Abstract: The present invention relates to pyrazine derivatives such as those represented by Formulas (I) and (II) below. X1 to X4 of the compounds of Formulas I and II may be characterized as electron withdrawing groups. In contrast, Y1 to Y4 of the compounds of Formulas I and II may be characterized as electron donating groups. Pyrazine derivatives of the present invention may be utilized in assessing renal function. In particular, an effective amount of a pyrazine derivative of the invention may be administered into a body of a patient. The pyrazine derivative that is in the body may be exposed to visible and/or infrared light to cause spectral energy to emanate from the pyrazine derivative. This emanating spectral energy may be detected and utilized to determine renal function of the patient.

Abstract: Substituted urea compounds useful in the treatment of diseases and C1-3alkyleneOR3 conditions related to DNA damage or lesions in DNA replication are disclosed formula (I), wherein X1 is null, —O—, —S—, —CH2—, or —N(R1)—; X2 is —O—, . -£>. -, or —N(R1)—,—. . Y xs 0 or S; or =y represents two hydrogen atoms attached to a common carbon atom, —W is selected from the group consisting of heteroaryl, aryl, heterocycloalkyl, cycloalkyl, and C1-6alkyl substituted with a heteroaryl. or aryl group; R6 is —C?C—R7 or heteroaryl; R8, R9, and R10, independently, are selected from the group consisting of halo, optionally substituted C1-6alkyl, C2-6alkenyl, C2-6alkynyl, OCP3, CF3, NO2, CN, NC, N(R3)2, OR3, CO2R3, C(O)N (R3)2, C(O)R3, N(R1)COR3, N(R1)C(O)OR3, N(R8)C(O)OR3, N(R1)C(O)C1-3alkyleneC(O)R3, N(R1)C(O)C1 -3alkyleneC(O)OR3, N(R1)C(O)C1-3alkyleneOR3, N(R1)C(O)C1-3alkyleneNHC(O)OR3, N(R1)C(O)C1-3alkyleneSO2.

Abstract: The present invention is to provide a compound represented by the general formula (1) exhibiting a high insecticidal effect and an insecticide comprising the compound as an active ingredient. The compound represented by the general formula (1) and an insecticide comprising the compound as an active ingredient, wherein, in the formula, A1, A2, A3 and A4 each represent a carbon atom or the like; R1 and R2 are each a hydrogen atom, an alkyl group or the like; G1 and G2 are each an oxygen atom or the like; X represents a hydrogen atom, a halogen atom or the like; n is an integer of 0 to 4; Q1 represents a substituted phenyl group, a substituted heterocyclic group or the like; Q2 represents a phenyl group having a haloalkyl sulfur group or the like, a heterocyclic group or the like.

Abstract: The present application describes deuterium-enriched telaprevir, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: The present invention relates to sodium channel blockers. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers.

Abstract: The present invention is directed to certain hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.

Abstract: The present invention relates to compounds represented by formula (I): where the structural variables are as defined herein. The compounds are useful for promoting hydration of mucosal surfaces.

Abstract: The present invention relates to compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention. The invention further relates to processes for preparing these compounds.

Abstract: A compound of formula (I) or tautomers, or stereoisomers, or solvates, or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, T, L, W, X, Y and A are as defined herein for the for treatment of conditions mediated by the blockade of an epithelial sodium channel, particularly an inflammatory or allergic condition.

Abstract: The invention relates to the use of (3,4-di-, 3,3,4-tri, 3,4,4-tri- or 3,3,4,4-tetra-)substituted pyrrolidine compounds for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; compounds that are part of a subclass of these substituted pyrrolidine compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; new compounds that are part of a subclass of these substituted pyrrolidine compounds; pharmaceutical formulations comprising said substituted pyrrolidine compounds, and/or a method of treatment comprising administering said substituted pyrrolidine compounds, a method for the manufacture especially of said new substituted pyrrolidine compounds, as well as novel intermediates, starting materials and/or partial steps for their synthesis

Abstract: The present invention relates to sodium channel blockers. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers.

