Abstract: Asenapine and related trans-isomer bicyclic compounds can be obtained by reducing a compound of formula (C) to preferentially form a trans-isomer compound of formula (D), followed by subsequent ring closure to form a compound of formula (B) such as asenapine.

Abstract: A method for the production of acetals and ketals of 3-amino-5-(hydroxymethyl) cyclopenlane-1,2-diols of formula (I): (and/or the enantiomer), where R1 is H, C1-6-alkyl, C3-8-cycloalkyl or benzyl and (i) R2 is methyl and R3 is ethyl, (ii) R2 is H and R3 is C1-6-alkyl or phenyl or (iii) R2 and R3 together form a group of formula —(CH2)n— with n=4 to 6, present as free amines or as salts of di- or tri-basic organic acids, starting from 2-acetyl-2-aza-bicyclo[2.2.1]hept-5-en-3-one of formula (II): (and/or the enantiomer). The method is equally useful, depending on the starting material, for the production of enantiomerically-pure compounds, or mixtures with arbitrary enantiomeric content.

Abstract: The object of the present invention is to provide a potassium channel opener having benzofuroindole skeleton representing the following formula (I) wherein, R1 is hydrogen, R2 is CF3, R3 is COOH, R4 is hydrogen, R5 is hydrogen or chloride and R6 is hydrogen or chloride.

Abstract: Inventors have developed a chromophore (nitrodibenzylfuranyl, or NBDF) for ultra efficient uncaging of a caged substrate (e.g., an organic molecule such as, for example, an amino acid, a biological molecules, such as, for example, second messengers inside cells). Photolysis of a NBDF derivative of EGTA (i.e. caged calcium) is about 50 times more efficient than others calcium cages (the quantum yield of photolysis is 0.6 and the extinction coefficient is 18,400. NDBF-EGTA has a 2-photon cross section of about 0.3-0.6 GM).

Abstract: The present invention relates to quinobenzoxazines analogs having the general formula: and pharmaceutically acceptable salts, esters and prodrugs thereof; wherein A, U, W, X, Z, B, L, R1, R3, R4 and R5 are substituents. The present invention also relates to methods for using such compounds.

Abstract: The present invention is directed to novel tetracyclic heteroatom containing derivatives, pharmaceutical compositions containing them, their use in the treatment of disorders mediated by one or more sex steroid hormone receptors and processes for their preparation.

Abstract: The present invention relates to 1-aza-dibenzoazulene derivatives, to their pharmacologically acceptable salts and solvates, to processes and intermediates for the preparation thereof as well as to their antiinflammatory effects, especially to the inhibition of tumour necrosis factor-? (TNF-?) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action.

Abstract: The disclosure relates to compounds, pharmaceutical compositions and methods for inhibiting PARP by use of the disclosed compositions.

Abstract: A process for preparing cyclopentadiene derivatives comprising the steps of: a) coupling a five membered heterocycle ring with a five or six membered heterocycle ring; b) reacting the obtained compound with a carbonilating system: c) reducing the obtained compound.

Abstract: The invention provides novel compounds useful as kinase inhibitors or as starting materials And/or intermediates in the synthesis of compounds useful as kinase inhibitors. The compounds have The general structure of formula (I) wherein A is a 3- to 8-membered ring, optionally substituted and/or heteroatom-containing, and R1, R2, R3, R4, R5, R6, X, Y, Z, p, and q are as defined herein. The compounds may also be in the form of a salt, ester, amide, or other analog. In preferred compounds, A is a 5- to 8-membered ring, R1 is hydrogen, q is a bond, X is N, Y is C?O, Z is N, R2 contains a terminal amino moiety, p is 1, and R3 and R4 are linked to form a pyrrole ring fused to a second cyclic group. Pharmaceutical compositions and methods for using the compounds are also provided.

Abstract: A thermally stable booster explosive and process for the manufacture of the explosive. The product explosive is 2,4,7,9-tetranitro-10H-benzo[4,5]furo[3,2-b]indole (TNBFI). A reactant/solvent such as n-methylpyrrolidone (NMP) or dimethyl formamide (DMF) is made slightly basic. The solution is heated to reduce the water content. The solution is cooled and hexanitrostilbene is added. The solution is heated to a predetermined temperature for a specific time period, cooled, and the product is collected by filtration.

Abstract: The present invention relates to novel Pyrrole-Type compounds, compositions comprising Pyrrole-Type compounds, and methods useful for treating or preventing cancer or a neoplastic disorder comprising administering a Pyrrole-Type compound. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a cancer cell or neoplastic cell. The present invention also relates to novel Pyrrole-Type compounds, compositions, and methods useful for treating or preventing a viral infection. The compounds, compositions, and methods of the invention are also useful for inhibiting the replication and/or infectivity of a virus. The present invention also relates to novel Pyrrole-Type compounds, compositions, and methods useful for causing immunosuppression. The present invention also relates to novel Pyrrole-Type compounds, compositions, and methods useful for treating or preventing an autoimmune disease.

