Abstract: A method for preparing a N-[(aliphatic or aromatic)carbonyl)]-2-aminoacetamide compound, and for preparing a cyclized compound therefrom, as well as novel resin bound intermediate compounds that are useful for preparing such compounds.

Abstract: This invention is directed to a [di(ether or thioether)heteroaryl or fluoro substituted aryl] compound or an N-oxide thereof or a pharmaceutically acceptable salt thereof, which is useful for inhibiting the production or physiological effects of TNF in the treatment of a patient suffering from a disease state associated with a physiologically detrimental excess of tumor necrosis factor (TNF). Compounds within the scope of the present invention also inhibit cyclic AMP phosphodiesterase, and are useful in treating a disease state associated with pathological conditions that are modulated by inhibiting cyclic AMP phosphodiesterase, such disease states including inflammatory and autoimmune diseases, in particular type IV cyclic AMP phosphodiesterase. The present invention is therefore directed to their pharmacological use for inhibiting TNF and/or cyclic AMP phosphodiesterase, pharmacological compositions comprising the compounds and methods for their preparation.

Abstract: This invention is directed to cyclic and acyclic analogs of hPTH(1-34) and hPTHrP(1-34), to pharmaceutical compositions comprising these peptide compounds, and to a method of treating diseases associated with calcium regulation in the body.

Abstract: This invention is directed to a process for preparing N6-substituted adenosine derivatives, to intermediates useful therefor and to methods of preparing these intermediates.

Abstract: The invention concerns pyrazine derivatives of formula (1) in which a pharmaceutical composition comprising at least one compound of formula: in which R represents a nitrogen atom, R1 and R3 each represent the same radical selected from the group consisting of —CO—NR5R6, —CO—N(CH(CH2OH)2)2, —CO—N(CH2OH)2, —CO—N(CH2—CH(CH2OH)2)2, —CO—N(CH2—(CHOH)n—CH2OH)2 in which n is equal to 0, 1, 2, 3 or 4, —CH2—O—R6, —NR5—CO—R6, —CH2—NR5R6, —CH2—N(CH2OH)2, —CH2—N(CH2—(CHOH)y—CH2OH)2 in which y is equal to 0, 1, 2, 3 or 4, —CH2—N(CH(CH2OH)2)2 and —CH2—N(CH2—CH(CH2OH)2)2 and R2 and R4 each represents a hydrogen atom, R5 represents a hydrogen atom or an alkyl radical, R6 represents a radical —CH2—(CHOH)m—CH2OH in which m is equal to 0, 1, 2, 3 or 4, -alk-O-alk-CH2OH, -alk-O-alk, —CH(CH2OH)2,

Abstract: A pharmaceutical composition containing at least one stereoisomer of at least one compound selected from: Or a salt thereof with an organic or inorganic acid.

Abstract: This invention is directed to a process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and &agr;,&bgr;-unsaturated carboxylic acid and aldehyde compounds and to polymeric hydroxylamine resin compounds useful therefor.

Abstract: Disclosure is a method for preparing &agr;-aspartyl-&bgr;-cyclohexylalaninamide, comprising carrying out a first step of amide formation of an &agr;-aspartyl phenylamine ester of general formula (II) wherein: R is a C1-C4 alkyl radical, and then performing a catalytic hydrogenation of the resulting &agr;-aspartyl phenylalaninamide ammonium salt, optionally released previously from its salt, and optionally transforming it into an addition acis salt.

Abstract: Provided herein are novel polyhydroxyalkylpyrazine derivatives useful in treating and preventing a plethora of diseases including diabetes, having a general formula of wherein Rc1 represents the chain (II) —CH(OR4)CH(OR3)CH(OR2)CH2OR1 and either Rc2 represents a hydrogen atom and either Rc3 represents the chain (III)—CH2CH(OR6)CH(OR7)CH2OR8 or Rc2 represents the chain (IV)—CH(OR5)CH(OR6)CH(OR7)CH2OR8 or chain (III) —CH2CH(OR6)CH(OR7)CH2OR8 and Rc3 represents a hydrogen atom, and 1 to 8 substituents R1, R2, R3, R4, R5, R6, R7, R8, identical or different, represent a radical independently selected among the radicals a) —COR9, b) —COOR10, c) —CR11R12OCOR13, d) —CR11R12OR13, e) —CONR14R15, and f) one or more pairs of the substituents R1, R2, R3, R4, R6, R7, R8, consecutive or separated by one of the other substituents R2, R3, R6, R7 can also form a group: —C(O)—; the other substituents R1, R2, R3, R4, R6, R7, R8 are hydrogen atoms

Abstract: Trauma of the central nervous system is prevented and treated by administering an effective amount of a low molecular weight heparin.

