Abstract: The present invention relates an improved process for the preparation of tetrahydro-?-carboline derivative of formula (V) which is useful as an intermediate for the preparation of Tadalafil of formula (I).

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

Abstract: Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof, wherein W, Q, X, X1, Y and Z are as defined herein. These compounds bind with high selectivity and/or high affinity to the benzodiazepine site of GABAA receptors and are therefore useful in the treatment of central nervous system (CNS) diseases and as probes for the localization of GABAA receptors in tissue samples. Also disclosed are intermediates useful in the preparation of these compounds.

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

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

Abstract: Substituted 2-pyridine cyclohexane-1,4-diamine compounds, a method for their production, pharmaceutical compositions containing them, and the use of such substituted 2-pyridine cyclohexane-1,4-diamine compounds for treating pain and various other medical conditions.

Abstract: Compounds of the formula (I) are disclosed and are useful in the treatment bacterial infections: wherein: R1 is Ar or Het; R2 is C1-6alkyl, (R?)2N—(CH2)m— or Ar—C0-6alkyl; X is H, C1-4alkyl, OR?, SR?, C1-4alkylsulfonyl, C1-4alkylsulfoxyl, CN, N(R?)2, CH2N(R?)2, NO2, CF3, CO2R?, CON(R?)2, COR?, NR?C(O)R?, F, Cl, Br, I, or CF3S(O)r—; R? is H, C1-6alkyl or Ar—C0-6alkyl; each R? independently is H, C1-6alkyl or Ar—C0-6alkyl; m is 1 or 2; n is 0, 1 or 2; and r is 0, 1 or 2; or a pharmaceutically acceptable salt thereof.

Abstract: Tetrahydrocarbazoles of formula where Q is —SO2—; —O—; or —(CO)—; X is —(CH)—; or —N—; m is from 1 to 3; t is 0 or 1 and the remaining substituents are as defined herein, are useful as antimicrobial active ingredients.

Abstract: Compounds of the formula (I) are disclosed which are Fab I inhibitors and are useful in the treatment bacterial infections: wherein: R1 is Ar or Het; R2 is H, C1-6alkyl or Ar-C0-6alkyl; X is H, C1-4alkyl, OR?, SR?, C1-4alkylsulfonyl, C1-4alkylsulfoxyl, CN, N(R?)2, CH2N(R?) 2, NO2, CF3, CO2R?, CON(R?)2, COR?, NR?C(O)R?, F, Cl, Br, I, or CF3S(O)r—; R? is H, C1-6alkyl or Ar-C0-6alkyl; and r is 0, 1 or 2; or a pharmaceutically acceptable salt thereof.

Abstract: This invention provides compounds which are useful as inhibitors of protein tyrosine phosphatases (PTPases). As inhibitors of PTPases, the compounds of the invention are useful for the management, treatment, control and adjunct treatment of diseases mediated by PTPase activity. Such diseases include type I diabetes, type II diabetes, immune dysfunction, AIDS, autoimmunity, glucose intolerance, obesity, cancer, psoriasis, allergic diseases, infectious diseases, inflammatory diseases, diseases involving the modulated synthesis of growth hormone or the modulated synthesis of growth factors or cytokines which affect the production of growth hormone, or Alzheimer's disease.

Abstract: The invention provides compounds of general formula (I) wherein Q, R, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.

Abstract: The present invention provides for compounds, compositions, methods and systems for inhibiting cell growth. More specifically, the present invention provides for methods, compounds and compositions which are capable of inhibiting mitosis in metabolically active cells. Compounds, compositions and methods of the present invention inhibit the activity of a protein involved in the assembly and maintenance of the mitotic spindle. One class of proteins which acts on the mitotic spindle is the family of mitotic kinesins, a subset of the kinesin superfamily.

Abstract: The invention provides compounds of formula (I) wherein R1 to R5 are as defined in the description, and their preparation. The compounds of formula (I) are useful as pharmaceuticals.

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: The present invention provides 2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3-b]indoles and 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles. These compounds are 5-HT ligands that are useful for treating diseases wherein modulation of 5-HT activity is desired.

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

Abstract: The invention provides novel lavendamycin analogs having the following general formula: 1

Abstract: A method for the manufacture of a substance having an apoptosis-inducing ability characterized in including a step of subjecting at least one compound selected from the following (a), (b), (c) and (d) [excluding uronic acid and/or uronic acid derivatives; and compounds which contain uronic acid and/or uronic acid derivatives] to a heating treatment: (a) pentose; (b) pentose derivatives; (c) compounds containing pentose; (d) compounds containing pentose derivatives.

Abstract: The present invention is directed to novel compounds represented by structural Formula (I): 1

Abstract: Compounds of general structural formula (I) and use of the compounds and salts and solvates thereof, as therapeutic agents as inhibitors of phosphodiesterase 5 cardiovascular disorders.