Abstract: The present invention relates to sodium channel blockers. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers.

Abstract: The present invention relates to sodium channel blockers. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers.

Abstract: The present invention relates to sodium channel blockers. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers.

Abstract: The present invention provides compound represented by formula (I): where the structural variables are defined herein. The compounds function as sodium channel blockers and may be used to treat a variety of respiratory conditions.

Abstract: The present invention relates to sodium channel blockers. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers.

Abstract: Method for preparing compounds of the formula (III) by reacting compounds of the formula (II) with a) an alcoholate or b) an alcohol R1-OH and a base in the presence of a Cu-containing catalyst and of a ligand, where X1-5 are independently of one another either carbon or nitrogen, or in each case two adjacent X1R1, with i=1?6, linked by a formal double bond together O, S, NRH or Nrl. The ligands preferably employed are acyclic and/or cyclic oligo- and polyglycols, oligo- and polyamides or oligo- and polyamine glycols of the general formula (IV) k is an integer >0 and n is an integer >1; X and Y are independently of one another O, NH or NR1.

Abstract: The present invention provides sodium channel blockers represented by formula (I): where the structural variables are defined herein. The compounds of the present invention may be used for treating a variety of conditions as described herein.

Abstract: 1. A cyclic compound of the formula (I) or a pharmacologically acceptable salt thereof, wherein X is ?CH— or ?N—, Y is —NH—, —NR4—, —S—, —O—, —CH?N—, —N?CH—, —N?N—, —CH?CH—, etc., R1 is a lower alkoxy group, an amino group, a heterocyclic ring containing N atom(s), or a hydroxy group substituted by a heterocyclic ring containing N atom(s) (each of which is optionally substituted), R2 is a lower alkylamino group which is optionally substituted by an aryl group, a lower alkoxy group which is optionally substituted by an aryl group, a lower alkoxy group substituted by an aromatic heterocyclic ring containing N atom(s), R3 is an aryl group, a heterocyclic ring containing N atom(s), a lower alkyl group, a lower alkoxy group, a cyclo lower alkoxy group, a hydroxy group substituted by a heterocyclic ring containing N atom(s), or an amino group (each of which is optionally substituted), and R3 and a substituent in Y may be combined to form a lactone ring.

Abstract: Compounds of formula I: or pharmaceutically acceptable salts thereof, are useful for controlling synaptic transmission in mammals.

Abstract: The present invention relates to sodium channel blockers. The present invention also relates to a variety of methods of treatment using these sodium channel blockers.

Abstract: The present invention relates to a compound represented by formula (I): where the structural variables are as defined herein. The compound is useful for promoting hydration of mucosal surfaces.

Abstract: Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein A, R1, R2, Rx, R8, R9 and n are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.

Abstract: This invention concerns a compound of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein R1 is hydrogen, hydroxy, cyano, amino, mono-or di(C1-4alkyl)amino, formyl, carboxyl, C1-6alkyl, hydroxyC1-6alkyl, polyhaloC1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-7cycloalkyl, C1-6alkyloxy, C1-6alkylcarbonyl, aminocarbonyl, —S(?O)m—NH2, mono-or di(C1-4alkyl)aminocarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyloxy, aryl, arylC1-6alkyl or aryloxy; R2 is hydrogen; halo; mercapto; formyl; cyano; carboxy; azido; hydroxy; oxiranyl; amino; mono- or di(C1-4alkyl)amino; formylamino; R5R6N—C(?O)—; R7—N?C(R8)—; C1-6alkyl-S(?O)m; aryl-S(?O)m; optionally substituted C2-6alkenyl; optionally substituted C2-6alkynyl; C1-6alkyloxy; hydroxyC1-6alkyloxy; aminoC1-6alkyloxy; mono- or di(C1-4alkyl)amino-C1-6alkyloxy; C1-6alkylcarbonyl; arylcarbonyl; Het1carbonyl; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; aryl; aryloxy; arylC1-6alkyloxy; arylthio; arylC1

Abstract: Compounds are provided which are represented by the formula: where the structural variables are defined herein. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers.

