The invention concerns venlafaxine-N-oxide and O-desmethylvenlafaxine-N-oxide as prodrugs of venlafaxine and its major (active) metabolite O-desmethylvenlafaxine respectively, to pharmaceutical compositions containing these N-oxides, to methods for preparing them, and methods for preparing compositions. The invention relates to N-oxide, having formula (1), wherein R1 is H or CH3, and tautomers, stereoisomers, hydrates and solvates thereof. The invention also relates to the uses of the N-oxides and compositions, particularly for the manufacture of medicaments useful in the treatment of affections or diseases effectively treatable - albeit with side effects - with venlafaxine.
C07C 291/04 - Compounds containing carbon and nitrogen and having functional groups not covered by groups containing nitrogen-oxide bonds containing amino-oxide bonds
A61K 31/135 - Amines, e.g. amantadine having aromatic rings, e.g. methadone
The invention concerns sildenafil N-oxide as prodrug, to pharmaceutical compositions containing this compound, to methods for preparing it, and methods for preparing compositions. The invention relates to 1-[[3-(6,7-dihydro-1-methyl-7-oxo-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-5-yl)-4-ethoxyphenyl]sulfonyl]-4-methyl-4-oxido-piperazine having formula (1A) and pharmacologically acceptable salts, hydrates and solvates thereof. The invention also relates to uses of the compound, and compositions containing it, particularly for the manufacture of medicaments useful in the treatment of affections or diseases effectively treatable - albeit with side effects - with sildenafil.
This invention relates to 4,5-dihydro-(1 H)-pyrazole (pyrazoline) derivatives as cannabinoid CB1 receptor modulators, to pharmaceutical compositions containing these compounds, to methods for their syntheses, methods for preparing novel intermediates useful for their syntheses, and methods for preparing compositions. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in disorders in which CB1 receptors are involved, or that can be treated via manipulation of those receptors. The compounds have formula (I) wherein the symbols have the meanings given in the specification.
C07D 231/06 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 409/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
4.
HETEROCYCLIC COMPOUNDS WITH AFFINITY TO MUSCARINIC RECEPTORS
Terwel, Louise, Heir Of Reinders, Jan H. (deceased)
Abstract
The present invention relates to heterocyclic compounds of the formula (I) wherein - the heterocycle comprises two double bonds which may be present at several positions, represented by the dashed lines ( -- ); - the heterocycle contains two heteroatoms, - W being N or NH; - Y being CH, O or NH, wherein if Y is O, X1 is CH and X2 is the residue C-Z-R2 or C-R3, wherein Z is NH, O, or S; and if Y is CH or NH, one of X1 and X2 is CH or N, the other being the residue C-Z-R2 or C-R3, wherein Z is NH or S; - R1 is selected from the structures (a), (b) and (c): - R2 is selected from (C1-C10)alkyl, (C2-C10)alkenyl and (C2-C10)alkynyl, optionally independently substituted with one or more substituents selected from halogen, hydroxy, cyano, oxo, (C1-C6)alkoxy, (C1-C6)alkylthio, (C1-C6)alkenyloxy, (C1-C6)alkenylthio, (C1-C4)alkoxy(C1-C4)alkoxy, (C5-C7)cycloalkyl, a 5-membered unsaturated heterocycle (optionally substituted with halogen), phenyl, phenyloxy and phenylthio, wherein the phenyl group is optionally substituted with halogen; or - R2 is an unbranched (C2-C8)alkyl substituted at the Za-symbol of a group with the formula (Ia) wherein if X1 is CH or N1 X1 is CH or N and X2a is C-Za-, or if X1 is C-Z-R2, X1a is C-Za- and X2a is CH or N; and the symbols Wa, Ya and Za and the substituent R1a have the same meanings as defined previously for the symbols W, Y and Z and the substituent R1, and are not independently selected, each of the symbols Wa, Ya and Za and the substituent R1 a representing identical symbols and substituents, respectively, as the symbols W, Y and Z and the substituent R1 in the other part of the structure of formula (I); - R3 is selected from (C4-C10) alkyl, (C2-C10) alkenyl and (C2-C10) alkynyl, optionally independently substituted with one or more substituents selected from halogen, hydroxy, cyano, (C1C6) alkoxy, (C1C6) alkylthio, (C1C6)alkenyloxy, (C1C6) alkenylthio, (C1-C4) alkoxy (C1-C4) alkoxy, (C5-C7) cycloalkyl, a 5-membered unsaturated heterocycle optionally substituted with halogen, phenyl, phenyloxy and phenylthio, wherein the phenyl group is optionally substituted with halogen; or a pharmaceutically acceptable salt, a solvate or hydrate thereof. The compounds of the invention have affinity to muscarinic receptors and may be used in the treatment, alleviation or prevention of muscarinic receptor mediated diseases and conditions.
