Abstract: Compounds according to the formula: 1

Abstract: Pyrazolo[4,3-c]pyridin-3-one derivatives substituted at the 2-position by an optionally substituted aryl or heteroaryl moiety, and having pendant substituents at the 7-position and optionally also at the 6-position, are selective ligands for GABAA receptors, particularly having high affinity for the &agr;2 and/or &agr;3 subunit, and are useful in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.

Abstract: A compound of formula 1a which is useful for treating reperfusion injury, and salts, prodrugs, and related compounds.

Abstract: Carboline derivatives of formula (I), are potent and selective inhibitors of cyclic guanosine 3′,5′-monophoshate specific phosphodiesterase (cGMP specific PDE) and have utility in a variety of therapeutic areas where such inhibition is thought to be beneficial, including the treatment of cardivascular disorders.

Abstract: The present invention relates to a naphthalimidobenzamide derivative represented by the following formula (1): (wherein, R1 represents a hydrogen atom, etc., Y represents a hydrogen atom or —CON(R4)—A2—X2, R2 and R4 are the same or different and each independently represents a hydrogen atom, etc., A1 and A2 are the same or different and each independently represents an alkylene group which may be interrupted at least once by —N(R3)— (R3 representing a hydrogen atom, etc.) and X1 and X2 are the same or different and each independently represents a (hetero)aryl group which may have a substituent, etc.) or salt thereof; and a pharmaceutical comprising it as an effective ingredient. The compound is useful as an antitumor agent and the like.

Abstract: Disclosed are compounds of the formula: wherein Ar, R1, W, X and m are substituents as defined herein.

Abstract: Combinatorial chemical libraries of the Formula [S]—C(O)—L′—Z containing dihyroxy amides and hydroxyphosphonate amides are disclosed, in which [S] represents a solid support and —L′—Z is a linker/ligand residue. In these libraries, Z is and Y is —P(O)(OR6)(OR7), —CH(OH)—COR8, —CH,CH═CH2—CH2CH(OH)CH2OH, —CH2CHO, —CH2CH2OH, —CH2CH2OC(O)NHR26, —CH2CH2NR27R28, or The combinatorial libraries are optionally encoded with tags. The use of these libraries in assays to discover biologically active compounds is also disclosed.

Abstract: This invention provides a series of substituted indoles which are useful in treating or preventing a condition associated with an excess of neuropeptide Y. This invention also provides the novel substituted indoles as well as pharmaceutical formulations with comprise as an active ingredient one or more of these substituted indoles.

Abstract: Cycloakano-indole and -azaindole derivatives are prepared by reaction of appropriately substituted carbonylic acids with amines. The cycloalkano-indole and -azaindole derivatives are suitable as active compounds for medicaments, preferably antiatherosclerotic medicaments.

Abstract: Compounds of general formula (1) are described: wherein ═W— is (1) ═C(Y)— where Y is a halogen atom, or an alkyl or —XRa group where X is —O—, —S(O)m— [where m is zero or an integer of value 1 or 2], or —N(Rb)— [where Rb is a hydrogen atom or an optionally substituted alkyl group] and Ra is a hydrogen atom or an optionally substituted alkyl group or, (2) ═N—; L is (1) a —C(R)═C(R1)(R2) or [—CH(R)]nCH(R1)(R2) group; is (2) a —(Xa)nAlk′Ar′, or Alk′XaAr′ group; or is (3) XaR1; Z is a group (A), (B), (C) or (D):  wherein Ar is a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms; Z1is a group —NR12C(O)— [where R12 is a hydrogen atom or an optionally substituted alkyl or (Alk)tAr group], —C(O)NR12—, —NR12

Abstract: Disclosed are compounds of the formula: wherein Ar, R1, W and X are substituents as defined herein, which compounds are effective neuropeptide Y1 receptor antagonists, and are therefore useful in the treatment of a wide variety of clinical conditions which are characterized by the presence of an excess of neuropeptide Y.

Abstract: A compound of formula and salts and solvates thereof, wherein R0, R1, and R2 are defined in the specification. A compound of the present invention is a potent and selective inhibitor of cGMP-specific PDE and has utility in a variety of therapeutic areas where such inhibition is beneficial.