Abstract: The present invention provides substituted pyrazine derivatives of Formula I, that are CRF1 receptor antagonists, including human CRF1 receptors. This invention also relates to use of compounds of the invention for treating a disorder or condition, the treatment of which can be effected or facilitated by antagonizing a CRF receptor, such as CNS disorders, particularly anxiety-related disorders and mood disorders.

Abstract: The present invention relates to compounds of general formula (I), wherein R1-R4 have the meanings given in the specification, A is CH2, CHOH or CH—(C1-C3-alkyl), B and C are independently CH2 or CH—(C1-C3-alkyl), and R5 is an aryl or heteroaryl group optionally substituted by the substituents listed in the specification.

Abstract: The present invention relates to pyrazinoylguanidine compounds represented by formula (I): where at least one of R3 and R4 is a group represented by formula (A): where the other structural groups are defined herein. The present invention also includes a variety of methods of treatment using these sodium channel blockers.

Abstract: The present invention relates to a compound represented by formula (I): in which at least one of R3 and R4 is a group represented by formula (A): where the structural variables are as defined herein. The compounds are useful for blocking sodium channels.

Abstract: The present invention relates to compounds represented by formula (I): in which at least one of R3 and R4 is a group represented by formula (A): where the structural variables are defined herein. The compounds are useful for blocking sodium channels.

Abstract: Heterocyclic substituted aminoazacyclic compounds of formula I Z—R3  I, wherein Z is a defined aminoazacycle and R3 is a defined heterocycle moiety, pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.

Abstract: The present invention relates to compounds, and prodrugs thereof, composition and methods useful for preventing and treating thrombotic conditions in mammals. The compounds of the present invention, and prodrugs thereof, selectively inhibit certain proteases of the coagulation cascade.

Abstract: A nitrogen-containing six-membered heterocyclic compound having substituents —X—A—R3, —N(R1)-(Ph substituted by R2), and —CONH2, a salt thereof, a prodrug thereof, and a Syk inhibitor containing the same as an active ingredient. (In the formula, A: a (substituted) lower alkylene, a (substituted) arylene, or the like; X: NR4, CONR4, NR4CO, O, or S; R1, R4: H, a lower alkyl, —CO-lower alkyl, or —SO2-lower alkyl; R2: H, a (substituted) lower alkyl, —O-lower alkyl, —S-lower alkyl, —O-aryl, nitro, cyano, or the like; R3: —CO2H, —CO2-lower alkyl, -lower alkylene-CO2H, —NH2, -alkylene-NH2 or the like.

Abstract: An aromatic nitrogen-containing 6-membered cyclic compound of the formula (I): wherein Ring A is a substituted or unsubstituted nitrogen-containing heterocyclic group; R1 is a substituted or unsubstituted lower alkyl group, —NH—Q—R3 (R3 is a substituted or unsubstituted nitrogen containing heterocyclic group, and Q is a lower alkylene group or a single bond), or —NH—R4 (R4 is a substituted or unsubstituted cycloalkyl group); R2 is a substituted or unsubstituted aryl group; one of Y and Z is ═CH—, and the other is ═N—, or a pharmaceutically acceptable salt thereof, these compounds exhibiting excellent selective PDE V inhibitory activities, and hence, being useful in the prophylaxis or treatment of penile erectile dysfunction, etc.

Abstract: Couplers for hair coloring compositions for oxidative dyeing of hair are compounds of the formula (1): where R1 and R2 are each individually selected from a hydrogen atom, a C1 to C3 alkyl group, a C1 to C5 mono or dihydroxyalkyl group; phenyl or benzyl optionally substituted with an alkoxy group, or R1 and R2 together with the nitrogen atom to which they are attached form a piperazine, piperidine, imidazole, or morpholine ring.

Abstract: The present invention relates to compounds, and prodrugs thereof, composition and methods useful for preventing and treating thrombotic conditions in mammals. The compounds of the present invention, and prodrugs thereof, selectively inhibit certain proteases of the coagulation cascade.