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 413/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/4427 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems
A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
C07D 453/02 - Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
5.
USE OF 5-HT6 ANTAGONISTS TO PREVENT RELAPSE INTO ADDICTION
The invention relates to a novel use of compounds and pharmaceutically acceptable salts thereof, which are 5-HT6 antagonists. These compounds are useful for the preparation of medicaments for preventing relapse into addiction, in particular relapse into addiction to substances of abuse, including opiates, hallucinogens, inhalants, phencyclidine, amphetamines, cocaine, cannabis, nicotine, and alcohol, into relapse to addiction to certain medicines, including sedatives, hypnotics and anxiolytics, and into relapse to certain addictive behaviors, including gambling.
This invention relates to compounds with a combination of cannabinoid-CB1antagonism and serotonin reuptake inhibition to pharmaceutical compositions containing these compounds, to methods for preparing the compounds, methods for preparing novel intermediates useful for their synthesis, and methods for preparing compositions. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in psychosis, anxiety, depression, attention deficits, cognitive disorders, obesity, drug dependence, Parkinson's disease, Alzheimer's disease, pain disorders, neuropathic pain disorders and sexual disorders. In particular the invention relates to compoundsof the general formula (I): wherein the symbols have the meanings given in the specification.
C07D 231/06 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
C07D 233/90 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/4155 - 1,2-Diazoles not condensed and containing further heterocyclic rings
Thisinvention concerns compounds with a combination of cannabinoid-CB1 antagonism and cholinesterase inhibition, to pharmaceutical compositions containing these compounds, to methods for preparing the compounds, methods for preparing novel intermediates useful for their synthesis, and methods for preparing compositions. The invention also relates to the uses of such compounds and compositions, particularly for treating Alzheimer's disease, cognitive disorders, memory disorders, dementia, attention deficits, traumatic brain injury, drug dependence, addiction and substance abuse. In particular the invention relates to compounds of the general Formula (1) wherein the symbols have the meanings given in the specification.
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/473 - QuinolinesIsoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
A61P 25/30 - Drugs for disorders of the nervous system for treating abuse or dependence
This invention concerns selective inhibitors of neurotensin degrading enzymes, to pharmaceutical compositions containing these compounds, to methods for preparing the compounds, methods for preparing novel intermediates useful for their synthesis, and methods for preparing compositions. The invention also relates to the uses of such compounds and compositions, particularly their use in the manufacture of medicaments for regulatingblood pressure orgastric emptying, or treating Parkinson s disease, anxiety, depression,orpsychosis. The compounds have the general formula (1) wherein the symbols have the meanings given in the specification.
The present invention relates to a thermostable solid composition containing nanosized micelles, the micelles containing a poorly soluble chemical substance, such as a biologically active substance, dissolved in an auxiliary material, and the micelles being embedded in a water soluble carrier. The invention further relates to a process for preparing a thermostable solid composition and to a process for preparing pharmaceutical dosage forms comprising the same.
A61K 47/36 - PolysaccharidesDerivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
10.
SULFONYLPYRAZOLINE CARBOXAMIDINE DERIVATIVES AS 5-HT6 ANTAGONISTS
This invention concerns sulfonylpyrazoline carboxamidine derivatives as antagonists of 5-HT6 receptors, to methods for the preparation of these compounds and to novel intermediates useful for their synthesis. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in Parkinson's disease, Huntington's chorea, schizophrenia, anxiety, depression, manic depression, psychoses, epilepsy, obsessive compulsive disorders, mood disorders, migraine, Alzheimer's disease, age related cognitive decline, mild cognitive impairment, sleep disorders, eating disorders, anorexia, bulimia, binge eating disorders, panic attacks, akathisia, attention deficit hyperactivity disorder, attention deficit disorder, withdrawal from abuse of cocaine, ethanol, nicotine or benzodiazepines, pain, disorders associated with spinal trauma or head injury, hydrocephalus, functional bowel disorder, Irritable Bowel Syndrome, obesity and type-2 diabetes. The compounds have the general formula (1), wherein the symbols have the meanings given in the description.
C07D 231/06 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 231/12 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
A61K 31/4155 - 1,2-Diazoles not condensed and containing further heterocyclic rings
A61P 25/00 - Drugs for disorders of the nervous system
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 407/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 407/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 409/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
11.
