Abstract: Novel compounds which are inhibitors of the binding of fibrinogen to the Gp IIb/IIIa platelet receptors, and which can be used therepeutically as antithrombotic agents

Abstract: A compound of the formula: wherein R1 and R2 each represents a lower alkyl, or R1 and R2 may be bonded together to form a ring; X represents a spacer of which the number of atoms constituting the principal chain is 1 to 15; Y represents an acyl, or a hydroxy, an amino or an aromatic group, each of which may be substituted; and ring A represents a 5- to 8-membered ring which may be further substituted apart from —X—Y, or a salt thereof is useful as a pharmaceutical composition for preventing or treating disease related to mitochondrial dysfunction.

Abstract: A process for the preparation of high quality amine oxides by reacting a tertiary or secondary amine with hydrogen peroxide as an oxidant in the presence of a recyclable heterogeneous layered double hydroxide exchanged with one of the anions of transition metal oxides as a catalyst in an organic solvent at a temperature ranging between 10-25° C. for a period of 1-6 hours under continuous stirring and separating the product by simple filtration and subsequently evaporation of solvents by known methods.

Abstract: The present invention relates to novel carboxy substituted acyclic carboxamide derivatives of formula (1)): and stereoisomers and pharmaceutically acceptable salts thereof and their use as tachykinin receptor antagonists. Such antagonists are useful in the treatment of tachykinin-mediated diseases and conditions disclosed herein including: asthma, cough, and bronchitis.

Abstract: Disclosed is a process for preparing a compound of the formula: wherein X1, X2, X3, X4, and X5 are independently selected from the group consisting of H, halo, alkyl, alkoxy, aryl, and aryloxy, and R is a protecting group, in which a compound having the formula wherein X1, X2, X3, X4, and X5 are as defined above, is treated with the following, in any sequence: (a) a non-nucleophilic strong base; (b) a chiral amino alcohol; and (c) a compound having the formula wherein L is a leaving group and R is as defined above. The compounds made by this process are useful intermediates for preparing compounds that are inhibitors of farnesyl protein transferase.

Abstract: The invention relates to new arylglycinamide derivatives of general formula I and the pharmaceutically acceptable salts thereof, wherein R1 and R2 together with the N to which they are bound form a ring of the formula  wherein is 2 or 3 and X denotes oxygen, N(CH2)nR6 or CR7R8, and R34 R5 R6 R7, R8, Ar and n have the meanings given in the specification, and the preparation and use thereof. The new compounds are valuable neurokinin (tachykinin)-antagonists.

Abstract: Disclosed are 4,4-disubstituted and 3,3-disubstituted piperidine compounds of formula I wherein D, E, G, J, R1, a, b, c, and d are defined in the specification, compositions containing them, and their use for treating medical disorders resulting from a deficiency in growth hormone.

Abstract: Compound of the formula (I): wherein Ar is a group of the following formula (Ar-1) or (Ar-2): A is a group of the formula: —Z—N(Q1)(Q2), —CO—R7 or —(CH2)p—CH(R8)—COR9, or a pharmaceutically acceptable acid addition salt thereof, a process for preparing the same, a pharmaceutical composition containing the same, and intermediates therefor. The compounds of the present invention show a potent affinity for 5-HT4 receptors, and they are useful as a gastrointestinal motility enhancer or a gastrointestinal prokinetic agent.

Abstract: Amide derivatives of 1,4 di-substituted piperidine compounds of the formula or a pharmaceutically acceptable salt, ester or solvate thereof, wherein Q and Q1 are each —CH═, or one of Q and Q1 is —CH═ and the other is —N═; X is —CH2— or Y and Z are —C(R5)═, or one of Y and Z is —C(R5)═ and the other is —N═; R1 is 1 to 3 substituents selected from H, halogen and alkoxy; R2 and R5 are 1 to 3 substituents selected from H, halogen, alkyl and alkoxy; and R3 and R4 are H or (C1-C6)alkyl are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed.

Abstract: Novel compounds are provided which are inhibitors of MTP and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases, and have the structure including pharmaceutically acceptable salts thereof, or prodrug esters thereof, A is where Z is N or CH, or where Z is  or CH2 when is a single bond; and wherein L1, R, R1, R3, R3′, R3a, R3b, R4, R4′, R5, R5a, X,  are as defined herein.

Abstract: This invention relates to &bgr;-alanine derivative represented by the following formula (I); 1

Abstract: Hindered amines substituted on the N-atom with an —O—E—OH moiety are particularly effective in stabilizing polyolefin and automotive coating compositions against the deleterious effects of oxidative, thermal and actinic radiation where the presence of the OH group on the compounds adds important properties not attainable by the use of normal —O—E moieties.

