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A head spore for the Tanzania acid new crystalline and its preparation method (by machine translation)

A head spore for the Tanzania acid new crystalline and its preparation method. The present invention provides a [6R – (6a, 7 alpha)] – 7 – [[ [4 – (2 – amino – 1 – carboxyl – 2 – oxo ethylidene) – 1, 3 – dithio-azetidine – 2 – yl] carbonyl] amino] – 7 – methoxy – 3 – [[ (1 – methyl – 1H – tetrazol – 5 – yl) thio] methyl] – 8 – oxo – 5 – thia – 1 – azabicyclo [4, 2, 0] Oct – 2 – ene – 2 – carboxylic acid the new crystalline form, this crystalline form X – ray powder diffraction pattern of a reflection angle of the 2 theta in the 11.66 ¡À 0.1 , 17 . 53 ¡À 0.1 , 17 . 72 ¡À 0.1 , 18 . 91 ¡À 0.1 , 20 . 01 ¡À 0.1 , 21 . 02 ¡À 0.1 , 22 . 24 ¡À 0.1 , 23 . 33 ¡À 0.1 and has a characteristic peak. Such a compound is crystalline form has good stability, and its preparation process is simple, lower cost, can be used in industrial production. (by machine translation)

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5H-CYCLOPENTA[D]PYRIMIDINES AS AKT PROTEIN KINASE INHIBITORS

Compounds of Formula I are useful for inhibiting AKT protein kinases. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed. Formula (I)

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[1,3,4] OXADIAZOLE DERIVATIVE AND APPLICATION THEREOF

The present invention belongs to the medicinal chemistry field, and specifically discloses a [1,3,4]oxadiazole derivative with the structure of general formula (I) and pharmaceutically acceptable salt thereof. The compound can be used to prepare a medicine for preventing or treating a disease of the central nervous system.

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HETEROCYCLIC SUBSTITUTED PIPERAZINES FOR THE TREATMENT OF SCHIZOPHRENIA

This invention relates to compounds of the formula 1 wherein X, Y, Z, A, R’, R2, R3, R4, R9, W’ and W2 are defined as in the specification, pharmaceutical compositions containing them and their use in the treatment of central nervous system and other disorders.

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Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6- fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5-trimethyl-4- thiazolidinone maleate

HP-236 (3-[4-[4-(6-Fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]- 2,5,5-trimethyl-4-thiazolidinone maleate; P-9236) (54) displayed a pharmacological profile indicative of potential atypical antipsychotic activity. A series of piperazinyl butyl thiazolidinones structurally related to this compound were prepared and evaluated in vitro for dopamine D2 and serotonin 5HT2 and 5HT(1A) receptor affinity. The compounds were examined in vivo in animal models of potential antipsychotic activity and screened in models predictive of extrapyramidal side effect (EPS) liability. The synthesis of these compounds, details of their structure-activity relationships, and discovery of a new lead, compound 50, as well as further development of the profiles of compounds 50 and 54 are described.

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INDOLES, 1H-INDAZOLES, 1,2-BENZISOXAZOLES, AND 1,2-BENZISOTHIAZOLES, AND PREPARATION AND USES THEREOF

The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds for example, indoles, 1H-indazoles, 1,2-benzisoxazoles, and 1,2-benzisothiazoles, which act as ligands for the alpha7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.

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A SHORT PROCESS FOR THE PREPARATION OF ZIPRASIDONE AND INTERMEDIATES THEREOF

A process for the preparation of oxindole derivative (Ziprasidone hydrochloride) of formula (I) comprising reacting compound of formula (II) with metal or metal compound mineral acid to give compound of formula (III) in a single step which is converted into compound of formula IV which is a key intermediate for the preparation of compound of compound of formula (I).

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Pro-drugs of 5-(2-(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)ethyl)-6-chloro-1,3-dihydro-2h-indol-2-one

The present invention relates to a pro-drug of ziprasidone or pharmaceutically acceptable salts thereof, processes for its preparation, and pharmaceutical compositions and methods of treatment comprising said pro-drug.

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Method for preparing Perospirone is (by machine translation)

The invention discloses a new method for preparing Perospirone is of the, type I and along link oneself dimethyl ester imide reaction, produce Perospirone is, the method avoids the alkylation intermediate, has the advantages of simple process, raw materials are easy, is suitable for industrial production, the product yield and purity are, and the like. (by machine translation)

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3-[4-(1-Substituted-4-piperazinyl)butyl]-4-thiazolidinone compounds

3-[4-1-substituted-4-piperazinyl)butyl]-4-thiazolidinone compounds which are useful as antipsychotic, analgesic, anticonvulsant and anxiolytic agents.

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