TITRATION SCHEDULE FOR BIFEPRUNOX FOR TREATING SCHIZOPHRENIA AND KITS FOR USE THEREIN
The present invention is directed to the use of a bifeprunox compound for a titration kit for a titration schedule to facilitate the initiation of the treatment of at least one central nerv ous s ystem condition or disorder by administering a plurality of dosage units of a comprising a compound 7-[4-([1,1'-biphenyl]-3-ylmethyl)-1-piperazinyl]-2(3H)- benzoxazolone (INN bifeprunox).
The present disclosure is directed to a daily dose of bifeprunox for the treatment of a patient with schizophrenia. Such dose is effectively used in methods for treating schizophrenia comprising administering to a patient a pharmaceutical composition comprising an effective amount of at least one bifeprunox compound, amongst other effects, resulting in a reduction of side effects associated with schizophrenia treatment such as: no weight gain, improvement of non-fasting triglyceride levels and/or total cholesterol levels. Treatment effects are e.g. a reduction of PANSS total score in a patient and an increase of the time to deterioration of schizophrenia and improvement of psychotic symptoms.
The invention concerns azaindole derivatives having the general formula (I) wherein the symbols have the meanings given in the specification. These compounds have a combination of partial nicotinic acetylcholine receptor agonism and dopamine reuptake inhibition. The invention also relates to pharmaceutical compositions containing these compounds, to methods for preparing them, methods for preparing novel intermediates useful for their synthesis, methods for preparing compositions, and uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in disorders in which nicotinic receptors and/or dopamine transporters are involved, or that can be treated via manipulation of those receptors.
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
A61P 25/30 - Drugs for disorders of the nervous system for treating abuse or dependence
A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
14.
ORAL PHARMACEUTICAL COMPOSITION OF A POORLY WATER-SOLUBLE ACTIVE SUBSTANCE
Provided in the present invention are improved oral pharmaceutical compositions comprising at least one poorly water soluble active agent, preferably endothelin conversion enzyme (ECE) inhibitor and/or neutral endopeptidase (NEP) inhibitor in an amount greater than 10% w/w of the composition, more preferably, with the alkali system co mprising a mixture of at least two alkaline compounds in the ratio 1:20 to 20:1, the active agent is SLV-306 or its pharmaceutically acceptable salts, esters, hydrates, solvates, isomers or derivatives thereof; a alkali system in an amount greater than 10% w/w of the composition preferably comprising a mixture of at least two alkaline compounds and optionally one or more pharmaceutically acceptable excipients. Also provided are process for preparation of such improved compositions and method of using such composition.
A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
A61K 45/08 - Mixtures of an active ingredient and an auxiliary substance neither being chemically characterised, e.g. antihistaminicum and surface active substance
15.
ORAL PHARMACEUTICAL COMPOSITION OF A POORLY WATER-SOLUBLE ACTIVE SUBSTANCE
The invention is related to an oral composition of Benzazepin-1-acetic acid derivatives comprising a) said active compound in an amount of between 10 and 65% of the total weight of the formulation; b) at least 10% w/w an alkaline compound or a mixture of alkaline compounds; c) optionally comprises auxiliary materials an amount of between 1% and 45% of the total weight of the formulation. The invention is further related to the above defined oral composition comprising sodium carbonate with a specific particle size and/or surface area as alkaline compound.
A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
A61K 45/08 - Mixtures of an active ingredient and an auxiliary substance neither being chemically characterised, e.g. antihistaminicum and surface active substance
16.
COMBINATION PREPARATIONS COMPRISING SLV308 AND A L-DOPA
The invention concerns the use of a combination preparation of SLV308 or its N-oxide, or pharmacologically acceptable salts of those compounds (I), (II) and L-DOPA, for simultaneous, separate or sequential use in the treatment of disorders requiring recovery of dopaminergic function, in particular Parkinson's disease and restless leg syndrome.
The invention concerns the use of a combination preparation of bifeprunox or its N-oxide, or pharmacologically acceptable salts of those compounds: and L-DOPA, for simultaneous, separate or sequential use in the treatment of disorders requiring recovery of dopaminergic function, in particular Parkinson's disease and restless leg syndrome.
The present invention relates to sulphur containing pyrazole derivatives, and their S-oxidized active metabolites, as selective cannabinoid CB1 receptor antagonists having a high CB1/CB2 receptor subtype selectivity, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said pyrazole derivatives, to pharmaceutical compositions comprising one or more of these pyrazole derivatives as active ingredients, as well as to the use of these pharmaceutical compositions for the treatment of psychiatric and neurological disorders. The compounds have the general formula (I) wherein the symbols have the meanings given in the specification.