Abstract: Novel compounds of the formula 1

Abstract: The present invention provides a short, convergent total synthesis of irinotecan and derivative compounds which comprises of a novel 4+1 radical annulation wherein the precursor is reacted with an aryl isonitrile having the formula wherein X is Br or I, and R4 is an alkyl group, an allyl group, a propargyl group or a benzyl group, and R16 is H, a C1-C6 alkoxy group, a group wherein p is an integer between 4 and 12, or a C1-C12 acyclic dialkylamino group. The present invention also provides novel chemical intermediates for such 4+1 radical annulations.

Abstract: There are disclosed compounds of formula (I) and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.

Abstract: 1,2-Bis-adducts of stable hindered nitroxide compounds with substituted ethylenes are prepared by reacting two equivalents of nitroxyl compound with an ethylenically unsaturated compound such as styrene or an acrylate ester. These adducts are very effective inhibitors to prevent the premature polymerization of ethylenically unsaturated monomers when such monomers are distilled, processed or stored.

Abstract: Orally-active nipecotamide glycolamide ester derivatives of formula (I): are disclosed as useful in treating platelet-mediated thrombotic disorders.

Abstract: The present invention concerns compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein n is 0, 1 or 2; m is 1 or 2, provided that if m is 2, then n is 1; p is 0, 1 or 2; ═Q is ═O or ═NR3; X is a covalent bond or a bivalent radical of formula —O—, —S—, —NR3—; R1 is Ar1; Ar1C1-6alkyl or di(Ar1)C1-6alkyl, wherein each C1-6alkyl group is optionally substituted with hydroxy, C1-4alkyloxy, oxo or a ketalized oxo substituent of formula —O—CH2—CH2—O— or —O—CH2—CH2—CH2—O—; R2 is Ar2; Ar2C1-6alkyl; Het or HetC1-6alkyl; R3 is hydrogen or C1-6alkyl; R4 is hydrogen; C1-4alkyl; C1-4aklyloxyC1-4alkyl; hydroxyC1-4alkyl; carboxyl; C1-4aklyloxycarbonyl or Ar3; R5 is hydrogen; hydroxy; Ar3; Ar3C1-6alkyloxy; di(Ar3)C1-6alkyloxy; Ar3C1-6alkylthio; di(Ar3)C1-6alkylthio; Ar3C1-6alkylsulfoxy; di(Ar3)C1-6alkylsulfoxy;

Abstract: New compounds are disclosed for multimerizing immunophilins and proteins containing immunophilin or immunophilin-related domains.

Abstract: The present invention provides a highly safe and easily operable process for producing 1-chlorocarbonyl-4-piperidinopiperidine or hydrochloride thereof in a high yield. Described specifically, the present invention relates to a process for producing 1-clorocarbonyl-4-piperidinopiperidine or hydrochloride thereof, which comprises reacting 4-piperidinopiperidine with a trialkylsilyl halide to obtain a 4-piperidinopiperidinyl trialkylsilyl, reacting it with a carbon dioxide gas to obtain a 4-piperidinopiperidinyl trialkylsilyl carbamate derivative, reacting the derivative with thionyl chloride or the like to obtain 1-chlorocarbonyl-4-piperidinopiperidine hydrochloride and optionally treating it with a strong base.

Abstract: This invention relates to sulfamides of formula (I) ##STR1## that are inhibitors of metalloproteases, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.

Abstract: A process for the re-racemisation of a (-)-2-phenylmethyl-3,3-dimethyl-piperidin-4-on derivative wherein a (-)-2-phenylmethyl-3,3-dimethyl-piperidin-4-on derivative of the formula 8.sub.BwhereinR.sub.2 denotes hydrogen C.sub.1 -C.sub.6 -alkyl, halogen, C.sub.1 -C.sub.8 -alkoxy, a benzoyl group bound via an oxygen or an alkylcarboxyl group having a straight chained or branched C.sub.1 -C.sub.6 -lower alkyl group--wherein the alkyl group may optionally be substituted by one or more halogen atoms which may be identical or different;is heated to yield a racemic mixture of compounds of the formulae 8.sub.A and 8.sub.

