Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6a, R6b, R7, R8, R9, X, b, k, m, and n, and the dashed lines are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.

Abstract: The present invention relates to novel heteroaryl diazabicycloalkane derivatives represented by general formula (I), any of its enantiomers or any mixture thereof, an N oxide thereof, a pharmaceutically acceptable salt thereof, in a labelled or un-labelled form, which are found to be cholinergic ligands at the nicotinic Acetyl Choline Receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neurodegeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.

Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6a, R6b, R7, R8, R9, X, b, k, m, and n, and the dashed lines are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.

Abstract: This invention provides [1,4]diazepino[6,7,1-jk]carbazole compounds of the formula: wherein: R1 and R2 are H, alkyl, alkoxy, halogen, fluorinated alkyl, —CN, —NH—SO2-alkyl, —SO2—NH-alkyl, alkyl amide, amino, alkylamino, dialkylamino, fluorinated alkoxy, acyl, phenoyl or thiophenoyl; R3, R4, R5 and R6 are H, alkyl, cycloalkyl, alkoxy or cycloalkoxy; R7 is H or alkyl; R8 is H or alkyl; and the dashed line indicates an optional double bond; or a pharmaceutically acceptable salt thereof, as well as methods and pharmaceutical compositions utilizing them for the treatment or prevention of disorders such as obsessive-compulsive disorder, depression, anxiety, schizophrenia, migraine, sleep disorders, eating disorders, obesity, epilepsy, and spinal cord injury.

Abstract: Disclosed is an acyl group-containing hexaazaisowurtzitane derivative represented by the following formula (I): W At Q(6−t), wherein t represents an integer of from 4 to 6, A independently represents an acyl group having 1 to 10 carbon atoms, each Q independently represents a hydrogen atom or an alkyl group having 1 to 10 carbon atoms, and W represents a hexavalent hexaazaisowurtzitane residue represented by the following formula (II): Also disclosed is a method for producing the above-mentioned acyl group-containing hexaazaisowurtzitane derivative. The acyl group-containing hexaazaisowurtzitane derivative of the present invention is useful as a precursor of a polynitrohexaazaisowurtzitane derivative which can be used not only as a material for explosives but also as an additive for propellants and explosives.

Abstract: The present invention provides a pyrrolidine compound of the formula (I) wherein each symbol is as defined in the specification, an optically active compound thereof and a pharmaceutically acceptable salt thereof. The present invention further provides a pharmaceutical composition containing a compound of the formula (I), an optically active compound thereof, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable additive. The compound of the present invention has a serotonin 2 receptor antagonistic action along with a platelet aggregation suppressive action, a peripheral circulation improving action and a lacrimation promoting action. Therefore, the compound of the present invention can be a useful medicine showing effect against thrombotic embolism, dry eye and the like.

Abstract: Compounds are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, including stroke.

Abstract: This invention provides compounds of the formula: 1

Abstract: This invention provides compounds of formula I having the structure 1

Abstract: The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.

Abstract: This invention provides compounds of the formulae: 1

Abstract: The present invention relates to novel N12, N13-bridged sugar derivatives of indolylopyrrolocarbazoles and pharmaceutical formulations thereof which exhibit topoisomerase-I activity and are useful in inhibiting the proliferation of tumor cells.

Abstract: Disclosed are the compounds Asamarine A and B, novel cytotoxic diterpene-alkaloids, that have been isolated from the sponge Raspailia sp. The structure of these compounds have been established on the basis of NMR data and confirmed by X-ray analysis. Also disclosed are compounds (I) and (II), wherein wherein R1 represents hydrogen or lower alkyl or lower alkanoyl; R2 represents hydrogen or lower alkyl; R3 is either an alkyl or a cycloalkyl group containing one or more isoprene units, or a monoterpene or a sesquiterpene or a sesquiterpene or a diterpene group; R4 or R5 represent hydrogen or lower alkyl; R6 represents lower alkyl; and X represents F or Cl or Br or I.

Abstract: This invention provides [1,4]diazepino[6,7,1-jk]carbazole compounds of the formula: 1

Abstract: This invention provides processes for synthesizing compounds of formula I: 1

Abstract: This invention provides a process for the preparation of 1, 2, 3, 4, 8, 9, 10, 10a-octahydro-7bH-cyclopenta[b][1,4]diazepino[6, 7, 1-hi]indole derivatives of the general formula: 1

Abstract: The present invention provides processes for the preparation of 1, 2, 3, 4, 8, 9, 10, 10a-octahydro-7bH-cyclopenta[b][1, 4]diazepino[6, 7, 1-hi]indole derivatives of the general formula: 1

Abstract: The present invention relates to novel heteroaryl diazabicycloalkane derivatives represented by general formula (I), any of its enantiomers or any mixture thereof, an N oxide thereof, a pharmaceutically acceptable salt thereof, in a labelled or un-labelled form, which are found to be cholinergic ligands at the nicotinic Acetyl Choline Receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neurodegeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.

Abstract: The present invention is directed to novel fused aryl and heteroaryl bridged indenopyrrolocarbazoles which are useful, inter alia, as therapeutic agents. The invention is also directed to methods for making and using the bridged indenopyrrolocarbazoles.

Abstract: Novel compounds of the formula wherein the substituents are defined as in the application having antibiotic properties.

Abstract: A nitro group-containing hexaazaisowurtzitane derivative represented by the following general formula (I): W An N(6−n)  (I) wherein n is an integer of 4 or 5, A is an acyl group having 1-10 carbon atoms with each acyl group being the same as or different from one or more of the others, N is a nitro group and W is a hexavalent hexaazaisowurtzitane residue represented by the following formula (II): a nitroso group-containing hexaazaisowurtzitane derivative represented by the following general formula (III): W An NS(6−n)  (III) wherein n is an integer of 4 or 5, A is an acyl group having 1-10 carbon atoms with each acyl group being the same as or different from one or more of the others, NS is a nitroso group and W is a hexavalent hexaazaisowurtzitane residue of formula (II) above, and an acyl group-containing hexaazaisowurtzitane derivative represented by the following general formula (IV): W Am H(6−m)  (IV) wherein N is an integer of 4-6,

Abstract: A method for acylating a hexakis (arylmethyl) hexaazaisowurtzitane (WB6) by reductively removing the arylmethyl groups in the presence of an acylating agent, characterized by contacting a WB6 (a) with a heterogeneous system reduction catalyst (b) in the presence of an acylating agent (c) and a reducing agent (d) in a solvent (e) for the WB6 (a) to reductively remove the arylmethyl groups from the WB6 (a) and acylate the same, and by preventing the WB6 (a) and the catalyst (b) from being contacted with each other when at least either of the acylating agent (c) and the reducing agent (d) is not present. In this method, the decomposition of the WB6 skeleton, which readily occurs in the beginning of the acylation of the WB6 as a starting material, can be highly effectively inhibited. This method can hence stably produce a tetraacylhexaazaisowurtzitane derivative in a high yield and is industrially advantageous.

Abstract: Processes and compositions for nitration of N-substituted isowurtzitane compounds with concentrated nitric acid at elevated temperatures to form HNIW and recovery thereof with high yields and purities. Polymorphic conversions to the epsilon HNIW crystal form at quanititative yields are also described.

Abstract: Disclosed is a method for producing an acyl group-containing hexaazaisowurtzitane derivative represented by the following formula (1),WA.sub.n H.sub.(6-n) (1)wherein n represents an integer of 4 or 6, each A independently represents an acyl group having 1 to 10 carbon atoms, H represents a hydrogen atom, and W represents a hexavalent hexaazaisowurtzitane residue represented by the following formula (2): ##STR1## which comprises: providing a composition system comprising a mixed solvent of a first solvent and a second solvent respectively having high and low dissolving abilities for the desired compound, wherein the mixed solvent has the desired compound dissolved therein; and removing the first solvent having a high dissolving ability from the composition system to thereby deposit crystals of the desired compound. The desired compound, which is useful as a precursor of high performance explosive additive, i.e.