Abstract: The present invention provides analogues of duocarmycins that are potent cytotoxins. Also provided are peptidyl and disulfide linkers that are cleaved in vivo. The linkers are of use in forming prodrugs and conjugates of the cytotoxins of the invention as well as other diagnostic and therapeutic moieties. The invention provides prodrugs and conjugates of the duocarmycin analogues with the linker arms of the invention.

Abstract: A thermally stable booster explosive and process for the manufacture of the explosive. The product explosive is 2,4,7,9-tetranitro-10H-benzo[4,5]furo[3,2-b]indole (TNBFI). A reactant/solvent such as n-methylpyrrolidone (NMP) or dimethyl formamide (DMF) is made slightly basic. The solution is heated to reduce the water content. The solution is cooled and hexanitrostilbene is added. The solution is heated to a predetermined temperature for a specific time period, cooled, and the product is collected by filtration.

Abstract: Biologically active xanthone derivatives, as well as compositions prepared from such derivatives, possessing anti-cancer activity, anti-inflammatory activity, anti-obesity activity, and/or hair growth promotion activity, and a method for producing such derivatives and compositions. The derivatives are obtained by utilizing a heating, extracting and condensing system that efficiently recovers the derivatives from a raw material.

Abstract: Compounds of formula useful for treating tumors, particularly mammary carcinoma and colon carcinoma.

Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6, R7, R8, R9, X, b, k, 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 invention provides organic compounds of the general structure (1) 1

Abstract: Compounds, compositions and methods are provided that are useful in the treatment and/or prevention of a condition or disorder mediated by a G-protein coupled receptor. In particular, the compounds of the invention are useful in the treatment and/or prevention of eating disorders, obesity, anxiety disorders and mood disorders.

Abstract: Benzo[b]furan dimers and processes for their preparation are provided. The invention provides a synthetic process for the preparation of benzo[b]furan dimer using mild reaction conditions, which provides a high substituent tolerance and is appropriate for use in solid phase syntheses for producing a library of benzo[b]furan dimers for biological screening.

Abstract: There are described tetrahydrocarbazoles of formula (1) or (2). The compounds are suitable as antimicrobial active ingredients.

Abstract: The present invention relates to novel compounds of the naphthopyran type with a fused heterocycle in the 5,6-position. These compounds have formula (I) or (II) given below: These compounds (I) or (II) have valuable photochromic properties. The invention further relates to their preparation, to their applications as photochromic substances, and to the (co)polymer compositions and matrices containing them.

Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6, R7, R8, R9, X, b, k, 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: Imido and amido substituted acylhydroxamic acids which reduce the levels of TNF&agr; and inhibit phosphodiesterase in a mammal. A typical embodiment is (3-(1,3-dioxoisoindolin-2-yl)-3-(3-ethoxy-4-methoxyphenyl)propanoylamino)propanoate.

Abstract: This invention provides a total synthesis of Merrillactone and Merrilactone analogues having the structure 1

Abstract: This invention relates generally to tetracyclic tetrahydroquinoline compounds, and analogues thereof, and pharmaceutically acceptable salt forms thereof, which are selective inhibitors of serine protease enzymes, especially factor VIIa; pharmaceutical compositions containing the same; and methods of using the same as anticoagulant agents for modulation of the coagulation cascade.

Abstract: Compounds of the general structural formula and use of the compounds and salts and solvates thereof, as therapeutic agents.

Abstract: The present invention is directed to the tartrate salts of 5,8,14-triazatetracyclo[10.3.1.02,11.

Abstract: The present invention is directed to the citrate salt of 5,8,14-triazatetracyclo[10.3.1.02,11.

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 relates to compounds, pharmaceutical compositions, and methods of using compounds of the formula: or a pharmaceutically acceptable salt, hydrate, prodrug, or mixtures thereof, wherein Y is alkylhalo, alkyl-CO—G, COG, a direct bond, C═O, O, NR11, or CR8; G is NR11R16, OR9, SR9, or R10; Z is O, S, or NR11; X is NR16, O, S, CR12R13, C═O, a bond, —CR12═CR13—, —C(R12R13)C(R14R15)—, or; Rhd 1, R2, R3, R4, R5, R6, R7, R8, R10, R12, R13, R14, or R15 are independently: hydrogen, halo, alkylhalo, hydroxy, C1-C9 straight or branched chain alkyl, C2-C9 straight or branched chain alkenyl group, C3-C8 cycloalkyl, C5-C7 cycloalkenyl, aryl, amino, alkylamino, nitro, nitroso, carboxy, or aralkyl; R9 is hydrogen, hydroxy, C1-C9 straight or branched chain alkyl, C2-C9 straight or branched chain alkenyl group, C3-C8 cycloalkyl, C5-C7 cycloalkenyl, aryl, amino, alkylamino, carboxy, or aralkyl; R11 or R16 are independently: hydrogen, halo, alkylha