Abstract: A compound of the formula wherein K is N; Q is CH2 or O; R6 is hydrogen, alkyl, allyl, 2-methylallyl, 2-butenyl, or cycloalkyl where the nitrogen of the ring of X is substituted by Y; E is O or S; Y is hydrogen, alkyl, aralkyl, substituted aralkyl, aryl, substituted aryl, heterocyclyl, substituted heterocyclyl, heterocyclylalkyl, or substituted heterocyclylalkyl; and n and p are independently 0, 1, 2, or 3, provided that n+p is at least 1; T is hydrogen, alkyl, alkylcarbonyl, alkylthiocarbonyl, halo, carboxyl, A and B are independently hydrogen, alkyl, hydroxyalkyl, alkoxyalkyl, or OR′; or a pharmaceutically acceptable salt thereof, a pharmaceutic-ally acceptable prodrug thereof, an N-oxide thereof, a hydrate thereof or a solvate thereof.

Abstract: Disclosed are thiazolobenzoheterocycles of the general formula Including their isomers, racemates, enantioners and salts thereof, as well as processes for preparing these compounds and medicaments containing them.

Abstract: The present invention relates to medicaments comprising at least one compound of formula: wherein either R1 represents a —CH(Ra)—CHOH—CHOH—CH2OH chain and R2 represents a —CH2—CHOH—CHOH—CH2OH chain, or R1 represents a —CHOH—CHF—CHOH—CH2OH chain and R2 represents a —CH2—CHF—CHOH—CH2OH chain, or R1 represents a —CHOH—CHOH—CHOH—Rb chain and R2 represents a —CH2—CHOH—CHOH—Rb chain, or R1 represents a —CH2—CHOH—CHOH—CH2OH chain and R2 represents a —CH2—CHOH—CHOH—CH2OH chain, or R1 and R2 are identical and each represent a —(CHOH)n—CH2OH chain in which n is equal to 1, 2, 3 or 4, Ra represents an alkoxy radical (1-6 C in a straight or branched chain) or a fluorine atom, and Rb represents a carboxyl, —CO—NH2 or —CH2—NH2 radical, or one of their stereoisomers or thei

Abstract: The present invention relates to pharmaceutical compositions containing, as an active ingredient, at least one compound of formula: in which R1 represents a radical —N(R4)R5, —N(R4)—CO—R5, —N(R4)—SO2R6 or one of its pharmaceutically acceptable salts, to the novel derivatives of formula (I), to their pharmaceutically acceptable salts and to their preparation.

Abstract: The present invention relates to the combination of riluzole and of gabapentin or one of their pharmaceutically acceptable salts and its use as a medicament which is useful in particular for the prevention and/or treatment of motoneuron diseases.

Abstract: This invention relates to compounds of formula which inhibit Factor Xa, to pharmaceutical compositions containing the compounds, and to the use of the compounds for the treatment of patients suffering from conditions which can be ameliorated by the administration of an inhibitor of Factor Xa.

Abstract: This invention relates to compounds of general formula (I): in which Ar is a group selected from: A1, A2, B, C, D, E, Q1-Q3, R1-R9, Z1 and Z2 are as defined in the disclosure, and Y represents carboxy or an acid bioisostere. These compounds inhibit the production or physiological effects of TNF and inhibit cyclic AMP phosphodiesterase. The invention is also directed to pharmaceutical compositions comprising compounds of formula (I), their pharmaceutical use and methods for their preparation.

Abstract: The present invention is directed to a process for preparing 2,4-dihydroxy-pyridine comprising heating a compound of the formula A wherein R is H, alkyl or aralkyl and phosphoric acid where the ratio of phosphoric acid to water is not less than about 27 to 1 weight %. The invention is also directed to a process for preparing 2,4-dihydroxy-3-nitropyridine comprising reacting 2,4-dihydroxypyridine with nitric acid. The processes of the present invention prepare intermediates which are useful in preparing compounds which are useful for treating cardiovascular disease marked by hypertension or myocardial ischemia, ameliorating ischenic injury or myocardial infarct size, or treating hyperlipidemia or hypercholesterolemia.

Abstract: This invention is directed to certain physiologically active compounds of formula (I) wherein represents a bicyclic ring system, of about 10 to about 13 ring members, in which the ring is an azaheterocycle, and the ring represents an azaheteroaryl ring, or an optionally halo substituted benzene ring; and N-oxides thereof, and their prodrugs, and pharmaceutically acceptable salts and solvates of the compounds of formula (I) and N-oxides thereof, and their prodrugs. Such compounds inhibit the production or physiological effects of TNF and inhibit cyclic AMP phosphodiesterase. The invention is also directed to pharmaceutical compositions comprising compounds of formula (I), their pharmaceutical use and methods for their preparation.

Abstract: The present invention relates to a method for the prevention or treatment of a motoneuron disease with a combination of an ergoline chosen from nicergoline and lumilysergol and of riluzole or one of its pharmaceutically acceptable salts.