59 results about "Phenylpiperidine" patented technology

The present invention provides a compound having the structure:whereinR1, R2, R3, R4, and R5 are each independently H, halogen, CF3 or C1-C4 alkyl,wherein two or more of R1, R2, R3, R4, or R5 are other than H;R6 is H, OH, or halogen; andB is a substituted or unsubstituted heterobicycle,wherein when R1 is CF3, R2 is H, R3 is F, R4 is H, and R5 is H, or R1 is H, R2 is CF3, R3 is H, R4 is CF3, and R5 is H, or R1 is Cl, R2 is H, R3 is H, R4 is F, and R5 is H, or R1 is CF3, R2 is H, R3 is F, R4 is H, and R5 is H, or R1 is CF3, R2 is F, R3 is H, R4 is H, and R5 is H, or R1 is Cl, R2 is F, R3 is H, R4 is H, and R5 is H, then B is other thanor a pharmaceutically acceptable salt thereof.

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 provides a synthesis method on the first aspect, and by means of the synthesis method, a target product, namely (R)-3-phenylpiperidine or / and (S)-3-phenylpiperidine is / are successfully prepared with N-protected 3-piperidone as a starting material; the invention provides a synthesis method on the second aspect, and by means of the synthesis method, the target product, namely the (R)-3-phenylpiperidine or / and the (S)-3-phenylpiperidine is / are successfully prepared with the same N-protected 3-piperidone as the starting material and by ingeniously utilizing an organic silicon reagent. Chiral intermediates alpha, beta and gamma of niraparib are synthesized from the (S)-3-phenylpiperidine correspondingly according to the third aspect, the fourth aspect and the fifth aspect of the invention. In one word, according to the synthesis method of the (R)-3-phenylpiperidine or / and the (S)-3-phenylpiperidine and the synthesis method of the chiral intermediates alpha, beta and gamma of the niraparib, the production cost is obviously lowered, and large-scale industrial production of niraparib medicines is facilitated.

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.

Compounds of general formula I[Chemical formula should be inserted here. Please see paper copy] R1 is selected from any one of phenyl, pyridinyl, pyrrolyl, thienyl, furanyl, imidazolyl, triazolyl, and pyridine N-oxide; where each R1 phenyl ring and R1 heteroaromatic ring may optionally and independently be further substituted by 1,2 or 3 substituents selected from straight and branched C1-C6 alkyl, NO2, CF3, C1-C6 alkoxy, chloro, fluoro, bromo, and iodo. The substitutions on the phenyl ring and on the heteroaromatic ring may take place in any position on said ring systems; are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts and pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain, anxiety and functional gastrointestinal disorders.

The invention discloses the application of a heterocyclic substituted phenylpiperazine (pyridine) derivative in antidepressant drugs. 1A and 5‑HT 7 The two receptors have good inhibitory activity, the compound has good antidepressant activity in vivo, has the effect of improving cognitive function and is well tolerated in animals. The heterocyclic substituted phenylpiperazine (pyridine) derivatives are compounds represented by general structural formula (I) or pharmaceutically acceptable salts thereof: