Abstract: Derivatives of pyrrolo[2,1-b]benzothiazepines with formula (I) where A is CH—CH2C?CH; R is hydrogen, halogen, C1-C4 alkoxy, C1-C4 alkylthio, C1-C4 alkyl, C5-C6 cycloalkyl; R1 is 1-peperazinyl, 1-homopiperazinyl and 1-piperidinyl; R2 is hydrogen, C1-C4 alkoxy, C1-C4 alkylthio, C1-C4 alkyl, CHO, CH?NOH,CH2OH. The formula (I) compounds are endowed with characteristic atypical anti-psychotic activity, and are therefore useful as medicaments, in particular for the treatment and prevention of schizophrenia, paranoid states, manic-depressive states, disorders of the affective sphere, social regression, personality regression, and hallucinations. Said compounds also present advantageous pharmacokinetic properties.

Abstract: This invention relates to novel compounds having the structural Formula (I) below: and their pharmaceutically acceptable salts, compositions and methods of use thereof. These novel compounds provide a treatment or prophylaxis of at least one symptom or condition associated with schizophrenia and other psychotic disorders, dementia and other cognitive disorders, anxiety disorders, mood disorders, sleep disorders, disorders usually first diagnosed in infancy, childhood, or adolescence, and neurodegenerative disorders.

Abstract: Provided is a novel synthesis of quetiapine, and pharmaceutically acceptable salts thereof, in which an alkali metal halide or siliyl halide is included in the reaction mixture.

Abstract: Disclosed is a process for the preparation of 11-(4-[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl)-dibenzo[b,f][1,4]thiazepine. In the process, low-priced 2,2?-dithiosalicylic acid as starting material is subjected to bond formation reaction with 1-chloro-2-nitrobenzene in a basic aqueous solution, a nitro group reduction reaction is conducted, cyclization and chlorination reactions are simultaneously carried out in the presence of a equivalent amount of halogenating agent, a reaction with piperazine is continuously conducted without separation, and a reaction with 2-haloethoxyethanol is conducted, thereby it is possible to economically producing Quetiapine, that is, 11-(4-[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl)-dibenzo[b,f][1,4]thiazepine, in an environmentally friendly manner.

Abstract: This invention relates to novel compounds having the structural Formula (I) below: and their pharmaceutically acceptable salts or tautomers, compositions and methods of use thereof. These novel compounds provide a treatment or prophylaxis of at least one symptom or condition associated with schizophrenia and other psychotic disorders, dementia and other cognitive disorders, anxiety disorders, mood disorders, sleep disorders, disorders usually first diagnosed in infancy, childhood, or adolescence and neurodegenerative disorders.

Abstract: The present invention is directed to a crystalline form the pharmaceutical compound 11-piperazin-1-yldibenzo[b,f][1,4]thiazepine as well as compositions, preparations, and pharmaceutical uses thereof.

Abstract: The present invention relates to novel crystalline forms of quetiapine hemifumarate, denominated quetiapine hemifumarate form II and quetiapine hemifumarate form III. These novel crystalline forms of quetiapine hemifumarate have been characterized by methods including x-ray powder diffraction (XRD), Fourier transform IR spectroscopy (FTIR), differential scanning calorimetry (DSC), and thermal gravimetric analysis (TGA). Methods for preparation of the novel crystalline quetiapine hemifumarate form II as its chloroform solvate and its dichloromethane solvate, form III as its chloroform solvate, and form I are provided.

Abstract: Formula (I) below: and their pharmaceutically acceptable salts or tautomers, compositions and methods of use thereof. These novel compounds provide a treatment or prophylaxis of at least one symptom or condition associated with schizophrenia and other psychotic disorders, dementia and other cognitive disorders, anxiety disorders, mood disorders, sleep disorders, disorders usually first diagnosed in infancy, childhood, or adolescence and neurodegenerative disorders.

Abstract: This invention relates to novel compounds having the structural Formula I below: and their pharmaceutically acceptable salts or tautomers, compositions and methods of use thereof. These novel compounds provide a treatment or prophylaxis of at least one symptom or condition associated with schizophrenia and other psychotic disorders, dementia and other cognitive disorders, anxiety disorders, mood disorders, sleep disorders, disorders usually first diagnosed in infancy, childhood, or adolescence and neurodegenerative disorders.

Abstract: Compounds the following formula: wherein Z is as described in the specification, pharmaceutically acceptable salts thereof, compositions comprising the same, and methods of treating bipolar disorder, an anxiety disorder, a mood disorder or schizophrenia or other psychotic disorder with said compounds.

Abstract: This invention relates to novel 11-[4-[2-(2-Hydroxyethoxy)ethyl]piperazin-1-yl]dibenzo[b,f][1,4]thiazepine derivatives, their acceptable acid addition salts, solvates, hydrates and polymorphs thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by antagonists of seratonergic 5HT1A and 5HT2 receptors, dopaminergic D1 and D2 receptor, histaminergic H1 receptors, and/or adrenergic ?1 and ?2 receptors.

Abstract: A method for the preparation of salts of 2-[2-(4-dibenzo[b,fj[1,4]thiazepin-11-yl-1-piperazinyl)ethoxy]ethanol (quetiapine) from the quetiapine base and the respective acid, wherein the salt is precipitated from a mixture of solvents, the mixture being either a mixture of an aromatic hydrocarbon and a ketone or ester, or that of an aromatic hydrocarbon, water and a ketone or ester. The salts of quetiapine are purified by partial crystallization, wherein only a part of the salt of quetiapine is dissolved in a C1 to C6 alcohol used.

Abstract: The invention relates to novel compounds and methods of using them for modulating sleep.

Abstract: The invention relates to novel compounds and methods of using them for modulating sleep.

Abstract: The invention relates to novel compounds and methods of using them for modulating sleep.

Abstract: This invention relates to compounds for the inhibition of histone deacetylase. More particularly, the invention provides for compounds of formula compounds of the Formula (I) and N-oxides, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, and racemic and scalemic mixtures, diastereomers and enantiomers thereof, wherein groups L, M, X and Y are as defined herein.

Abstract: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are triphenyl methane analogs. The compounds and compositions can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers, inflammatory, degenerative and vascular diseases, including various ocular diseases, and parasitic infections. Representative triphenyl methane analogs include triphenyl methane analogues of various dyes, hormones, sugars, peptides, oligonucleotides, amino acids, nucleotides, nucleosides, and polyols. The compounds are believed to function by inhibiting tNOX expression, the effects of ROS, and/or the production of HIF2. Thus, the compounds are novel therapeutic agents for a variety of cancers and other diseases.

Abstract: 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 neuropsychiatric disorders. In some embodiments, the analogs are amino substituted diaryl[a,d]cycloheptenes.

Abstract: The present invention relates to a process for preparing and purifying crystalline quetiapine hemifumarate, which comprises preparing crystalline quetiapine hemifumarate via a crystalline salt, which is not a salt of fumaric acid.

Abstract: 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, depression, schizophrenia).

Abstract: The present invention relates to a process for preparing crystalline quetiapine hemifumarate, which comprises crystallizing or re-crystallizing quetiapine hemifumarate from a mixture of water and a water soluble alcohol.

Abstract: 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.

Abstract: The present application describes deuterium-enriched quetiapine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: The invention comprises a process for preparing quetiapine and/or its salts, including, quetiapine fumarate. The process generally comprises reacting dibenzothiazepinone (dibenzo[bf][1,4]thiazepin-11(10H)-one) with phosphorous oxychloride in the presence of triethylamine in an aromatic organic solvent such as toluene or, preferably, xylene at reflux temperature to obtain an aromatic hydrocarbon solution of 11-chloro-dibenzo[bf][1,4]thiazepine. Thereafter, the 11-chloro-dibenzo[bf][1,4]thiazepine is reacted with 2-(2-piperazin-1-ylethoxy)-ethanol to yield, following several processing steps, quetiapine. Compound I can then be further reacted with fumaric acid at elevated temperature to yield quetiapine fumarate. The resulting quetiapine fumarate obtained is suitable for use in pharmaceutical preparations.

Abstract: The present invention is directed to salts the pharmaceutical compound 11-piperazin-1-yldibenzo[b,f][1,4]thiazepine as well as compositions, preparations, and pharmaceutical uses thereof.

Abstract: The present invention relates to a novel polymorph of Quetiapine fumarate and a simple method for its preparation.

Abstract: The present invention relates to 11-(piperazin-1-yl)dibenzo[b,f][1,4]oxazapine compounds of the formula: where the variables are as defined herein, their salts and pharmaceutically acceptable compositions thereof. Methods of preparing these compounds are also described. These compounds may be used in the treatment of disorders such as schizophrenia, treatment resistant schizophrenia, bipolar disorder, psychotic depression, treatment resistant depression, schizophrenia-associated depression, treatment resistant OCD, autism, senile psychosis, psychotic dementia, L-DOPA induced psychosis, psychogenic polydipsia, psychotic symptoms of neurological disorders, sleep disorders.

Abstract: A process for the preparation of an 11-(4-substituted-1-piperazinyl)dibenzo[b,f][1,4]thiazepine derivative, of general Formula (I), where A is hydrogen or a —(CH2)2—OH group or a —(CH2)2-0-(CH2)2—OH group, or of a salt thereof, comprises a step in which 10H-dibenzo[b,f][1,4]thiazepin-11-one is reacted with a piperazine derivative in the presence of a titanium alkoxide of general formula Ti(OR)4, where R is a straight or branched alkyl group, having from one to eight carbon atoms to obtain said Formula I derivative or a salt thereof. Where A is —CH2)2-0-(CH2)2—OH, then the piperazine derivative is 1-(2-(2-hydroxyethoxy)ethyl)piperazine and the 11-(4-substituted-1-piperazinyl)dibenzo[b,f][1,4]thiazepine is quetiapine, (11-(4-(2-(2-hydroxyethoxy)ethyl)-1-piperazinyl)dibenzo[b,f][1,4]thiazepine). The process may comprise an additional step of reacting the quetiapine with fumaric acid to obtain quetiapine hemifumarate.

Abstract: The invention is directed to compositions and methods useful for treating Central Nervous System (CNS) disorders. Furthermore, the invention provides compositions and methods of treating sleep disorders. More specifically, the invention is directed to the compositions and use of derivatized, histamine antagonists for the treatment of sleep disorders.

Abstract: The present invention relates to novel polymorphic forms of quetiapine fumarate, processes for their preparation and pharmaceutical compositions containing them.

Abstract: Provided is a novel synthesis of quetiapine employing phase transfer catalyst.

Abstract: 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, depression, schizophrenia).

Abstract: The present invention relates to novel polymorphic forms of quetiapine fumarate, processes for their preparation and pharmaceutical compositions containing them.

Abstract: Provided is a novel synthesis of quetiapine employing phase transfer catalyst.

Abstract: The present invention relates to novel crystalline forms of quetiapine hemifumarate, denominated quetiapine hemifumarate form II and quetiapine hemifumarate form III. These novel crystalline forms of quetiapine hemifumarate have been characterized by methods including x-ray powder diffraction (XRD), Fourier transform IR spectroscopy (FTIR), differential scanning calorimetry (DSC), and thermal gravimetric analysis (TGA). Methods for preparation of the novel crystalline quetiapine hemifumarate form II as its chloroform solvate and its dichloromethane solvate, form III as its chloroform solvate, and form I are provided.

Abstract: The present invention provides novel compounds of Formula I: 1

Abstract: Crystalline 11-(4-[2-(2-hydroxyethoxy) ethyl]-1-piperazinyl)-dibenzo[b,f] [1,4]thiazepine (I) may be prepared by crystallising 11-(4-[2-(2-hydroxyethoxy) ethyl]-1-piperazinyl)-dibenzo[b,f] [1,4]thiazepine from a non-aromatic solvent such as ethyl acetate, isobutyl acetate, methyl iso-butylketone or methyl tert-butyl ether, preferably in the absence of water. The crystalline material produced may be converted into a pharmaceutically acceptable salt such as a fumarate. The crystalline 11-(4-[2-(2-hydroxyethoxy) ethyl]-1-piperazinyl)-dibenzo [b,f] [1,4]thiazepine may be used to treat psychoses.

Abstract: Polycondensated heterocycles with a pyrrole[2,1-b][1,3]benzothiazepine structure of the following formula (I) where the groups are defined as in the description are disclosed. As compared to known antipsychotic agents, these compounds present substantial activity associated with a simultaneous reduction in unwanted extrapyramidal symptoms. These compounds can be formulated in pharmaceutical compositions for the treatment of psychoses such as, for example, schizophrenia.

Abstract: Crystalline 11-(4-[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl)-dibenzo[b,f][1,4]thiazepine (I) may be prepared by crystallizing 11-(4-[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl)-dibenzo[b,f][1,4]thiazepine from a non-aromatic solvent such as ethyl acetate, isobutyl acetate, methyl iso-butylketone or methyl tert-butyl ether, preferably in the absence of water. The crystalline material produced may be converted into a pharmaceutically acceptable salt such as a fumarate. The crystalline 11-(4-[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl)-dibenzo[b,f][1,4]thiazepine may be used to treat psychoses.

Abstract: The invention relates to substituted 1,4-benzothiazepine-1,1-dioxide derivatives and their acid addition salts. 1,4-Benzothiazepine-1,1-dioxide derivatives of formula 1, wherein R1, R2, R3, and Z have the meanings indicated in the specification, physiologically tolerable salts, and physiologically functional derivatives thereof, and also processes for their preparation, are described. The compounds are suitable, for example, as hypolipidemics.

Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, A, X, T, Q, Z, U, Y, Ar, p and n are as defined in the specification. These compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).

Abstract: This invention relates to certain heterocyclic compounds and their pharmaceutically acceptable salts, which are useful for sensitizing multidrug-resistant tumor cells to anticancer agents and multidrug resistant forms of malaria, tuberculosis, leishmania and amoebic dysentery to chemotherapeutants. The compounds and their pharmaceutically acceptable salts are also inhibitors of the active drug transport capability of P-glycoprotein which is encoded by the human MDR1 gene, as well as of certain other related ATP-binding-cassette transporters from eukaryotic and prokaryotic organisms (e.g., pfmdr from Plasmodium falciprum, and murine mdr1 and mdr3 gene products).

Abstract: A compound represented by the formula (I) or (II) or a salt thereof wherein R' represents hydrogen atom or a C.sub.1-6 alkyl group; R.sup.2 and R.sup.3 independently represent a hydrogen atom or a C.sub.1-6 alkyl group, or R.sup.2 and R.sup.1 may combine together to represent a 5- or 6-membered cycloalkyl group; R.sup.4 represents, for example, a hydrogen atom or a C.sub.1-6 alkyl group; R.sup.4 represents, for example, a hydrogen atom or a C.sub.1-6 alkyl group; R.sup.6 represents a hydrogen atom or a C.sub.1-6 alkyl group; X represents --NR.sup.7 --, --O--, --CHR.sup.7 -- or --S-- in which R.sup.7 represents, for example, a hydrogen atom or a C.sub.1-6 alkyl group; and Y represents a phenylene group or a pyridinediyl group. The compounds are useful as agents for enhancing the activities of retinoid compounds.

Abstract: 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.sub.1 is selected from O, S, SO, SO.sub.2, CH.sub.2, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCl, and C.dbd.CHCN;X.sub.2 --- is selected from N.dbd., CH.sub.2 --, CH.dbd. and C(O)--;n is 1 or 2;R.sub.1 is selected from H and the .alpha.-carbon side chain of an amino acid;R.sub.2 and R.sub.3 are selected independently from H, OH, --NH.sub.2, --C(O)NH.sub.2 .dbd.O, .dbd.S,halo,cyano, C.sub.1-9 alkyl, C.sub.1-9 alkoxy, C.sub.1-4 alkylS--, C.sub.1-4 alkylSO--, C.sub.1-4 alkylSO.sub.2 --, phenoxy, benzyloxy and piperonyloxy; andH* is in either the R- or the S-configuration,and acid addition salts, solvates and hydrates thereof.

Abstract: 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.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCl, C.dbd.CHCN, N--C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO;X.sub.2 . . . is selected from N.dbd., CH.sub.2 --, CH.dbd., C(O)--, O--, and S--;Y is selected from N and CH;R.sub.1 represents C.sub.1-4 alkyl;n is 0, 1 or 2;q is 1 or 2; andZ is C.sub.5-10 alkyl optionally substituted with OH, halo, C.sub.1-4 alkyl or C.sub.1-4 alkoxy and optionally incorporating a heteroatom selected from O, N and S;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.

Abstract: 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.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCl, C.dbd.CHCN, N--C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO;X.sub.2 - - - is selected from N.dbd., CH.sub.2 --, CH.dbd., C(O)--, O--, and S--;Y is selected from CH and N;Z is cyanoR.sub.1 represents C.sub.1-4 alkyl;m is 0, 1, 2 or 3;n is 0, 1 or 2;q is 1 or 2; andD is a 5, 6 or 7-membered, saturated or unsaturated, homo- or heterocyclic ring; 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.

Abstract: 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.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCl, C.dbd.CHCN, N-C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO;X.sub.2 - - - is selected from N.dbd., CH.sub.2 --, CH.dbd., C(O)--, O--, and S--;n is 1 or 2;R.sub.1 is selected from H and an amino acid side chain;R.sub.2 is selected from H, OH, C.sub.1-9 alkyl, C.sub.1-9 alkoxy, and benzyloxy; andR.sub.3 is selected from H, OH, halo, cyano, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, phenoxy, benzyloxy, .dbd.O, .dbd.S, C.sub.1-4 alkylsulfonyl, C.sub.1-4 alkylsulfonyl, C.sub.1-4 alkylthio, amino, and aminocarbonyl;and acid addition salts, solvates and hydrates thereof.

Abstract: 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.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--NEt.sub.2, C.dbd.CHCl, C.dbd.CHCN, N--C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO;X.sub.2 --is selected from N.dbd., CH.sub.2 --, CH.dbd., C(O)--, O--, and S--;n is 1 or 2; andZ is selected from C.sub.1-6 alkyl optionally substituted with a substituent selected from OH, halo, C.sub.1-4 alkyl and C.sub.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.

Abstract: 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.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCl, C.dbd.CHCN, N-C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO;X.sub.2 -- is selected from N.dbd., CH.sub.2 --, CH.dbd., C(O)--, O--, and S--;R.sub.1 represents C.sub.1-4 alkyl;Y is selected from CH and N;n is 0, 1 or 2;q is 1 or 2;R.sub.2 is C.sub.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.sub.1-4 alkyl and halogen-substituted C.sub.1-4 alkyl;and acid addition salts, solvates and hydrates thereof.