- Synthesis method of N-benzyl-4-piperidine formaldehyde
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The invention belongs to the technical field of medicine synthesis, and particularly relates to a synthesis method of N-benzyl-4-piperidine formaldehyde. According to the invention, 4-piperidinecarboxylic acid is used as a raw material; an esterification reaction is carried out to generate 4-methyl piperidinecarboxylate hydrochloride; an alkylation reaction is carried out on N-benzyl-4-methyl piperidinecarboxylate hydrochloride to generate N-benzyl-4-methyl piperidinecarboxylate; n-benzyl-4-methyl piperidinecarboxylate is hydrolyzed to obtain N-benzyl-4-piperidinecarboxylic acid, N-benzyl-4-piperidinecarboxylic acid is subjected to an acylation reaction to generate N-benzyl-4-piperidinecarboxamide, N-benzyl-4-piperidinecarboxamide is dehydrated to obtain 1-benzylpiperidine-4-nitrile, and 1-benzylpiperidine-4-nitrile is subjected to a reduction reaction to generate N-benzyl-4-piperidineformaldehyde. The method is mild in reaction condition, simple in aftertreatment and high in yield, N-benzyl-4-piperidinecarboxaldehyde can be obtained at the high yield at the temperature of 0 DEG C, column chromatography is not needed, and repeatability is high.
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Paragraph 0030-0032
(2020/08/18)
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- SPIRO-LACTAM NMDA RECEPTOR MODULATORS AND USES THEREOF
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Disclosed are compounds having potency in the modulation of NMDA receptor activity. Such compounds can be used in the treatment of conditions such as depression and related disorders as well as other disorders.
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Page/Page column 27
(2019/08/26)
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- CEREBLON BINDERS FOR THE DEGRADATION OF IKAROS
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The present invention provides cereblon binders for the degradation of Ikaros or Aiolos by the ubiquitin proteasome pathway along with their use in therapeutic applications as described herein.
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Page/Page column 398
(2019/10/23)
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- A process for the preparation of intermediate the Pu card must benefit new process (by machine translation)
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The invention discloses a compound of formula (I) indicated by the 1 - (3 - a oxygen propyl) - 4 - amino piperdine preparation method, it includes such as the following steps: (1) a compound of formula (II) in the reaction in a solution of ammonia the system results in the type (III) compound; (2) the compound of formula (III) with 1, 3 - dibromo - 5, 5 - dimethyl hydantoin in the reaction under alkaline condition is the system results in the type (I) compound. This preparation method without special reaction equipment requirements, the operation is simple, and is suitable for industrial production; high yield, three wastes, low cost; high purity, heavy metal residue problem. (by machine translation)
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Paragraph 0040; 0041; 0042; 0043
(2017/07/20)
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- HETEROAROMATIC DERIVATIVES AND PHARMACEUTICAL APPLICATIONS THEREOF
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Disclosed are heteroaryl derivatives, pharmaceutical composition and uses in the manufacture of a medicine for treating respiratory diseases, especially for chronic obstructive pulmonary disease (COPD).
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Paragraph 00373
(2016/05/02)
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- Aromatic heterocyclic derivatives and applications of aromatic heterocyclic derivatives in medicines
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The present invention discloses aromatic heterocyclic derivatives and applications of the aromatic heterocyclic derivatives in medicines, and specifically provides a class of aromatic heterocyclic compounds or stereoisomers, geometric isomers, tautomers, racemic bodies, nitrogen oxides, hydrates, solvates, metabolites, pharmaceutically acceptable salts or prodrugs thereof, and pharmaceutical compositions containing the compounds. The present invention further discloses uses of the compounds or pharmaceutical compositions in drug preparation, wherein the drug is used for treatment of respiratory diseases, particularly chronic obstructive pulmonary disease (COPD).
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Paragraph 0920-0923
(2016/10/09)
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- SUBSTITUTED 1-AMINOPHTHALAZINE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC APPLICATION THEREOF
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The invention concerns 1-amino-phthalazine derivatives of general formula (I): Wherein A, B, L, R, R1, R2, R3, R4, R5 and R7 are as defined herein. The invention also concerns the preparation of said compounds and their therapeutic use.
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Page/Page column 16
(2009/05/28)
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- Novel betaines of the hexaalkylguanidinio-carboxylate type
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Betaines 7a, b and 8a, b have been prepared from 3- and 4-piperidinecarboxylic acid and N,N,N′N′-tetraalkyl- chloroformamidinium chlorides via the corresponding methyl esters. These betaines are highly hygroscopic, thermally very stable, and, with the exception of 7b, have rather low melting points. They undergo a surprisingly facile alkaline cleavage of the hexaalkylguanidinium moiety. They react with dichloromethane by a twofold nucleophilic substitution to form methylene dicarboxylates such as 11. The NMR (1H, 13C) data of betaines 7 and 8 are discussed.
- Walter, Matthias,Maas, Gerhard
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scheme or table
p. 1617 - 1624
(2010/06/22)
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- Fibrinogen receptor antagonists
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This invention relates to compounds of the formula: which are effective for inhibiting platelet aggregation, pharmaceutical compositions for effecting such activity, and a method for inhibiting platelet aggregation.
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- Exploring the structure-activity relationships of [1-(4-(4- tert-butyl-3'-hydroxy)benzhydryl-4-benzylpiperazine] (SL-3111), a high-affinity and selective δ-opioid receptor nonpeptide agonist ligand
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SL-3111 [1-(4-tert-butyl-3'-hydroxy)benzhydryl-4- benzylpiperazine] is a de novo designed, high-affinity and selective nonpeptide peptidomimetic agonist of the δ-opioid receptor. In a previous report we had described the unique biological characteristics of this ligand and also a need for further structural evaluation. To pursue this, we have introduced a completely different heterocyclic template (2 and 3), which, based on molecular modeling studies, may present the required structural features to properly orient the pharmacophore groups. We also have made more subtle changes to the original piperazine scaffold (5 and 11). The biological activities of these compounds revealed an important participation of the scaffold in the ligand-receptor interaction. To further explore functional diversity on the scaffold, we have maintained the original piperazine ring and introduced four different functionalities at position 2 of the heterocyclic ring (15a-d; a = CH2-O-CH2-Ph; b = Me; c = CH2Ph; d = CH2OH). The biological activities observed for these compounds showed a very interesting trend in terms of the steric effects of the groups introduced at this position. A decrease of almost 2000-fold in affinity and potency at the δ- receptor was observed for 15c compared with 15b. This difference may be explained if we postulate that the bioactive conformation of these peptidomimetics is close to the minimal energy conformations calculated in our study. On the basis of these findings we have realized the importance of this position to further explore and simplify the structure of future generations of peptidomimetic ligands.
- Alfaro-Lopez, Josue,Okayama, Toru,Hosohata, Keiko,Davis, Peg,Porreca, Frank,Yamamura, Henry I.,Hruby, Victor J.
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p. 5359 - 5368
(2007/10/03)
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