Abstract: A multi-branched compound which can give a compound having a relatively high molecular weight but a low viscosity and having excellent coating performances, and can give a solvent-less composition having sufficient coating performances and having a low viscosity sufficient for forming a coating, and which can serve to decrease the amount of a low-molecular-weight compound having performance problems and the multi-branched compound is obtained by reacting a core compound obtained by subjecting (a) a polyamino compound having a molecule containing a primary or secondary amino group and (b-1) an active-hydrogen-containing (meth)acrylic compound in Michael addition reaction with (c) a vinyl-group-containing compound having a functional group reactive with the active hydrogen.

Abstract: New compounds are disclosed for multimerizing immunophilins and proteins containing immunophilin or immunophilin-related domains. The compounds are of the formulaM.sup.1 --L--M.sup.2where M.sup.1 and M.sup.2 are independently moieties of the formula: ##STR1## in which B.sup.1, B.sup.2, B.sup.3, R.sup.1, R.sup.2, n, W, X and Y are as defined.

Abstract: A compound of formula: ##STR1## in which: Ar represents a pyrid-2-yl or a phenyl which is unsubstituted or substituted by a halogen, a methyl or a (C.sub.1 -C.sub.4)alkoxy;R.sub.1 represents a methyl group;R.sub.11 represents hydrogen;or R.sub.1 and R.sub.11 together represent a --(CH.sub.2).sub.3 -- group;R.sub.2 represents a hydroxyl; a (C.sub.1 -C.sub.7)alkoxy; a (C.sub.1 -C.sub.7)acyloxy; a cyano; an --NR.sub.6 R.sub.7 group; an --NR.sub.3 COR.sub.4 group; an --NR.sub.3 COOR.sub.8 group; an --NR.sub.3 SO.sub.2 R.sub.9 group; an --NR.sub.3 CONR.sub.10 R.sub.12 group; a (C.sub.1 -C.sub.7)acyl group; a (C.sub.1 -C.sub.7)alkoxycarbonyl; a --CONR.sub.10 R.sub.12 group; a --CH.sub.2 OH group; a (C.sub.1 -C.sub.7)alkoxymethyl; a (C.sub.1 -C.sub.7)acyloxymethyl; a (C.sub.1 -C.sub.7)alkylaminocarbonyloxymethyl; a --CH.sub.2 NR.sub.13 R.sub.14 group; a --CH.sub.2 NR.sub.3 COR.sub.4 group; a --CH.sub.2 NR.sub.3 COOR.sub.8 group; a --CH.sub.2 NR.sub.3 SO.sub.2 R.sub.9 group; a --CH.sub.2 NR.sub.3 CONR.sub.10 R.sub.

Abstract: A new process is described for the preparation of a compound of the formula I ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4, independently of each other, are C.sub.1 -C.sub.8 alkyl or C.sub.1 -C.sub.5 hydroxyalkyl, or R.sub.1 and R.sub.2 together with the carbon atom they are attached to are C.sub.5 -C.sub.2 cycloalkyl, or R.sub.3 and R.sub.4 together with the carbon atom they are attached to are C.sub.5 -C.sub.12 cycloalkyl; R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9, independently of each other, are H, C.sub.1 -C.sub.8 alkyl, C.sub.2 -C.sub.8 alkenyl, C.sub.5 -C.sub.12 aryl, C.sub.1 -C.sub.4 haloalkyl, an electron withdrawing group, or C.sub.6 -C.sub.12 aryl which is substituted by a residue selected from C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halogen; and R.sub.7 and R.sub.

Abstract: Compounds of formula I ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, and Q.sup.4 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists Substance P and NKA, useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.

Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as selective alpha-1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing orthostatic hypotension. One such tissue is found surrounding the urethral fining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.

Abstract: Carboxamide derivatives of pyrrolidine, piperidine, and hexahydroazepine of formula (I): ##STR1## are disclosed as useful in treating platelet-mediated thrombotic disorders.

Abstract: This invention relates to compounds of the formula: ##STR1## which are effective for inhibiting platelet aggregation, pharmaceutical compositions for effecting such activity, and a method for inhibiting platelet aggregation.

Abstract: Orally-active nipecotamide glycolamide ester derivatives of formula (I): ##STR1## are disclosed as useful in treating platelet-mediated thrombotic disorders.

Abstract: Compounds within the genus represented by the structural formula I ##STR1## or a pharmaceutically acceptable salt thereof, wherein: T is substituted phenyl or substituted pyridyl; ##STR2## R.sup.4 is methyl or ethyl; and Z is substituted piperidinyl.

