3S*,4R*,5R*)-4-Carboxy-3-[N-(5-Isopropyl-2-methoxy-benzyl)amino]-5-me thyl-2-phenylpyrrolidine and (2S*,3S*,5S*)-5-Carboxy-3-[N-(2-methoxy-5-trifluoromethoxybenzyl)amino]-2- phenylpiperidine. The novel substituted azaheterocyclecarboxylic acids in this invention have excellent substance P antagonistic activity and are thus useful for the treatment of gastrointestinal disorders, central nervous system disorders, allergy, inflammatory diseases, asthma, pain, emesis or migraine in mammals, especially humans.

Crystalline forms of 4-[2-(4-methylphenylsulfanyl)-phenyl]piperidine and salts thereof are provided e.g. for the treatment of neuropathic pain.

The invention relates to the technical field of medicines, and relates to a preparation method of a medicine ALK inhibitor AP26113. The method comprises the following steps: (1) carrying out substitution reaction of aromatic amine on 2,4,5-trichloropyrimidine and 2-(dimethyloxyphosphate)aniline under the action of an acid applying agent to obtain an intermediate 1 (2,5-dichloro-N-(2-(dimethylphosphine)phenyl)pyrimidine-4-amine), and pulping the intermediate; (2) carrying out aromatic amine substitution reaction on 2-nitro-5-fluoroanisole and 1-methyl-4-(4-piperidyl)-piperazine under the actionof an acid applying agent to obtain a compound 1-(1-(3-methoxy-4-nitrophenyl)piperidin-4-yl)4-methylpiperazine, dissolving the compound with an organic solvent, and extracting the compound with an acidic solvent; (3) carrying out palladium-carbon catalytic hydrogenation on the product obtained in the step (2) to obtain an intermediate 2 (2-methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperazinyl]-aniline); (4) carrying out amine substitution reaction on the intermediate 1 and the intermediate 2 under an acidic catalytic condition to obtain a crude product of Brigatinib. The yield of the Brigatinibreaches 50% or above, and the purity of the Brigatinib reaches 99.9% or above.

Substituted phenylpiperidines and phenylpyrrolidines of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions.

The present invention relates to compounds which have therapeutic effects against disorders in the central nervous system, and in particular new 4-(ortho,meta-disubstituted phenyl)-1-alkypiperidines.

wherein R1, R2, and R3 are as defined.

The present invention relates to a novel series of 4-phenylpiperazines, 4-phenyl-piperidines and 4-phenyl-1,2,3,6-tetrahydropyridines compound of general formula (I) wherein A is alkylene, alkenylene, alkynylene, and C3-7 cycloalkylene; R<1> is a C3-10 alkyl, alkenyl, or alkynyl group, cycloalk(en)yl, cycloalk(en)yl-alk(en/yn)yl, trifluoromethylsulfonyl, or alkylsulfonyl, R<2> - R<5> are optional substituents; R<9> and R<10> are hydrogen, alkyl or together form an ethylene or propylene bridge; W is O or S; V is O, S, CR<6>R<7>, or NR<8> wherein R<6>, R<7>, and R<8> are hydrogen or alkyl, alkenyl, cycloalkyl, cycloalkylalkyl, optionally substituted arylalkyl or aryl, or R<6> and R<7> constitute a 3-7 membered spiroring; Z is -(CH2)m-, m being 2 or 3 or Z is -CH=CH-; X is N, C or CH; show effects on central serotonin 5-HT1A and dopamine D2 receptors. Thus the novel compounds are useful in the treatment of certain psychic and neurologic disorders in particular psychosis.