Abstract: The invention relates to compounds of formula I 1

Abstract: The invention relates to polycyclic aryl and heteroaryl substituted 4-pyridone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.

Abstract: Compounds of formula (I), pharmaceutically acceptable salts or in vivo hydrolysable esters thereof, wherein: Ring X is phenyl or a six membered heteroaryl ring containing one or two ring nitrogens where said nitrogens are optionally oxidised to form the N-oxide; R1 and R2 are substituents as defined within; R3 and R4 are defined within and are alkyl or halo alkyl or together form a halocycloalkyl ring; R5 is a substituent as defined within; Y—Z is a linking group as defined within; are useful in the production of a elevation of PDH activity in a warm-blooded animal such as a human being. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are described.

Abstract: Diacylhydrazine derivatives of general formula (I) wherein X, Y, Z, R1, 2 and R3 are as defined herein, and their physiologically acceptable salts or solvates thereof, are integrin inhibitors and can be used to combat thromboses, myocardial infarcts, coronary cardiac diseases, arteriosclerosis, inflammations, tumors, osteoporosis, infections, and restenosis following angioplasty or during pathological processes that are maintained or propagated by angiogenesis.

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

Abstract: The present invention relates to compounds, and prodrugs thereof, composition and methods useful for preventing and treating thrombotic conditions in mammals. The compounds of the present invention, and prodrugs thereof, selectively inhibit certain proteases of the coagulation cascade.

Abstract: PDE4 inhibition is achieved by novel compounds, e.g., N-substituted aniline and diphenylamine analogs.

Abstract: This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.

Abstract: This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.

Abstract: This invention relates to compounds which are IP receptor antagonists and which are represented by Formula (I): wherein G2 is a heteroaryl group containing one or two nitrogen atoms substituted with a carboxylic acid group, said heteroaryl ring containing one or two nitrogen atoms, and G1 is as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.

Abstract: Disclosed are novel 1,4-disubstituted benzo-fused compounds wherein G, X, L, Q, n and Y are defined herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are processes of making such compounds.

Abstract: Compositions, methods of use, isolation and biosynthesis of diimino-piperazine derivatives useful for the modification of sphingolipid metabolism and other biological functions are described. The preferred derivative is 2,6-bis-(&ohgr;-aminobutyl)-3,5-diimino-piperazine. This is a naturally occurring biochemical compound isolated from cells. The diimino-piperazine derivatives are useful as therapeutic agents when administered to patients to treat diseases and disorders involving cell regulation.

Abstract: The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, —R1—R2— is a bivalent radical of formula wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C1-6alkyl or hydroxy; R3 is hydrogen or halo; R4 is hydrogen or C1-6alkyl; R5 is hydrogen or C1-6alkyl; L is C3-6cycloalkyl, oxoC5-6cycloalkyl, C2-6alkenyl, or L is a radical of formula —Alk—R6—, Alk—X—R7, —Alk—Y—C(═O)—R9, or —Alk—Y—C(═O)—NR11R12 wherein each Alk is C1-12alkanediyl; and R6 is hydrogen, amino, cyano, C1-6alkylsulfonylamino, C3-6cycloalkyl, oxoC5-6cycloalkyl, aryl or a heterocyclic ringsystem; R7 is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C3-6cycloalkyl, aryl or a heterocyclic ringsystem; X is O, S, SO2 or NR8; said R8 being hydrogen or C1-6alkyl; R9 is hydrogen, C1-6alkyl, C3-

Abstract: A compound of formula (I) wherein R1 is phenyl substituted by one or more halogen atoms; R2 is —NH2; R3 is —NH2 or hydrogen; R4 is —CXNRaRb, —CXNH—(CH2)y—NRaRb; wherein X is ═O or ═S; y is an integer zero, 1 or 2; Ra and Rb, which may be the same or different, are selected from hydrogen and C1-4 alkyl or together with the nitrogen atom to which they are attached form a saturated 5- or 6-membered heterocycle containing one or two nitrogen heteroatoms, which heterocycle can be further substituted with one or more C1-4 alkyl groups; and pharmaceutically acceptable derivatives thereof.