Abstract: The invention relates to tuned multifunctional linker molecules for charge transport through organic-inorganic composite structures. The problem underlying the present invention is to provide multifunctional linker molecules for tuning the conductivity in nanoparticle-linker assemblies which can be used in the formation of electronic networks and circuits and thin films of nanoparticles.

Abstract: A chemical compound of formula (I), wherein n is 1, 2 or 3; R1 and R2 are independently selected from hydrogen and alkyl; R3 is alkyl; R4 to R7 are independently selected from hydrogen, halogen, hydroxy, alkyl, aryl, alkoxy, aryloxy, alkylthio, arylthio, alkylsulfoxyl, alkylsulfonyl, arylsulfoxyl, arylsulfonyl, amino, monoalkylamino, dialkylamino, nitro, cyano, carboxaldehyde, alkylcarbonyl, arylcarbonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, alkoxycarbonylamino, aminocarbonyloxy, monoalkylaminocarbonyloxy, dialkylaminocarbonyloxy, monoalkylaminocarbonylamino and dialkylaminocarbonylamino, or R5 and R6 together form a carbocyclic or heterocyclic ring, and pharmaceutically acceptable salts and prodrugs thereof, and the use thereof in therapy, particularly for the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders, diabetes insipidus, and sleep apnea, and particularly for the treatment of obesity

Abstract: The dihydroindole C-ring found in CC-1065/duocarmycin analogs is formed by the 5-exo-trig radical cyclization of an aryl halide onto a tethered vinyl chloride forming with chlorine installed as a suitable leaving group for subsequent cyclopropane spirocyclization. The versatility of this approach is disclosed in the context of six CC-1065/duocarmycin analogs previously synthesized in this laboratory.

Abstract: The present invention is directed to novel fused pyrrolocarbazoles and isoindolones, including pharmaceutical compositions, diagnostic kits, assay standards or reagents containing the same, and methods of using the same as therapeutics. The invention is also directed to intermediates and processes for making these novel compounds.

Abstract: Compounds of the Formulae (I) and (II): wherein R1, R2, R3, X, Y and Z are as defined in the specification which compounds are useful in the treatment of disorders associated with smooth muscle contraction via potassium channel modulation.

Abstract: The invention relates to processes for the preparation of 4a,5,9,10,11,12-hexahydro-6H-benzofuro[3a,3,2-ef][2]benzazepine, or derivatives thereof. Furthermore, the invention also relates to the compounds formed during the preparation of 4a, 5,9,10,11,12-hexahydro-6H-benzofuro[3a,3,2-ef][2]benzazepine.

Abstract: Compounds of the Formulae (I) and (II): 1

Abstract: This invention relates to compounds, pharmaceutical compositions, and methods for the treatment or prevention of neural or cardiovascular tissue damage related to cerebral ischemia and reperfusion injury in an animal by administering Poly(ADP-ribose) polymerase (“PARP”) inhibitors.

Abstract: Compounds of the Formulae (I) and (II): wherein R1, R2, R3, X, Y and Z are as defined in the specification which compounds are useful in the treatment of disorders associated with smooth muscle contraction via potassium channel modulation.

Abstract: There are provided compounds of formula (I), wherein R1 is a hydrogen, chlorine or bromine atom or a methyl, methylthio, hydroxy, cyano or carboxamido group; R2 is C1-C3 alkyl or an alkyl group; R3 and R4 are independently a hydrogen atom, a C1-C5 alkyl group, a C3-C5 alkenyl group, a C5-C6 cycloalkyl C1-C3 alkyl group, a phenyl-C3-C5 alkenyl or phenyl group: which groups are optionally substituted by C1-C3 alkyl, C1-C3 alkoxy, triflouromethyl, hydroxy or amino group; or a group of formula (a), wherein R6 is hydrogen atom or a C1-C3 alkyl group and R7 is a phenyl group, a substituted phenyl group as described above or a heterocyclic ring, R5 is a hydrogen or bromine atom or an organic residue and R is H or an organic residue, or a pharmaceutically acceptable salt thereof. A process for their preparation and the pharmaceutical compositions comprising them are also provided.

Abstract: The field of this invention is antitumor antibiotics. More particularly, the present invention relates to analogs of duocarmycin and CC-1065, which analogs have antitumor antibiotics activity.