The invention relates to a novel use of compounds and pharmaceutically acceptable salts thereof, which are muscarinic, in particular muscarine-1 (M1) agonists. These compounds are useful for the preparation of medicaments for treatment, amelioration or prevention of impulse control disorders. These include impulse control disorders 'Not Elsewhere Classified' such as intermittent explosive disorder, pyromania, kleptomania, pathological gambling and trichotillomania; and impulse control disorders 'Not Otherwise Specified' such as: compulsive buying disorder, binge eating and binge drinking disorder, impulsive self-injurious behaviour such as pathological skin picking, nail-biting and nose-picking, gouging, head banging and self- biting; paraphilic sexual addictions, including exhibitionism, fetishism, frotteurism, pedophilia, masochism, sadism, transvestic fetishism and voyeurism; compulsive Internet use and excessive mobile phone use.
A61K 31/00 - Medicinal preparations containing organic active ingredients
A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia
20.
N-OXIDES OF PYRIDYLMETHYLPIPERAZINE AND -PIPERIDINE DERIVATIVES
The invention concerns N-oxides of certain pyridylmethylpiperazine and -piperidine derivatives as alternatives or as ◠prodrugs' of their respective parent compounds, to pharmaceutical compositions containing these N-oxides, to methods for preparing them, and methods for preparing compositions. The invention relates to N-oxides of compounds having formula (a), wherein the symbols have the meanings given in the description, and wherein the oxidized nitrogen atom may be the nitrogen atom in the pyridyl ring of R5, or the nitrogen atom in the piperidine ring (when Z is carbon) or either one of the nitrogen atoms in the piperazine ring (when Z is nitrogen), or b똫th the nitrogen atom connected to R5 via a methylene group, ánd the nitrogen atom in the pyridyl ring of R5, and tautomers, stereoisomers, pharmacologically acceptable salts, hydrates and solvates thereof. The invention also relates to the uses of such N-oxides and compositions, particularly for the manufacture of a medicament useful in the treatment of affections or diseases of the central nervous system caused by disturbances in either the dopaminergic or serotinergic systems, for example Parkinson's disease, aggression, anxiety disorders, autism, vertigo, depression, disturbances of cognition or memory and in particular schizophrenia and other psychotic disorders.
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
This invention is directed to 4,5-dihydro -(1 H)-pyrazole (pyrazoline) derivatives as cannabinoid CB1 receptor modulators, to pharmaceutical compositions containing these compounds, to methods for the preparation of these compounds, methods for preparing novel intermediates useful for their synthesis, and methods for preparing compositions. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in disorders in which CB1 receptors are involved, or that can be treated via manipulation of those receptors. The compounds have the general formula (I) wherein the symbols have the meanings given in the specification.
C07D 231/06 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
A61P 25/00 - Drugs for disorders of the nervous system
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 405/06 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 409/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 409/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07C 49/213 - Unsaturated compounds containing keto groups bound to acyclic carbon atoms containing six-membered aromatic rings
The present invention provides a salt form, and compositions thereof, useful as a modulator of one or more GPCRs and which exhibits desirable characteristics for the same. The present invention also provides methods for preparing said salt form, which is derived from 8-4-⏧3-(5-fluoro- 1 H-indol-3-yl)-propyl] -piperazin- 1 -yl } -2-methyl-4H- benzo⏧l,4]oxazin-3-one and glucuronic acid.
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/538 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia
23.
N-OXIDES AS PRODRUGS OF PIPERAZINE & PIPERIDINE DERIVATIVES
The present invention relates to N-oxides of certain piperazine and piperidine derivatives and to methods for the preparation of these compounds. The invention also relates to the use of compounds disclosed herein for the manufacture of a medicament giving a beneficial effect. A beneficial effect is disclosed herein or apparent to a person skilled in the art from the specification and general knowledge in the art. The invention also relates to the use of a compound of the invention for the manufacture of a medicament for treating or preventing a disease or condition. More particularly, the invention relates to a new use for the treatment of a disease or condition disclosed herein or apparent to a person skilled in the art from the specification and general knowledge in the art. In embodiments of the invention specific compounds disclosed herein are used for the manufacture of a medicament useful in the treatment of CNS-disorders, in particular the treatment of anxiety disorders, including generalized anxiety disorder and panic disorder, obsessive compulsive disorder, aggression, addiction (including craving), depression, autism, vertigo, schizophrenia and other psychotic disorders, Parkinson's disease and disturbances of cognition and memory. The compounds have the general formula (1) wherein the symbols have the meanings given in the specification.
C07D 263/58 - BenzoxazolesHydrogenated benzoxazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
A61K 31/423 - Oxazoles condensed with carbocyclic rings
A61P 25/00 - Drugs for disorders of the nervous system
patents