Abstract: Disclosed are compounds of the formula: wherein Ar, R1, R2, R3, W, X, Y, and Z are substituents as defined herein, which compounds are highly selective partial agonists or antagonists at human CRF1 receptors and are useful in the diagnosis and treatment of treating stress related disorders such as post traumatic stress disorder (PTSD) as well as depression, headache and anxiety.

Abstract: The new arylacetamides are obtained by first converting appropriately substituted arylacetic acids into the acetyl chlorides and then converting these into the amides using the appropriate amines. The new arylacetamides can be used as active compounds in medicaments, in particular in antiatherosclerotic medicaments.

Abstract: The invention provides a process for the preparation of a compound of general formula (I): wherein Im represents an imidazolyl group of the formula: and R1 represents a hydrogen atom or a group as herein defined including —CO2R5, —COR5, —CONR5R6 or —SO2R5 wherein R5 and R6, which may be the same or different, are as herein defined with the proviso that R5 does not represent a hydrogen atom when R1 represents a group —CO2R5 or —SO2R5; one of the groups represented by R2, R3 and R4 is a hydrogen atom or a C1-6alkyl, C3-7cycloaklyl, C3-6alkenyl, phenyl or phenyl C1-3alkyl group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C1-6alkyl group; and n represents 2 or 3; which comprises reacting a compound of formula (II) or a protected derivative thereof, with a compound of formula (III): HOCH2-Im  (III) or a salt thereof in the presence of an acid at an elevat

Abstract: The subject invention involves compounds having the structure: wherein the C.sub..alpha. --N.sub..beta. and C.sub.5 -C.sub.6 bonds are independently single or double bonds, R1 is selected from alkyl, aryl, and heterocycle; R2-R13 are independently selected from hydrogen and other substituents; and pharmaceutically-acceptable salts thereof. The subject invention also involves pharmaceutical compositions containing such compounds, and methods for treating or preventing diseases and disorders using such compounds.

Abstract: Disclosed are compounds of the formula: ##STR1## wherein Ar, R.sup.1, W and X are substituents as defined herein, which compounds are (1) antagonists at CRF.sub.1 receptors and are, therefore, useful in the diagnosis and treatment of stress related disorders such as post traumatic stress disorder (PTSD) as well as depression, headache and anxiety; and (2) are neuropeptide Y.sub.1 receptor antagonists, and are therefore useful in the treatment of a variety of clinical conditions which are characterized by the presence of an excess of neuropeptide Y.

Abstract: Disclosed are compounds of the formula: ##STR1## wherein Ar is optionally substituted aryl or heteroarylR.sub.1 is hydrogen or alkyl;R.sub.7 is hydrogen or alkyl;R.sub.2 is hydrogen, halogen, alkyl or alkoxy; orR.sub.1 and R.sub.2 taken together with the ring to which they are attached form a 5-9 membered saturated or aromatic ring optionally having a hetero atom selected from oxygen, sulfur or nitrogen;R.sub.3 and R.sub.4 are independently hydrogen, alkyl, cycloalkyl, aryl or heteroaryl groups; orR.sub.3 and R.sub.4 together with the nitrogen atom to which they are attached form a 5-8 membered ring; andR.sub.

Abstract: Carboline derivatives of formula (I), are potent and selective inhibitors of cyclic guanosine 3',5'-monophosphate specific phosphodiesterase (cGMP specific PDE) and have utility in a variety of therapeutic areas where such inhibition is thought to be beneficial, including the treatment of cardiovascular disorders.

Abstract: Compounds of the formula: ##STR1## which are useful as anti-ulcer agent are provided.

Abstract: This invention relates to 4-substituted .beta.-carbolines and .beta.-carboline analogs that inhibit Ca.sup.+2 influx and interleukin-2 (IL-2) production. The 4-substituted .beta.-carbolines and .beta.-carboline analogs of this invention are represented by formula (I): ##STR1## wherein Q, n, R, R', R" and R.sub.1 -R.sub.4 are as defined herein. This invention also relates to methods for producing .beta.-carbolines. Because of their selective immunomodulating properties, the compounds and pharmaceutical compositions of this invention are particularly well suited for preventing and treating immune disorders, including autoimmune disease, inflammatory disease, organ transplant rejection and other disorders associated with IL-2 mediated immune response.

