"Rail travel at high speeds is not possible because passengers, unable to breathe, would die of asphyxia."
|8338599||Compounds having a potentiating effect on the activity of ethionamide and uses thereof|
The present invention relates to the use of compounds with a potentiating effect on the activity of antibiotics that are activatable via the EthA enzymatic pathway, for the preparation of a medicament for preventing and/or treating mycobacterial infections such as t...
|8222414||Indole compounds as an inhibitor of cellular necrosis|
The present invention relates to new indole compounds, pharmaceutically acceptable salts or isomers thereof which are useful for the prevention or treatment of cellular necrosis and necrosis-associated diseases. The present invention also relates to a method and a c...
|7829712||Pyridazine derivatives for inhibiting human stearoyl-CoA-desaturase|
Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I) where x, y, G, J, K, L, M, Q, W, V, R2, R3, R5, R5a, R6, R6a, R7...
|7777036||Heterocyclic derivatives and their use as therapeutic agents|
Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I) where y, G, K, L, M, W, V, R2, R3, R4...
|7432264||Antimicrobial biaryl compounds|
Provided are antibacterial biaryl compounds having micromolar MIC activity against Gram-negative and Gram-positive pathogens, including a methicillin-resistant S. aureus strain. ...
|7429667||Phenylamino isothiazole carboxamidines as MEK inhibitors|
The invention concerns compounds which inhibit MEK and which have activity as anti-neoplastic agents. These compounds include N-substituted-3-hydroxy-5-arylamino-isothiazole-4-carboxamidines. Also included are the tautomeric isothiazol-3(2H)-ones. ...
|7427620||Azole derivative useful as antifungal agents with reduced interaction with metabolic cytochromes|
The present invention relates to novel compounds, of the general formula (I), the N-oxide forms thereof, the salts thereof with pharmaceutically acceptable acids and the stereochemical isomers thereof, which are useful as antifungal agents; to pharmaceutical composi...
|7414048||4,5-dihydro-isoxazole derivatives and their pharmaceutical use|
The present invention is concerned with the compounds of formula wherein m, n and p are each independently 0 or 1 and q is 0, 1, 2, 3, 4 or 5; -A1=A2-A3=A4- is a pyridinylidene, p...
|7405218||Isothiazole derivatives useful as anticancer agents|
The present invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein X1, R1, R2 and R3 are as defined herein....
|7405217||N-aroyl piperazine derivatives as orexin receptor antagonists|
This invention relates to N-aroyl cyclic amino derivatives and their use as pharmaceuticals. ...
|7354919||Isoxazole compositions useful as inhibitors of ERK|
Described herein are compounds that are useful as protein kinase inhibitors, especially inhibitors of ERK, having the formula: where A, B, R1, R2, T and Ht are described in the specification. The compo...
|7351822||Serine protease inhibitors|
Compounds of formula (I) in which R2, X, Y, Cy, L and Lp(D)n have the meanings given in the specification, are inhibitors of the serine protease, Factor Xa and are useful in the treatment of cardiovasc...
|7348347||Substituted 4,5,6,7-tetrahydrobenzthiazol-2-ylamine compounds|
Substituted 4,5,6,7-tetrahydrobenzothiazol-2-ylamine compounds, a method for their production; pharmaceutical compositions comprising them, and methods of use for modulating biological functions and/or treating or inhibiting various medical conditions such as, e.g.,...
|7345043||Inhibitors of histone deacetylase|
Disclosed are compounds which inhibit histone deacetylase (HDAC) enzymatic activity. Also disclosed are pharmaceutical compositions comprising such compounds as well as methods to treat conditions, particularly proliferative conditions, mediated at least in part by ...
|7342017||1,2,5-Thiadiazol-3-yl-piperazine therapeutic agents useful for treating pain, depression and anxiety|
A compound of formula: (wherein X, R1, R3, R4, and R5 are disclosed herein) or a pharmaceutically acceptable salt thereof (a “Thiadiazolylpiperazine Compound”), pharmaceutical...
|7335660||Isochroman compounds for treatment of CNS disorders|
This invention relates to compounds of formula (I) where R1 to R12, —W—V—, —X—Y—, p and n have the values defined in claim 1, their preparation and use as pharmaceuticals for the tre...
|7329749||Piperazinylcarbonylquinolines and -isoquinolines|
Compound of the formula (I) in which R1, R2 and alk are as defined in Claim 1, are potent 5-HT2A antagonist and are suitable for the treatment of psychoses, schizophrenia, depression, neurological disorders, memory disorders, Parkins...