Abstract: The invention relates to a compound of the following general formula [I] or a medicinally acceptable salt thereof, or a solvate thereof, ##STR1## wherein R.sup.1 represents alkyl, alkenyl, alkynyl, alkoxy, hydroxy, cyano, or halogen; R.sup.2 represents hydrogen, hydroxy, or halogen; R.sup.3 represents hydrogen, alkyl, or amidino; Ring A represents a 5 to 11-membered cyclic amino group which may be substituted, which cyclic amino group may be bridged between two carbon atoms in optional positions. The compound of this invention is useful for the prevention or treatment of cerebral tissue impairment due to the vasospasm following cerebral hemorrhage.

Abstract: Hexabenzylhexaazaisowurtzitane is converted to tetracetyl, dibenzyl azaisowurtzitane. The benzyl groups are removed by catalytic transfer hydrogenolysis leaving a pair of available nitrogens. The available nitrogens are acetylated, and the resulting intermediate is converted to CL-20 with a strong nitrating agent.

Abstract: What is claimed is a process for preparing macropolycyclic polyamines of the formula ##STR1## where A.sup.1, A.sup.2, A.sup.3 and A.sup.4 are as defined in the description. These compounds are prepared by a novel improved process by reacting a cyclic amine of the formula ##STR2## with a compound of the formula X--A.sup.2 --Y or X--A.sup.3 --Y where A.sup.1, A.sup.2, A.sup.3 and A.sup.4 are as defined in the description and X and Y are a leaving group.

Abstract: 9,10-DIAZATRICYCLO[4,4,1,1.sup.2,5 ]DECANE (la) AND 2,7-DIAZATRICYCLO[4,4,0,0.sup.3,8 ]DECANE (1b) DERIVATIVES HAVING ANALGESIC ACTIVITY.

Abstract: Processes and compositions for nitration of N-substituted isowurtzitane compounds with concentrated nitric acid at elevated temperatures to form HNIW and recovery of gamma HNIW with high yields and purities. Polymorphic conversion of HNIW crystals to epsilon HNIW crystals is also disclosed.

Abstract: Novel indolocarbazole derivatives potentially useful for the treatment of dementias characterized by tau hyperphosphorylation [Alzheimer's disease (AD), frontal lobe degeneration (FLD), argyrophilic grains disease, subacute sclerotizing panencephalitis (SSPE) as a late complication of viral infections in the CNS], and cancer.

Abstract: A process for preparing a N,N'-difluorodiazoniabicycloalkane salt of the formula: ##STR1## by reacting a corresponding diazabicycloalkane or diazabicycloalkane Br.o slashed.nsted acid salt and fluorine in the presence of a Br.o slashed.nsted acid or in the presene or absence of a base, by reacting a corresponding N,N'-difluorodiazoniabicycloalkane salt and an acid or salt, by reacting a corresponding diazabicycloalkane and fluorine in the presence of a Br.o slashed.nsted acid and then reacting an intermediate product and an acid or salt, or by reacting a corresponding diazabicycloalkane Br.o slashed.nsted acid salt and fluorine in the presence or absence of a base and then reacting an intermediate product and an acid or salt.

Abstract: A process for the preparation of tetraazamacrocycles of general formula (I) ##STR1## wherein n, p and q can independently be 0 or 1, comprising the following steps:a): condensation of polyamines with a glyoxal derivative;b): condensation of the resulting compound with an alkylating agent;c): oxidation of the resulting compound with an oxidizing agent, to give a mixture of oxidated products which is submitted tod): hydrolysis in acid aqueous solution, to give the compound of formula (I).