Abstract: The present invention concerns the use of beta-carboline derivatives of formula I bearing at least a free or esterified carboxylic group on the piperidine ring, for the preparation of pharmaceutical compositions having antimetastatic properties.

Abstract: Compound of formula (I): ##STR1## in which: m represents an integer from 1 to 4 inclusive, and n and p an integer from 0 to 4 inclusive,X represents O, S or a single bond,R.sub.1 represent hydrogen or halogen, or alkyl, alkoxy, hydroxy, trihaloalkyl or trihaloalkoxy,R.sub.2, R.sub.3 and R.sub.4, which may be same or different, each represents hydrogen or alkyl,R.sub.5 represents hydrogen or halogen, or alkoxy, aryloxy or heteroaryloxy,R.sub.6, R.sub.7 and R.sub.8, which may be same or different, each represents hydrogen or alkyl, or together form, with the atoms carrying them respectively, an optionally substituted heterocycle,R.sub.9 represents SO.sub.3 H, --CO.sub.2 R.sub.10, --CO--NR.sub.11 R.sub.12, or --NR.sub.13 R.sub.14, wherein R.sub.10, R.sub.11, R.sub.12, R.sub.13 and R.sub.14 each represents hydrogen or alkyl or together (R.sub.11 /R.sub.12 ; R.sub.13 /R.sub.

Abstract: The invention provides novel lavendamycin analogs having the following general formula: ##STR1## and quinoline-5,8-diones having the following formula: ##STR2## Methods of making and using and compositions containing these compounds are also disclosed.

Abstract: A compound of formula (I) ##STR1## and salts and solvates thereof, in which: R.sup.0 represents hydrogen, halogen or C.sub.1-6 alkyl;R.sup.1 represents hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, haloC.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkylC.sub.1-3 alkyl, arylC.sub.1-3 alkyl or heteroarylC.sub.1-3 alkyl;R.sup.2 represents an optionally substituted monocyclic aromatic ring selected from benzene, thiophene, furan and pyridine or an optionally substituted bicyclic ring ##STR2## attached to the rest of the molecule via one of the benzene ring carbon atoms and wherein the fused ring A is a 5- or 6-membered ring which may be saturated or partially or fully unsaturated and comprises carbon atoms and optionally one or two heteroatoms selected from oxygen, sulphur and nitrogen; andR.sup.3 represents hydrogen or C.sub.1-3 alkyl, or R.sup.1 and R.sup.3 together represent a 3- or 4-membered alkyl or alkenyl chain.

Abstract: A compound of formula ##STR1## and salts and solvates thereof, wherein R.sup.0, R.sup.1, and R.sup.2 are defined in the specification. A compound of the present invention is a potent and selective inhibitor of cGMP-specific PDE and has utility in a variety of therapeutic areas where such inhibition is beneficial.

Abstract: Tricyclic compounds are described as well as methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A (72 kD gelatinase) and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, cancer metastasis, tumor angiogenesis, arthritis, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes.

Abstract: Disclosed are compounds of the formula: ##STR1## wherein Ar is optionally substituted aryl or heteroarylR.sub.1 is hydrogen or alkyl;R.sub.7 is hydrogen or alkyl;R.sub.2 is hydrogen, halogen, alkyl or alkoxy; orR.sub.1 and R.sub.2 taken together with the ring to which they are attached form a 6 membered aromatic ring optionally having a nitrogen atom,R.sub.3 and R.sub.4 are independently hydrogen, alkyl, cycloalkyl, aryl or heteroaryl groups; or R.sub.3 and R.sub.4 together with the nitrogen atom to which they are attached form a 5-8 membered ring; andR.sub.

Abstract: The invention relates to a process and intermediates for the preparation of enantiomerically pure cycloalkanoindolecarboxylic acids and azaindolecarboxylic acids and pyrimido?1,2a!indolecarboxylic acids and their activated derivatives, characterized in that the tolyl acetic acid is first esterified with a chiral alcohol, then diastereoselective substitution at .alpha.-carbon atoms is carried out and this product is halogenated in the tolyl group and then reacted with appropriate cycloalkanoindoles, cycloalkanoazaindoles or pyrimido?1,2a!indoles. It is possible by this method to prepare specifically, in high purity, the enantiomerically pure carboxylic acids which are intermediates for valuable medicaments.