|7300939||Substituted 1-propiolylpiperazine compounds, their preparation and use|
Substituted 1-propiolylpiperazine compounds corresponding to formula I in which X denotes N or C—R2, and n is an integer from 0 to 8, a method for producing such substituted 1-propiolylpiperazine com...
|7294628||Piperazinylacylpiperidine derivatives, their preparation and therapeutic use thereof|
The invention relates to substituted 1-piperazinylacylpiperidine derivatives of general formula (I) in which: n is 1 or 2; R1 represents a halogen at...
|7291633||6H-oxazolo[4,5-e]indole derivatives as nicotinic acetylcholine receptor ligands and/or serotonergic ligands|
Compounds of the formula I in which R1, R2, R3 and R4 are as defined in claim 1, are ligands of the nicotinic acetylcholine receptor and/or serotonergic ligands and are suitable for the prophylaxis or treatment of psychose...
|7273882||Aminoacetamide acyl guanidines as β-secretase inhibitors|
There is provided a series of substituted acyl guanidines of Formula (Ik) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R2, R3, R4, R5, R
|7253173||4(Phenyl-piperazinyl-methyl) benzamide derivatives and their use for the treatment of pain of gastrointestinal disorders|
Compounds of general formula (I) wherein R1, R2 and R3 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in pa...
|7241764||4(phenyl-piperazinyl-methyl) benzamide derivatives and their use for the treatment of pain or gastrointestinal disorders|
Compounds of general formula:[Chemical formula should be inserted here. Please see paper copy] wherein R1, R2, and R3 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions includin...
|7238689||Isoxazoline derivative and herbicide comprising the same as active ingredient|
An isoxazoline derivative represented by the following general formula [I]: wherein R1 and R2 may be the same or different and are each an alkyl group; R
|7229998||Thiazole and oxazole derivatives as activators of human peroxisome proliferator activated receptors|
The present invention provides a compound of formula (I): wherein R1–R5, R25, R26, Y and X2 are as defined herein. The compounds a...
|7220745||Heterocyclic compounds useful to treat HCV|
The present invention relates to substituted diphenyl heterocycle compounds and pharmaceutical compositions thereof that inhibit replication of HCV virus. The present invention also relates to the use of the compounds and/or compositions to inhibit HCV replication a...
|7220744||Monocyclic substituted phenyl methanones|
The present invention relates to compounds of formula I wherein R1, R2, X1, and X2 are as defined in the specification an...
Compounds of Formula 1 [Region α]−[Region β]−[Region γ]−[Region δ] (I) which are useful as modulators of chemokine activity. The invention also provides pharmaceutical formulations and m...
|7211668||PNA monomer and precursor|
This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers:
The present invention relates to substituted bis-arylsulfonamide and arylsulfonamide compounds of the general formula (I) or the formula (II), which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obesity, type II...
|7166608||-aroyl piperazine derivatives as orexin receptor antagonists|
This invention relates to N-aroyl piperazine derivatives of formula (I), wherein: Y represents NR2; m represents 1, 2 or 3; p represents 0 or 1; X is O, S, C═O, SO2, or CH═CH—; Ar1 is aryl, or a mono or bicyclic heteroaryl grou...
|7160886||Acylated piperazine derivatives as melanocortin-4 receptor agonists|
Certain novel N-acylated piperazine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of disease...
Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful ...
|7141570||N-aryl-2-oxazolidinone-5-carboxamides and their derivatives|
The present invention provides antibacterial agents having the formula I described herein. ...
|7119203||Piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids and their use as protease inhibitors|
This invention is directed generally to proteinase (also known as “protease”) inhibitors, and, more particularly, to piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metallop...
|7115639||Pyrrolidine oxadiazole- and thiadiazole oxime derivatives being oxytocin receptor antagonists|
The present invention is related to pyrrolidine oxadiazole and thiadiazole derivatives for use as pharmaceutically active compounds, as well as pharmaceutical formulations containing such pyrrolidine oxadiazole derivatives. Said pyrrolidine derivatives are useful in...
|7105670||Intermediates useful in the preparation of diaminothiazoles|
Disclosed are novel diaminothiazoles that are selective inhibitors of Cdk4. These compounds and their pharmaceutically acceptable salts and esters are anti-proliferative agents useful in the treatment or control of solid tumors, in particular breast, colon, lung and...
|RE39265||Heteroarylpiperidines, and their use as antipsychotics and analgetics|
Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. The compound...
|7091219||Bis-sulfonamide hydroxyethyl-amino retroviral protease inhibitors|
Bis-sulfonamido hydroxyethylamino compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to retroviral protease inhibiting compounds of the formula:
|7056924||Substituted heterocyclic compounds|
Disclosed are novel heterocyclic derivatives, useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, ...