3158-80-3Relevant academic research and scientific papers
PROCESS FOR PREPARATION OF DIBENZOTHIAZEPINONE COMPOUNDS
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Page/Page column 11-12, (2011/10/13)
The present invention discloses a process for the preparation of dibenzothiazepinone compounds of Formula I. The process for preparation of a dibenzothiazepinone compound of Formula I comprises reaction of compound of formula II in the presence of an acid catalyst comprising phosphorus pentoxide and methanesulfonic acid. The dibenzothiazepinone compounds of Formula I are key intermediate for the preparation of 2-(2-(4-dibenzo[b,f][1,4]thiazepine-11-yl-1-piperazinyl)ethoxy)ethanol known as quetiapine and its derivatives, which are effective antipsychotic substances.
COMPOUNDS WITH 7-MEMBER CYCLE AND THE PHARMACEUTICAL USE THEREOF FOR PREVENTING AND TREATING DIABETES AND METABOLISM SYNDROME
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Page/Page column 36, (2010/07/06)
The invention discloses a new use of a class of heptacyclic compounds in the preparation of formulations for the prevention and treatment of diabetes and metabolic syndromes; the present invention also discloses a new class of heptacyclic compounds; the present invention also discloses a process for preparing the heptacyclic compounds and a composition containing the same. The heptacyclic compounds of the present invention can be used to effectively preventing or treating diseases such as diabetes and metabolic syndromes.
AMINO SUBSTITUTED DIARYL[A,D]CYCLOHEPTENE ANALOGS AS MUSCARINIC AGONISTS AND METHODS OF TREATMENT OF NEUROPSYCHIATRIC DISORDERS
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Page/Page column 95-96, (2008/06/13)
Disclosed herein are analogs of clozapine and pharmaceutically acceptable salts, esters, amides, or prodrugs thereof; methods of synthesizing the analogs; and methods of using the analogs for treating neuorpsychiatric disorders. In some embodiments, the analogs are amino substituted diaryl[a,d]cycloheptenes.
IRON CATALYZED CROSS-COUPLING REACTIONS OF IMIDOYL DERIVATIVES
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Page/Page column 21; 50; 51, (2010/11/27)
Disclosed is a process for preparing a compound of formula A - N=C(D)(B), from a compound of formula A-N=C(E)(B) and a compound of formula D-M using an iron catalyst, where the process has is represented by Equation (I).
Iron-catalyzed cross-coupling of imidoyl chlorides with Grignard reagents
Ottesen, Lars K.,Ek, Fredrik,Olsson, Roger
, p. 1771 - 1773 (2007/10/03)
A general, high yielding rapid iron-catalyzed cross-coupling reaction between Grignard reagents and imidoyl chlorides is described. These reactions are typically completed within 5 min, resulting in high yields of 71-96% using 5% iron catalyst in a THF-NM
USE OF N-DESMETHYLCLOZAPINE AND RELATED COMPOUNDS AS DOPAMINE STABILIZING AGENTS
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Page/Page column 113, (2010/11/24)
Disclosed herein is the use of N-desmethylclozapine (NDMC) and related compounds to treat a variety of neuropsychiatric diseases including psychosis. It is shown that NDMC and related compounds are agonists or partial agonists at D2 and D3 dopamine receptors and thus may be effective as a dopamine stabilizing agent, allowing it to be used to treat or provide reduced incidence of Extrapyramidal symptoms (EPS) and/or tardive dyskinesias (TD). Also disclosed is administering NDMC and related compounds in combination with other anti-psychotic agents.
AMINO SUBSTITUTED DIARYL[A,D]CYCLOHEPTENE ANALOGS AS MUSCARINIC AGONISTS AND METHODS OF TREATMENT OF NEUROPSYCHIATRIC DISORDERS
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Page/Page column 93, (2008/06/13)
Disclosed herein are analogs of clozapine and pharmaceutically acceptable salts, esters, amides, or prodrugs thereof; methods of synthesizing the analogs; and methods of using the analogs for treating neuorpsychiatric disorders. In some embodiments, the analogs are amino substituted diaryl[a,d]cycloheptenes.
Atypical antipsychotic agents having low affinity for the D2 Receptor
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, (2008/06/13)
The present invention provides novel compounds of Formula I: The invention further relates to pharmaceutical compositions comprising compounds of Formula I and to methods of using compounds of Formula I to treat neuropsychiatric disorders (e.g., psychosis
MUSCARINIC RECEPTOR LIGANDS
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, (2008/06/13)
Described herein are D4 receptor-selective compounds of the general formula I: STR1 wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5-or 6-membered, homo-or heterocyclic rings;X 1 is selected from CH 2, O, NH, S, C=O, CH--OH, CH--NEt 2, C=CHCl, C=CHCN, N--C. sub.1-4 alkyl, N-acetyl, SO 2 and SO;X 2--is selected from N=, CH 2--, CH=, C(O)--, O--, and S--; n is 1 or 2; andZ is selected from C 1-6 alkyl optionally substituted with a substituent selected from OH, halo, C. sub.1-4 alkyl and C 1-4 alkoxy;and acid addition salts, solvates and hydrates thereof. Their use as ligands for dopamine receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which the M1/M2 receptor is implicated, such as schizophrenia, is also described.
DOPAMINE RECEPTOR LIGANDS
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, (2008/06/13)
Described herein are D4 receptor-selective compounds of the general formula: STR1 wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5-or 6-membered, homo-or heterocyclic rings;X 1 is selected from CH 2, O, NH, S, C=O, CH--OH, CH--N(C 1-4 alkyl) 2, C=CHCl, C= CHCN, N-C 1-4 alkyl, N-acetyl, SO 2 and SO;X. sub.2--is selected from N=, CH 2--, CH=, C(O)--, O--, and S--;R 1 represents C 1-4 alkyl;Y is selected from CH and N;n is 0, 1 or 2;q is 1 or 2;R 2 is C 1-6 alkyl optionally incorporating a heteroatom selected from N, O and S; D is cyclohexane or benzene; andE is a saturated or unsaturated 5-or 6-membered heterocycle incorporating 1, 2 or 3 heteroatoms selected from O, N, and S, wherein E is optionally substituted with 1 or 2 substituents selected from halogen, C 1-4 alkyl and halogen-substituted C 1-4 alkyl;and acid addition salts, solvates and hydrates thereof. Their use as ligands for dopamine receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which the D4 receptor is implicated, such as schizophrenia, is also described.