Abstract: Disclosed are naphthopyran-type compounds having a pyrrole group annelated in position 5.6, as well as compositions and particularly (co)polymer matrices containing them. These compounds, compositions, and matrices have photochromic properties. These [pyrrole]naphthopyran compounds have the general formula: Articles containing these photochromic compounds, such as ophthalmic and/or solar glasses, lenses, glazing, devices, and the like, are also disclosed.

Abstract: A compound of formula (I) ##STR1## in which: m, and n, which may be identical or different, represent 0 or 1,X and Y, which may be identical or different, represent hydrogen or halogen or alky, trihaloalkyl, alkoxy, hydroxyl, cyano, nitro, amino, alkylamino or dialkylamino,Z represent a linear or branched C.sub.4 to C.sub.12 alkylene chain in which one or more --CH.sub.2 -- are optionally replaced by any one of the following atoms or groups: --NR--, --O--, --S--, --SO--, --SO.sub.2 --, or --CONH--, or by a substituted or unsubstituted heterocylcic,A forms, with two adjacent carbon atoms of the phenyl ring, a phenyl, naphthyl or tetrahydronaphthyl ring or a heterocycle, ##STR2## and medicinal products containing the same are useful as anticancer agent.

Abstract: Methods for treating infection and related compositions, compounds of formula I as defined in the application and methods for preparing same, are provided. In general, the compounds inhibit transfer ribonucleic acid (tRNA) synthetase and are useful as antimicrobial agents.

Abstract: The present invention provides compounds of formula I and II: ##STR1## wherein X is --O--, --S--, or --NR.sup.5 --;Y is --O--, --S--, --CH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, or --NR.sup.5 --;B is --CH.sup.2 -- or --CO--;R.sup.1, R.sup.2, and R.sup.3 are each independently --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), --OSO.sub.2 (C.sub.4 -C.sub.6 alkyl), --OSO.sub.2 CF.sub.3, Cl, or F;n is 1 or 2;W is CH.sub.2 or C.dbd.O;R.sup.4 is 1-piperidinyl, 2-oxo-1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 2-oxo-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino;R.sup.5 is C.sub.1 -C.sub.3 alkyl, --COC.sub.6 H.sub.5, --CO(C.sub.1 -C.sub.6 alkyl), --C(O)OC.sub.6 H.sub.5, --C(O)O(C.sub.1 -C.sub.6 alkyl), --SO.sub.2 (C.sub.1 -C.sub.6 alkyl), --SO.sub.2 C.sub.6 H.sub.5, or --SO.sub.2 CF.sub.3 ;or a pharmaceutically acceptable salt or solvate thereof.

Abstract: Analogs of antitumor antibiotics CC-1065 and the duocarmycins are synthesized which possess systematic and extensive modifications in the DNA binding subunits attached to a 1,2,9,9a-tetra-hydro-cyclo-propa[c]benz[e]indol-4-one (CBI) alkylation subunit. The analogs have potent cytotoxic activity and are efficacious antitumor compounds.

Abstract: A compound of the formula: whereinQ is an optionally substituted carbon atom or N(O)p wherein p is 0 or 1;Y is an optionally substituted methylene group, S(O)q wherein q is an integer of 0 to 2, or an optionally substituted imino group;Z.sup.1 is a C.sub.1-3 alkylene group which may have an oxo group or a thioxo group and may contain etherified oxygen or sulfur within the carbon chain;Z.sup.2 is an optionally substituted C.sub.1-3 alkylene group;Ar is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group;one of R.sup.1 and R.sup.2 is a hydrogen atom, a halogen atom, a hydroxyl group, an optionally substituted lower alkyl group, or an optionally substituted lower alkoxy group;the other is a halogen atom, a hydroxyl group, an optionally substituted lower alkyl group, or an optionally substituted lower alkoxy group; orR.sup.1 and R.sup.2 taken together with adjacent --c.dbd.c-- form a ring; andring A is a benzene ring which may be substituted in addition to R.sup.1 and R.

Abstract: The present invention relates to heterocyclic compounds which have been found to have anti-tumour activity. More specifically, the invention concerns pyrrolo[2,3-b]carbazoles and 1H-[1] benzothieno [2,3-f] indoles, methods for their preparation, pharmaceutical formulations containing them and their use as anti-tumour agents. The compounds have low toxicity against normal cell lines whilst exhibiting anti-tumour cell activity.

Abstract: The present invention relates to heterocyclic compounds which have been found to have anti-tumor activity. More specifically, the invention concerns pyrrolo?3,2-b!carbazoles and 1H-?1! benzothieno ?2,3-f! indoles, methods for their preparation, pharmaceutical formulations containing them and their use as anti-tumor agents. The compounds have low toxicity against normal cell lines while exhibiting anti-tumor cell activity.