Abstract: The invention provides compounds of formula (I) wherein R1 to R5 are as defined in the description, and their preparation. The compounds of formula (I) are useful as pharmaceuticals.

Abstract: Compounds of the general structural formula 1

Abstract: Compounds of the general structural formula 1

Abstract: The invention relates to hydroxamic and carboxylic acid derivatives. Compounds of the formula: are disclosed. These compounds are useful for the treatment of diseases mediated by inhibitors of matrix metalloproteinase, ADAM, ADAM-TS enzymes, and/or TNF&agr;-mediated diseases including degenerative diseases and certain cancers.

Abstract: A composition includes a substituted dihydro- or tetrahydro-&bgr;-carboline of formula (II) or (III), wherein the aromatic ring of the carboline may include one or more substituents selected from the group consisting of hydroxy, C1-6 alkoxy, benzyloxy, C1-6 acyloxy, amino, C1-6 alkyl, C1-6 dialkylamino, halogen, and carboxy, and the C-1 position of the carboline may include a substitutent selected from the group consisting of a carbocyclic group and a heterocyclic group. The composition may include a salt or a prodrug of the substituted dihydro- or tetrahydro-&bgr;-carboline. The composition may further includes a pharmaceutically acceptable carrier, diluent, or excipient.

Abstract: The present invention relates to novel indole derivatives, to their preparation and to their use, as inhibitors of the enzyme poly(ADP-ribose)polymerase or PARP (EC 2.4.2.30), for producing drugs.

Abstract: Compounds of the formula (I) are disclosed and are useful in the treatment bacterial infections: 1

Abstract: The present invention is directed to compounds of formula (I) wherein the variables are defined in the specification, which bind to somatostatin receptors and block Na channels.

Abstract: Compounds, compositions and methods for modulating the activity of receptors are provided. In particular compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder directly or indirectly related to the activity of the receptors.

Abstract: The present invention is in the field of medicine, particularly in the treatment of Type II diabetes and obesity. More specifically, the present invention relates to selective &bgr;3 receptor agonists useful in the treatment of Type II diabetes and obesity.

Abstract: This invention provides compounds which are useful as inhibitors of protein tyrosine phosphatases (PTPases). As inhibitors of PTPases, the compounds of the invention are useful for the management, treatment, control and adjunct treatment of diseases mediated by PTPase activity. Such diseases include type I diabetes, type II diabetes, immune dysfunction, AIDS, autoimmunity, glucose intolerance, obesity, cancer, psoriasis, allergic diseases, infectious diseases, inflammatory diseases, diseases involving the modulated synthesis of growth hormone or the modulated synthesis of growth factors or cytokines which affect the production of growth hormone, or Alzheimer's disease.

Abstract: The present invention provides novel compounds of Formula (I), its prodrug forms, or pharmaceutically acceptable salts thereof. The compounds of this invention are inhibitors of serine proteases, Urokinase (uPA), Factor Xa (FXa), and/or Factor VIIa (FVIIa), and have utility as anti cancer agents and/or as anticoagulants for the treatment or prevention of thromboembolic disorders in mammals. The present invention also provides a process for the selective acylation of an amino group.

Abstract: Compounds of formula (I) are disclosed which are Fab I inhibitors and are useful in the treatment bacterial infections, wherein: R1 is Ar or Het; R2 is H, C1-6alkyl or Ar—C0-6alkyl; X is H, C1-4alkyl, OR′, SR′, C1-4alkylsulfonyl, C1-4alkylsulfonyl, CN, N(R′)2, CH2N(R′)2, NO2, CF3, CO2R′, CON(R′)2, COR′, NR′C(O)R′, F, Cl, Br, I, or CF3S(O)r; R′ is H, C1-6alkyl or Ar—C0-6alkyl; and r is 0, 1 or 2; or a pharmaceutically acceptable salt thereof.

Abstract: The present invention provides novel compounds of the Formula (I) its prodrug forms, or pharmaceutically acceptable salts thereof. Preferred (I) compounds of the present invention comprise a pyrrolo pyridinyl, pyrrolo pyrimidinyl or indole nucleus. The compounds of this invention are inhibitors of Factor Xa (FXa), Factor VIIa (FVIIa) and/or serine proteases, Urokinase (uPA), and have utility as anti-coagulants for the treatment or prevention of thromboembolic disorders in mammals and as anticancer agents.

Abstract: The invention provides an asymmetric cyanine dye compound having the structure 1

Abstract: The present invention relates to compounds of the general formula (I) 1

Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I):

Abstract: The invention provides compounds of general formula (I) wherein Q, R, R2, R4, R5, R6, R7 and R8 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.

