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Processes and intermediates for preparing 3-(1-piperazinyl)-1,2-benzisothiazole

The present invention relates to processes for the preparation of 3-(1-piperazinyl)-1,2-benzoisothiazole or its pharmaceutically acceptable salt and to novel intermediates used in the process.

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Isothiazole – Wikipedia,
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Benzisothiazole and benzisoxazole piperazine derivatives

Disubstituted N,N-piperazinyl derivatives are disclosed wherein one substituent is benzisothiazol-3-yl or benzisoxazol-3-yl and the other is alkylene attached to heterocycles such as azaspiro[4.5]decanedione, dialkylglutarimide, thiazolidinedione and spirocyclopentylthiazolidinedione or butyrophenone-like groups. The compounds have psychotropic properties and 8-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]butyl]-8-azaspior[4.5]decane-7,9-dione is a typical embodiment having selective antipsychotic activity.

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Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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New benzenesulphonamide compounds

A compound of formula (I): 1 wherein:Ra represents a hydroxy, alkoxy, aryloxy or arylalkyloxy group,A represents a CH group or a nitrogen atom, in which case R1 is as defined in the description,or R1-A together represent an oxygen atom or a group, 2 ?wherein R3 and R4 are as defined in the description,R2 being a hydrogen atom or an alkyl group,Rb and Rc, which may be identical or different, each represents a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, a hydroxy group or a trihaloalkyl group,n is an integer of from 2 to 6 inclusive,m and p are integers of from 0 to 6 inclusive,its enantiomers, diastereoisomers, and addition salts thereof salts thereof with a pharmaceutically acceptable acid or base, a medicinal product containing the same is useful as antagonist of TXA2 receptor and 5-HT2 receptor.

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Isothiazole – Wikipedia,
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CINNOLINE DERIVATIVES AS PHOSPHODIESTERASE 10 INHIBITORS

The present invention is directed tojcjnnoline compounds of formula (I) that are PDE 1 inhibitors, pharmaceutical compositions containing such compounds and process for preparing such compounds. This invention is also directed to methods of treating diseases treatable by inhibition of PDElO enzyme, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.

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Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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Electric Literature of 107869-45-4, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.107869-45-4, Name is (3aR,6S)-8,8-Dimethyl-4,5,6,7-tetrahydro-3H-3a,6-methanobenzo[c]isothiazole 2,2-dioxide, molecular formula is C10H15NO2S. In a Article£¬once mentioned of 107869-45-4

Chemistry of Oxaziridines. 18. Synthesis and Enantioselective Oxidations of the <(8,8-Dihalocamphoryl)sulfonyl>oxaziridines

The synthesis and enantioselective oxidations of <(8,8-dihalocamphoryl)sulfonyl>oxaziridines 13 are reported.These reagents are prepared in two steps from the (camphorylsulfonyl)imine 4 by treatment of the corresponding azaenolate with electrophilic halogen sources followed by biphasic oxidation of the resulting dihalo imine 6-9 with m-CPBA/K2CO3.Of these oxaziridines the dichloro reagent 13b, available on a multigram scale, affords the highest enantioselectivities for the asymmetric oxidation of sulfides to sulfoxides (42-74 percent) and for the hydroxylation of enolates (often better than 95 percent ee).In general the molecular recognition is predicted and explained in terms of minimization of nonbonded steric interactions in the transition states.For the asymmetric oxidation of sulfides to sulfoxides, secondary electronic factors related to the polarity of the sulfide and oxaziridine also play a role.Definitive evidence for chelation of the metal enolate with the C-X bond in 13 is not found.The molecular recognition is interpreted in terms of the higher reactivity of the reagents and an active-site structure which is sterically complementary with the enolate.For the asymmetric hydroxylation of the Z- and E-enolates of propiophenone (16a), the Z-enolate exhibits much higher stereoselectivity than the E-enolate: >95 percent vs 22 percent ee.

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Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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PROCESS FOR PREPARING ZIPRASIDONE

The present invention relates to improved process for preparing Ziprasidone an its acid addition salts thereof. The invention particularly provides a method f purifying Ziprasidone base thereby providing substantially pure Ziprasidone and i acid addition salts, hydrates, solvates etc.

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Isothiazole – Wikipedia,
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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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Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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Synthesis and Biological Evaluation of Five-Atom-Linker-Based Arylpiperazine Derivatives with an Atypical Antipsychotic Profile

Herein we describe a focused set of new arylpiperazine derivatives as potential broad-spectrum antipsychotics. The general structure contains a quinolinone-like moiety, an arylpiperazine moiety, and a five-atom linker. Among them, 7-(5-(4-(benzo[d]isothiazol-4-yl)piperazin-1-yl)pentyl)quinolin-2(1H)-one (S6) shows a promising preclinical profile. Compound S6, characterized by partial D2R agonism, 5-HT1AR agonism, 5-HT2AR antagonism, and blockade of SERT activities, was found to decrease psychosis- and depressive-like symptoms in rodents. The polypharmacological profile of S6 could provide opportunities for the treatment of various other central nervous system disorders such as anxiety, depression, and psychoses associated with dementia. Furthermore, S6 demonstrated acceptable safety, toxicology, and pharmacokinetic profiles, and has been selected as a preclinical candidate for further evaluation in schizophrenia.

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Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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3-[4-(1-substituted-4-piperazinyl)butyl]-4-thiazolidinone and related compounds

There are disclosed compounds of the formula, STR1 where n is 0, 1 or 2; A is STR2 where X in each occurrence is independently hydrogen, halogen, loweralkyl, hydroxy, nitro, loweralkoxy, amino, cyano, trifluoromethyl or methylthio; Y in each occurrence is independently hydrogen, halogen, loweralkyl, hydroxy, nitro, loweralkoxy, amino, cyano, trifluoromethyl or methylthio; m is 1 or 2; k is 1 or 2; R1 and R2 are independently hydrogen, loweralkyl, STR3 or aryl except that when R1 is STR4 or aryl, R2 is hydrogen, or alternatively R1 +R2 taken together with the carbon atom to which they are attached form a cyclopentane, cyclohexane, cycloheptane, pyran, thiopyran, indan or piperidine ring; R3 and R4 are independently hydrogen or loweralkyl, or alternatively R3 +R4 taken together with the carbon atom to which they are attached form a cyclopentane, cyclohexane, cycloheptane, pyran, thiopyran, pyrrolidine or piperidine ring, the term aryl signifying an unsubstituted phenyl group or a phenyl group substituted with 1, 2 or 3 substituents each of which being independently loweralkyl, loweralkoxy, hydroxy, halogen, loweralkylthio, cyano, amino or trifluoromethyl, which are useful as antipsychotic, analgesic, anticonvulsant and anxiolytic agents.

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Isothiazole – Wikipedia,
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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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Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com