Abstract: The present invention relates to diazabicyclic compounds and, specifically, to compounds of the formula ##STR1## wherein A, G, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.7 are as defined in the specification. The compounds of formula I are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders.

Abstract: A process of synthesizing HBIW using a mineral acid, such as perchloric acid, as the acid catalyst is disclosed. According to the process, glyoxal, adjusted to a pH from 4 to 7, and benzylamine are reacted in the presence of the mineral acid for sufficient time to form HBIW. The resulting HBIW is then isolated according to conventional separation techniques.

Abstract: A new compound, 2,4,6,8,10,12-hexanitro-2,4,6,8,10,12-hexaazaisowurtzitane (2,4,6,8,10,12-hexanitro-2,4,6,8,10,12-hexaazatetracyclo?5.5.0.0.sup.5,9.0 3,11 !dodecane) is disclosed and a method of preparation thereof. The new compound is useful as a high energy, high density explosive.

Abstract: Certain aralkyl diazabicycloalkyl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychoses and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein each of R, R.sup.1, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from hydrido, lower-alkyl, benzyl, and haloloweralkyl; wherein each of R.sup.2, R.sup.3 and R.sup.10 through R.sup.13 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein each of R.sup.8 and R.sup.

Abstract: A compound of formula (I): ##STR1## in which R.sub.1 represents a hydrogen atom or a straight or branched (C.sub.1 -C.sub.4)alkyl group; andA represents a 5,6-dihydro-4H-imidazo[4,5,1-ij]quinol-2-yl group, a 4,5-dihydroimidazo[1,5,4-de][1,4]benzoxazin-2-yl group, a 4-methyl-4,5-dihydroimidazo[1,5,4-de][1,4]benzoxazin-2-yl group, a 4-phenyl-4,5-dihydroimidazo[1,5,4-de][1,4]benzoxazin-2-yl group, a 4-phenylmethyl-4,5-dihydroimidazo[1,5,4-de][1,4]benzoxazin-2-yl group, a 5-methyl-4,5-dihydroimidazo[1,5,4-de][1,4]benzoxazin-2-yl group, a 5,6-dihydro-4H-imidazo[1,5,4-de]quinoxalin-2-yl group, a 6-oxo-5,6-dihydro-4H-imidazo[4,5,1-ij]quinol-2-yl group, or a 5-methyl-4,5,6,7-tetrahydroimidazo[4,5,1-jk][1,4]benzodiazepin-2-yl group which may be unsubstituted or substituted in the 6-position by a phenylmethyl group;or an addition salt thereof with a pharmaceutically acceptable acid.

Abstract: The invention relates to an addition compound which is obtainable by reaction of a diamine of the formula I, ##STR1## where R.sup.1 is (C.sub.2 -C.sub.4)-alkylene or 1,2- or 1,3-cyclo-(C.sub.3 -C.sub.7)-alkylene andR.sup.2 and R.sup.3, which are identical or different, are (C.sub.1 -C.sub.3)-alkyl or hydrogen orR.sup.2 and R.sup.3 together are (C.sub.2 -C.sub.4)-alkylene, with fullerenes C.sub.60 and/or C.sub.70. The fullerene derivatives are useful as electrically conducting materials.

Abstract: 2-aryl-ethane-sulphonic acids of the formulaAr.sup.1 --CH.sub.2 --CH.sub.2 --SO.sub.3 H (I),in whichAr.sup.1 denotes a carbocyclic or heterocyclic aromatic radical which can be bound to an anellated benzene nucleus,can be obtained by reaction of the underlying vinyl aromatic compound with sulphurous acid, if the reaction is carried out in the presence of an amine of the formulaN(R.sup.1,R.sup.2,R.sup.3 (III),in whichR.sup.1, R.sup.2 and R.sup.3 have the meaning mentioned in the description.