Abstract: A 1,2-di-substituted piperidine derivative or a salt thereof expressed by the following Formula (I): ##STR1## wherein one of A and B is a hydrocarbon group of C.sub.1-30 expressed by R.sup.1 and the other is --(CH.sub.2)n-NR.sup.2 R.sup.3 ; Y is --CO--, --CONR.sup.5 -- or --COO--; Z is --O--, --OCO--, --OCONR.sup.6 -- or --NR.sup.6 --; R.sup.2 and R.sup.3 individually represent a hydrogen a lower alkyl, a phenyl or a benzyl group, or together represent a heterocycle having 3-7 members; --NR.sup.5 --(CH.sub.2)n-NR.sup.2 R.sup.3 and --NR.sup.6 --(CH.sub.2)n-NR.sup.2 R.sup.3 of --(Y).sub.1 --A and --Z--B may be the following Group W: ##STR2## wherein ring E is a heterocycle of 6 or 7 members including two nitrogen atoms and R.sup.2 is a hydrogen, a lower alkyl, a phenyl or a benzyl group; R.sup.

Abstract: Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.21, R.sup.27, R.sup.28, X, Y, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations of compounds of the above formula with acetylcholinesterase inhibitors.

Abstract: This invention relates to compound of formula (I) which are effective for inhibiting platelet aggregation, pharmaceutical compositions for effecting such activity, and a method for inhibiting platelet aggregation.

Abstract: Compounds of formula (I), a method for obtaining them and pharmaceutical compositions containing them are described. The compounds are useful as human NK.sub.3 receptor antagonists.

Abstract: Novel compounds, compositions and methods effective for the prevention and treatment of mast-cell mediated inflammatory disorders are described. The compounds, compositions and methods are effective for the prevention and treatment of inflammatory diseases associated with the respiratory tract, such as asthma and allergic rhinitis, as well as other types of immunomediated inflammatory disorders, such as rheumatoid arthritis, conjunctivitis and inflammatory bowel disease, various dermatological conditions, as well as certain viral conditions. The compounds comprise potent and selective inhibitors of the mast cell protease tryptase. The compositions for treating these conditions include oral, inhalant, topical and parenteral preparations as well as devices comprising such preparations.

Abstract: Products are described which can be obtained by reacting components a), b) and c), where component a) is a compound of the formula I or a mixture of compounds of the formula I, component b) is a compound of the formula II or a mixture of compounds of the formula II and component c) is a compound of the formula III or a mixture of compounds of the formula III, ##STR1## in which the general symbols are as defined in claim 1, the compound of the formula I being, for example, pentaerythritol, thiodiethylene glycol, 1,4-butanediol, 1,4-propanediol, diethylene glycol, triethylene glycol, diethanolamine or glycerol, the compound of the formula II being, for example, sunflower oil or coconut fat, and the compound of the formula III being, for example, methyl 3-(3',5'-di-tert-butyl-4'-hydroxyphenyl)propionate. The abovementioned products can be used as liquid antioxidants in polymers and lubricants.

Abstract: Method of treating or reducing the risk of human disease or condition in which the synthesis or oversynthesis of nitric oxide forms a contributory part wherein a therapeutically effective amount of the compound of formula (I) as defined in the specification is administered to a person suffering from or susceptible to such disease or condition.

Abstract: Compounds of formula (I), wherein Y is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, OH, CN, NO.sub.2, Si(CH.sub.3).sub.3, CF.sub.3 or halogen, and T is a group (a) or (b), and wherein the remaining substituents have the following definitions: X is O, S or NR.sub.13 ; A is O or NR.sub.4 ; R.sub.1 is hydrogen, C.sub.1 -C.sub.4 alkyl, halo-C.sub.1 -C.sub.4 alkyl, cyclopropyl, C.sub.1 -C.sub.4 alkoxymethyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio or cyano; R.sub.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, cyano unsubstituted or substituted C.sub.1 -C.sub.6 alkoxycarbonyl, unsubstituted or substituted di(C.sub.1 -C.sub.6 alkyl)aminocarbonyl, unsubstituted or substituted C.sub.1 -C.sub.6 alkyl-S(O).sub.q, unsubstituted or substituted aryl-S(O).sub.q, unsubstituted or substituted heteroaryl, unsubstituted or substituted heterocyclyl, unsubstituted or substituted heterocyclylcarbonyl or unsubstituted or substituted phenyl; and R.sub.

Abstract: Heterocyclic compounds IR.sup.1 --X--L (I)whereL is a cyclic carbamate residue, a lactonoxy residue or a lactam residue,X is an oxygen-containing group ##STR1## where A is a linker, and R.sup.1 is an organic radical or a group L,are used as activators for inorganic peroxy compounds, in particular as cold bleach activators or optical brighteners in detergents, cleaners and bleaches and in disinfectants.