Abstract: N-heterocyclic moiety containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Abstract: The present invention relates to a method of treating a disease in the central nervous system via the metabotropic glutamate receptor system, the use of the known as well as novel pyridino(2,3-b) indoles (formula Ib) for the preparation of a medicament for treating said diseases, novel therapeutic active pyridino(2,3-b) indoles, a method for preparing the same and pharmaceutical compositions comprising these compounds.

Abstract: Compound of formula (I): ##STR1## in which: m, n, which are identical or different, represent 0, 1 or 2,R.sub.1, R.sub.2, which are identical or different, represent hydrogen, optionally substituted alkyl, aryl, or form with the carbon atom carrying them carbonyl or (C.sub.3 -C.sub.7)cycloalkyl,R.sub.3 represents hydrogen, alkyl, hydroxyl or aryl,R.sub.4 represents any of the groups as defined in the description,X represents --SO.sub.2 --, --CO-- or --SO.sub.2 NH--,R.sub.5 represents optionally substituted alkyl, (C.sub.3 -C.sub.7)cycloalkyl, aryl or heterocyclic,A represents an aryl ring or a heterocycle,its isomers as well as its addition salts with a pharmaceutically acceptable acid or base and medicinal products containing the same are useful as metalloprotease inhibitors.

Abstract: The present invention provides novel tetrahydro-beta-carboline compounds having useful central nervous system activity. Further, there is provided tetrahydro-beta-carboline related compounds which are useful intermediates and have beneficial central nervous system activity. The invention provides formulations and methods for using the novel tetrahydro-beta-carboline and related compounds. Such compounds are particularly useful for the modulation of a 5-HT.sub.2B receptor.

Abstract: Specified imidazoquinoline derivatives represented by the formula (I): ##STR1## where Q represents an optionally substituted phenyl, pyridyl or furyl group; Y represents either a hydrogen atom or, when taken together with Z, an oxygen atom and a methylene group; Z represents a hydrogen atom, a hydroxymethyl group, a carboxymethyl group, a 2-oxo-1-pyrrolidinyl group or the following formula (III):--A--R.sup.2 (III)(where A represents an oxygen atom, a sulfur atom or the group --NH--);or salts of such derivatives inhibit the increase of eosinophils and are useful as agents for preventing and/or treating diseases that manifest the increase of eosinophils.

Abstract: Amides and sulphonamides of benzylamines having heterocyclic substituents are prepared by first converting the corresponding carboxylic acids into the corresponding amines and then substituting these on the amine nitrogen in a corresponding manner. The new amides and sulphonamides of benzylamines having heterocyclic substituents can be used as active compounds in medicaments, in particular in antiatherosclerotic medicaments.

Abstract: A compound of formula (I). The present invention relates to therapeutically active .beta.-carboline derivatives, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating a central nervous system ailment related to the inhibition of GABA uptake via the GAT-4 subtype carrier.

Abstract: Heterotricyclically substituted phenyl-cyclohexanecarboxylic acid derivatives are prepared by reacting the heterocyclic compounds with cyclohexanecarboxylic acid derivatives which are substituted by benzyl halide radicals. The compounds can be employed as active compounds in medicaments.

Abstract: The present invention pertains to a method of preparing substituted and unsubstituted N-hydroxy-2-aminobutane diacid derivatives which can be dehydrated to 2-aminobut-2-ene dioic acid derivatives, which can be subsequently converted to pyridine and quinoline derivatives.

Abstract: The present invention relates to therapeutically active non competitive antagonists, acting selectively at the metabotropic glutamate receptor. The novel compounds are useful in treating diseases in the central nervous system by modulating synaptic transmission via the metabotropic glutamate receptor.

Abstract: Fibrinogen receptor antagonists of the general formula:X-A-Y-Z-B Iand which includes, for example, the compounds of formula ##STR1## are useful for inhibiting the binding of fibrinogen to blood platelets, inhibiting the aggregation of blood platelets, treating thrombus formation or embolus formation, and preventing thrombus or embolus formation.