Abstract: The present invention relates to novel N,N'-difluorinated diazabicycloalkane derivatives which are useful as electrophilic fluorinating agents, processes for preparing such N,N'-difluorinated diazabicycloalkane derivatives and methods of using such compounds as fluorinating agents. The invention also presents novel N-fluorinated azaazoniabicycloalkane-Lewis acid adduct intermediates which are formed in the processes for preparing such N,N'-difluorinated diazabicycloalkane derivatives.

Abstract: Process for preparing enantiomerically pure imidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-thiones of formula ##STR1## starting from 2,6-dihalo-3-nitrobenzyl derivatives (II) and suitably N-protected 1,2-diaminopropanes (III) ##STR2## Novel enantiomerically pure intermediates of formula (III) and (IV) prepared in the course of the present process.

Abstract: The invention relates to novel cholecystokinin antagonists of the formula ##STR1## wherein R.sup.1 is aryl or substituted aryl, and a pharmaceutically acceptable salt thereof useful as cholecystokinin antagonists.

Abstract: New indolocarbazoles of formula: ##STR1## or a pharmaceutically acceptable salt thereof, processes for their preparation, compositions containing, and methods for using the composition for the inhibition of protein kinases, such as protein kinase C, for the prevention and/or treatment of heart and blood vessel diseases such as thromboses, arterioscleroses, hypertension, or for inflammatory processes, allergies, cancers, viral diseases, and certain degenerative damages of the central nervous system are disclosed.

Abstract: The invention is a process for preparing 1,4-diazoniabicycloalkanes of Formula I wherein the corresponding 1-hydro-4-aza-1-azoniabi-cycloalkane salt of the 1,4-diazabicycloalkane is fluorinated in the presence of an alkali metal salt under reaction conditions sufficient to form the desired 1,4-diazoniabicycloalkane. ##STR1## wherein n represents 0, 1 or 2;each R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 independently represents hydrogen, C.sub.1 -C.sub.6 alkyl, aryl, C.sub.1 -C.sub.6 alkyl-substituted aryl or aryl-substituted C.sub.1 -C.sub.6 alkyl; andeach X.sup.- represents a counterion or 2X.sup.- represents a single divalent counterion.

Abstract: 1,3-Oxazole and 1,3-thiazole compounds of formula I, and their pharmaceutically acceptable salts and prodrugs: ##STR1## wherein X represents oxygen or sulphur;R.sup.1 represents a non-aromatic azacyclic or azabicyclic ring system.

Abstract: Conformationally constrained tricyclic derivatives of the thienodiazocine and thienothiadiazocine classes of compounds and ring homologs thereof are topically effective carbonic anhydrase inhibitors useful in the treatment of ocular hypertension and glaucoma associated therewith.

Abstract: Novel tetrahydroimidazo[1,4]benzodiazepin-2-(thi)ones possessing anti-HIV-1 activity, compositions containing these compounds as active ingredients, and methods of treating subjects suffering from HIV-1 infection by administering these compounds.

Abstract: A tricyclic compound represented by the general formula (1) and salts thereof. ##STR1## A method for producing the tricyclic compound and salts thereof, and an antimicrobial agent containing the tricyclic compound and salts thereof as an active ingredient are also disclosed.

Abstract: Novel hydrogenated heterocyclic compounds, containing two nitrogen atoms, of the formula ##STR1## in which R.sub.1, R.sub.2, R.sub.3, R.sub.5 and Rhd 7 are each, independently of the others, hydrogen or lower alkyl, m is 2 or 3, n is 1 or 2, and either R.sub.4 and R.sub.6 are each hydrogen or R.sub.4 and R.sub.6 together form an additional bond, in free form or in form of a salt, can be used as pharmaceutical active ingredients and can be manufactured in a manner known per se.

Abstract: Novel benzo[b]pyrrolo[3,2,1-jk]benzodiazepines, intermediates and processes for the preparation thereof, and methods for alleviating pain utilizing the compounds or compositions thereof are disclosed.