Abstract: New compounds of the formula (A) ##STR1## a process for their preparation and their use in the manufacture of pharmaceutical preparations. The new compounds have both local anaesthetic and analgesic effect.

Abstract: The present invention is directed to certain piperidines, pyrrolidines, and hexahydro-1H-azepines of the general structural formula: ##STR1## wherein B is selected from: ##STR2## and R.sup.1, R.sup.1a, R.sup.2a, R.sup.3a, R.sup.3b, R.sup.4, R.sup.4a, R.sup.4b, R.sup.4c, R.sup.5, D, X, Y, n, x and y are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such compounds as the active ingredient thereof are also disclosed.

Abstract: Novel compounds are provided which are inhibitors of MTP and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases, and have the structure ##STR1## including pharmaceutically acceptable salts thereof, or prodrug esters thereof,A is ##STR2## where Z is N or CH, or where Z is ##STR3## or CH.sub.2 when --- is a single bond; Q is (1)--O--;(2)--S--; or ##STR4## B is: ##STR5## and wherein L.sup.1, R, R.sup.1, R.sup.3, R.sup.3 ', R.sup.3a, R.sup.3b, R.sup.4, R.sup.4 ', R.sup.5, R.sup.5a, X, ##STR6## are as defined herein.

Abstract: A compound of formula: in which:Ar represents a pyrid-2-yl or a phenyl which is unsubstituted or substituted by a halogen, a methyl or a (C.sub.1 -C.sub.4)alkoxy;R.sub.1 represents a methyl group;R.sub.11 represents hydrogen;or R.sub.1 and R.sub.11 together represent a --(CH.sub.2).sub.3 -- group;R.sub.2 represents a hydroxyl; a (C.sub.1 -C.sub.7)alkoxy; a (C.sub.1 -C.sub.7)acyloxy; a cyano; an --NR.sub.6 R.sub.7 group; an --NR.sub.3 COR.sub.4 group; an --NR.sub.3 COOR.sub.8 group; an --NR.sub.3 SO.sub.2 R.sub.9 group; an --NR.sub.3 CONR.sub.10 R.sub.12 group; a (C.sub.1 -C.sub.7)acyl group; a (C.sub.1 -C.sub.7)alkoxycarbonyl; a --CONR.sub.10 R.sub.12 group; a --CH.sub.2 OH group; a (C.sub.1 -C.sub.7)alkoxymethyl; a (C.sub.1 -C.sub.7)acyloxymethyl; a (C.sub.1 -C.sub.7)alkylaminocarbonyloxymethyl; a --CH.sub.2 NR.sub.13 R.sub.14 group; a --CH.sub.2 NR.sub.3 COR.sub.4 group; a --CH.sub.2 NR.sub.3 COOR.sub.8 group; a --CH.sub.2 NR.sub.3 SO.sub.2 R.sub.9 group; a --CH.sub.2 NR.sub.3 CONR.sub.10 R.sub.

Abstract: Piperidine derivatives, process for obtaining them and pharmaceutical compositions containing them, of formula ##STR1## used as neurokinin receptor antagonists, which are, in particular, useful for the treatment of all substance P- and neurokinin-dependent pathologies.

Abstract: The invention relates to a diphenylmethylene piperidine derivative of the formula ##STR1## wherein n is 1 or 2; or a pharmaceutically acceptable salt thereof, for use in therapy, in particular for use as a dopamine antagonist for the treatment or prophylaxis of psychotic disorders.

Abstract: Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which A is methylene or O; B is methylene or O; g is 0,1,2,3 or 4; R.sub.1 is an optional substituent; U is an alkylene chain optionally substituted by one or more alkyl; Q represents a divalent group containing nitrogen atoms; and T represents CO.HET, have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behavior, panic attacks, social phobias, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the neuroendocrine system, stress, prostatic hypertrophy, and spasticity.

Abstract: A pharmaceutically-acceptable aqueous solution which is isobaric or hyperbaric, and isotonic, with respect to cerebrospinal fluid (CSF), comprises a 1-alkyl-N-(2,6-dimethylphenyl)-2-piperidinecarboxamide anesthetic agent such as bupivacaine or levobupivacaine and a saccharide. If the amount of the anesthetic agent is no more than 0.75% w/v, a salt or another additional non-saccharide is present. Accordingly, the amount of the saccharide can be kept below that which would provide isotonicity in the absence of the additional non-saccharide.

Abstract: The invention relates to a process for producing a carboxamide of the formula ##STR1## which comprises reacting ##STR2## with an excess of urea in water, wherein the variables in the above formulae are as described herein.