Abstract: The present invention is directed to compounds of the formula wherein the variables are defined in the specification, which bind to somatostatin receptors and block Na channels.

Abstract: Compositions for the oxidation dyeing of keratin fibers, containing at least one oxidation base and at least one coupler chosen from indolizine derivative comprising at least one cationic group Z, Z being chosen from quaternized aliphatic chains, aliphatic chains comprising at least one quaternized saturated ring, and aliphatic chains comprising at least one quaternized unsaturated ring. Methods of using these cationic indolizine derivatives as couplers for the oxidation dyeing of keratin fibers, in combination with at least one oxidation base, and to dyeing processes using them. Some of these cationic indolizine derivatives are novel.

Abstract: The present invention concerns compounds of formula (I) the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Alk is C5-12alkanediyl; n is 1 or 2; p is 1 and q is 2; or p is 2 and q is 1; X is —O—, —S—, —S(═O)—, —S(═O)2— or NR2; each R1 is independently hydrogen, halogen, C1-6alkyl, nitro, hydroxy or C1-4alkyloxy; R2 is hydrogen, C1-6alkyl, aryl or C1-6alkyl substituted with aryl; aryl is phenyl or phenyl substituted with a halogen or C1-6alkyl; D is an optionally substituted benzophenone or 3-benzisoxazolyl; having central &agr;2-adrenoceptor antagonist activity. It further relates to their preparation, pharmaceutical use and compositions.

Abstract: Compounds of the formula (I) are disclosed which are FabI inhibitors and are useful in the treatment bacterial infections: wherein: R1 is Ar or Het; R2 is H, C1-6alkyl or Ar—C0-6alkyl; X is H, C1-4alkyl, OR′, SR′, C1-4alkylsulfonyl, C1-4alkylsulfoxyl, CN, N(R′)2, CH2N(R′)2, NO2, CF3, CO2R′, CON(R′)2, COR′, NR′C(O)R′, F, Cl, Br, I, or CF3S(O)r—; R′ is H, C1-6alkyl or Ar—C0-6alkyl; and r is 0, 1 or 2; or a pharmaceutically acceptable salt thereof.

Abstract: The present invention provides 2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3-b]indoles and 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles. These compounds are 5-HT ligands that are useful for treating diseases wherein modulation of 5-HT activity is desired.

Abstract: The present invention relates to compounds of the general formula (I) The compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).

Abstract: A composition includes a substituted dihydro- or tetrahydro-&bgr;-carboline of formula (II) or (III), wherein the aromatic ring of the carboline may include one or more substituents selected from the group consisting of hydroxy, C1-6 alkoxy, benzyloxy, C1-6 acyloxy, amino, C1-6 alkyl, C1-6 dialkylamino, halogen, and carboxy, and the C-1 position of the carboline may include a substitutent selected from the group consisting of a carbocyclic group and a heterocyclic group. The composition may include a salt or a prodrug of the substituted dihydro- or tetrahydro-&bgr;-carboline. The composition may further includes a pharmaceutically acceptable carrier, diluent, or excipient.

Abstract: A compound of formula (I) wherein: R1 is C1-C6-alkyl substituted by a group selected from OH, C1-C6-alkoxy, —OCONHC1-C6-alkyl, —OCONHC1-C6-alkyl, —NHSO2C1-C6-alkyl, and —NHCOC1-C6-alkyl, or R1 is C1-C6-alkyl substituted by a saturated or unsaturated 5- or 6-membered heterocycle containing one or two heteroatoms selected from the group consisting of nitrogen and oxygen, the heterocycle optionally substituted by a group selected from C1-C4-alkyl, halogen, and benzyl; R2 and R3 together with the nitrogen form a saturated or unsaturated 5- or 6-membered heterocyclic ring optionally containing nitrogen or oxygen as an additional heteroatom, the heterocyclic ring thereof substituted by a group selected from phenyl, benzyl, and diphenylmethyl, each of these groups optionally mono- or di-substituted by one or two groups selected from CF3, C1-C4-alkyl, C1-C4-alkoxy, phenyl, benzyl, halogen, and OH, or R2 and R3 together with the nitrogen form a saturated or unsaturated 5-

Abstract: The invention relates to certain indolinone compounds, their method of synthesis, and a combinatorial library consisting of the indolinone compounds. The invention also relates to methods of modulating the function of protein tyrosine kinases using indolinone compounds and methods of treating diseases by modulating the function of protein tyrosine kinases and related signal transduction pathways.

Abstract: Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof, wherein W, Q, X, X1, Y and Z are as defined herein. These compounds bind with high selectivity and/or high affinity to the benzodiazepine site of GABAA receptors and are therefore useful in the treatment of central nervous system (CNS) diseases and as probes for the localization of GABAA receptors in tissue samples. Also disclosed are intermediates useful in the preparation of these compounds.

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