Abstract: Tetrahydro-beta-carboline compounds having useful central nervous system activity are enclosed.

Abstract: The present invention provides methods for binding a 5-HT.sub.2B receptor in mammals using a both known and novel compounds. Further, the invention provides a method for treating or preventing 5-HT.sub.2B related conditions. Finally, the invention provides an article of manufacture.

Abstract: Cycloalkano-indole and -azaindole derivatives are prepared by reaction of appropriately substituted carboxylic acids with amines. The cycloalkano-indole and -azaindole derivatives are suitable as active compounds for medicaments, preferably antiatherosclerotic medicaments.

Abstract: Compounds of the formula: ##STR1## in which R.sub.1 represents a hydrogen or halogen atom or a methyl or C.sub.1 -C.sub.4 alkoxy group, R'.sub.1 represents a hydrogen or halogen atom, R".sub.1 represents a hydrogen atom or a methoxy group, R.sub.3 represents a C.sub.1 -C.sub.3 alkyl group, R.sub.4 represents a 2,3-dihydro-1H-inden-2-yl, 2,3-dihydro-1H-inden-1-yl or 1,2,3,4-tetrahydronaphthalen-1-yl group, or R.sub.3 and R.sub.4 together form, with the adjacent nitrogen atom, a 1,2,3,4-tetrahydroisoquinol-2-yl, 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinol-2-yl, 5,8-dimethoxy-1,2,3,4-tetrahydroisoquinol-2-yl, 1,2,3,4-tetrahydro-9H-pyrido[3,4-b]indol-2-yl, 1,2,3,4-tetrahydro-9H-pyrido[4,3-b]indol-3-yl, 4,5,6,7-tetrahydrothieno[2,3-c]pyrid-6-yl, 2,3-dihydro-1H-isoindol-2-yl or 2,3,4,5-tetra-hydro-1H-3-benzazepin-3-yl, group are useful in the treatment of cerebral disorders.

Abstract: The invention provides lavendamycin analogs having the following formula: ##STR1## wherein X, Y and R.sup.1 through R.sup.9 are defined in the specification, and salts of these analogs. The invention also provides a method of making the lavendamycin analogs. The lavendamycin analogs have antitumor and antimicrobial activity. Also, methods of treating cancer using lavendamycin methyl ester, 7-butyramido-2-methylquinoline-5,8-dione or 7-butyramido-2-formylquinoline-5,8-dione.

Abstract: The present invention provides novel tetrahydro-beta-carboline compounds having useful central nervous system activity. Further, there is provided tetrahydro-beta-carboline related compounds which are useful intermediates and have beneficial central nervous system activity. The invention provides formulations and methods for using the novel tetrahydro-beta-carboline and related compounds. Such compounds are particularly useful for the modulation of a 5-HT.sub.2B receptor.

Abstract: The present invention is directed to compounds of the following formula I: ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, A, n, X, and Y are as defined hereinafter. The compounds of formula I are useful in treating central nervous system disorders. The compounds are ligands for the BZD binding site on GABA-A receptors, and are thus useful as muscle relaxants, hypnotics/sedatives including sleep-aids, anxiolytics, anticonvulsants/antiepileptics, anti-inebriants, and antidotes for drug overdose (particularly benzodiazepine overdose).

Abstract: The present invention provides novel tetrahydro-beta-carboline compounds and intermediates having useful central nervous system activity. The invention provides formulations and methods for using the tetrahydro-beta-carboline and related intermediate compounds. Finally, the invention provides an article of manufacture.

Abstract: Trifluoromethylpyrroloindolecarboxylic acid ester derivatives, and optical isomers and pharmaceutically acceptable salts thereof are provided which are represented by the general formula (1): ##STR1## or the general formula (2): ##STR2## The compounds are antineoplastic agents which are selective to cancer cells, effective also to solid cancer, and less toxic.

Abstract: The present invention provides novel tetrahydro-beta-carboline compounds having useful central nervous system activity. Further, there is provided tetrahydro-beta-carboline related compounds which are useful intermediates and have beneficial central nervous system activity. The invention provides formulations and methods for using the novel tetrahydro-beta-carboline and related compounds. Such compounds are particularly useful for the modulation of a 5-HT.sub.2B receptor.