93535-13-8

Upstream product

• 92161-65-4 methyl 2-((4-chloro-2-nitrophenyl)thio)benzoate 

Downstream Products

• 3158-80-3 8-chloro-10H-dibenzo[b,f][1,4]thiazepin-11-one 

Relevant academic research and scientific papers

AMINO SUBSTITUTED DIARYL[A,D]CYCLOHEPTENE ANALOGS AS MUSCARINIC AGONISTS AND METHODS OF TREATMENT OF NEUROPSYCHIATRIC DISORDERS

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.

USE OF N-DESMETHYLCLOZAPINE AND RELATED COMPOUNDS AS DOPAMINE STABILIZING AGENTS

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

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.

BICYCLIC NONANE AND DECANE COMPOUNDS HAVING DOPAMINE RECEPTOR AFFINITY

Described herein are D4 receptor-selective compounds of the general formula: STR1 wherein: A and B are independently selected, substituted or unsubstituted, unsaturated 5-or 6-membered, homo-or heterocyclic rings;X 1 is selected from O, S, SO, SO 2, CH. sub.2, C=O, CH--OH, CH--N(C 1-4 alkyl) 2, C= CHCl, and C=CHCN;X 2---is selected from N= , CH. sub.2--, CH= and C(O)--;n is 1 or 2; R 1 is selected from H and the α-carbon side chain of an amino acid;R 2 and R 3 are selected independently from H, OH,--NH 2,--C(O)NH 2 =O, =S,halo, cyano, C 1-9 alkyl, C 1-9 alkoxy, C 1-4 alkylS--, C 1-4 alkylSO--, C 1-4 alkylSO 2--, phenoxy, benzyloxy and piperonyloxy; andH* is in either the R-or the S-configuration,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.

DOPAMINE RECEPTOR LIGANDS

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.

MUSCARINIC RECEPTOR LIGANDS

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.