Abstract: Novel piperzine derivatives substituted on one nitrogen by an aromatic system and on the other nitrogen by (2,5-dioxopyrrolidin)-1-yl) alkanes or (2,6-dioxopiperidin-1-yl) alkanes have been found to exhibit selective .alpha..sub.1A adrenergic activity. The compounds are useful for treatment of disease conditions, such as peripheral vascular disease, congestive heart failure, hypertension and especially benign prostatic hypertrophy.

Abstract: Novel piperzine derivatives substituted on one nitrogen by an aromatic system and on the other nitrogen by (2,5-dioxopyrrolidin)-1-yl) alkanes or (2,6-dioxopiperidin-1-yl) alkanes have been found to exhibit selective .alpha..sub.1A adrenergic activity. The compounds are useful for treatment of disease conditions, such as peripheral vascular disease, congestive heart failure, hypertension and especially benign prostatic hypertrophy.

Abstract: The invention relates to a process for the synthesis of 1-[4-Arylpiperazin-1-yl]-3-[2-oxopyrrolidin/piperidin-1-yl]propanes used as potential therapeutic agents for hypertension, ischemia, cardiovascular and other adrenergic receptors related disorders, having general formula 1 ##STR1## wherein Ar represents a phenyl ring substituted by the groups like halo, alkoxy, alkyl or heteroaryl, n=1 or n=2; a process of preparing said compounds and a method of treating hypertension, ischemia, cardiovascular and other adrenergic receptors related disorders.

Abstract: Compounds represented by the following formula (I) or pharmaceutically acceptable salts thereof and a process for producing the same are disclosed. The compounds have progesterone receptor binding inhibitory activity and, hence, can be used as therapeutic and prophylactic agents for progesterone-related diseases. Specifically, they are useful as carcinostatic agents for breast cancer and ovarian cancer, therapeutic agents for hysteromyoma, endometriosis, meningioma, and myeloma, abortifacients, oral contraceptive pills, and therapeutic and prophylactic agents for osteoporosis and climacteric disturbance. ##STR1## wherein R.sup.1 represents alkyl or aralkyl; R.sup.

Abstract: This invention relates to a series of arylsubstituted piperazines, of Formula I ##STR1## pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention selectively inhibit binding to the .alpha.-1a adrenergic receptor, a receptor which has been implicated in benign prostatic hyperplasia. As such the compounds are potentially useful in the treatment of this and other disease.

Abstract: Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics and anti-pruritic agents are provided.The compound of formula I, having the structure: ##STR1## wherein R.sub.1, R.sub.2 ;X; and ArY, Z and n are as described in the specification.

Abstract: The present invention provides a compound of formula I, or a pharmaceutically acceptable salt thereof: ##STR1## wherein Z, E, Q, T, U, V and L are as defined herein; processes for its preparation and its use in the treatment of conditions for which the administration of an agonist selective for the 5-HT.sub.1D.alpha. receptor subtype is indicated, such as migraine.

Abstract: The invention provides novel benzindole derivatives, processes for producing them, as well as a neuroprotective agent, an agent to prevent or treat diseases involving the degeneration, retraction or death of neurons, and an analgesic, each containing the benzindole derivatives as an active ingredient.

Abstract: The present invention relates to double prodrugs of pharmacologically active glycoprotein IIb/IIIa antagonists of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of lower alkyl of about 2 to about 8 carbon atoms, cycloalkyl, and aralkyl; R is selected from the group consisting of alkoxy, ##STR2## wherein R.sup.50 is H or alkyl; and ##STR3## wherein R.sup.50 is H or alkyl; and pharmaceutically acceptable salts thereof.

Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.

Abstract: The invention relates to compounds of the formula ##STR1## These compounds are neurokinin antagonists. These compounds are useful in the treatment of chronic airway diseases such as asthma.

Abstract: A class of N-substituted piperazine, piperidine and tetrahydropyridine derivatives, linked by a fluoro-substituted alkylene chain to a fused bicyclic heteroaromatic moiety such as indolyl, and further substituted at the 4-position by an optionally substituted alkenyl, alkynyl, aryl-alkyl or heteroaryl-alkyl moiety, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D recptor agonists.

Abstract: The invention relates to compounds of the formula ##STR1## in which: A is a divalent radical selected from:A.sub.1) --O--CO--A.sub.2) --CH.sub.2 --O--CO--A.sub.3) --O--CH.sub.2 --CO--A.sub.4) --O--CH.sub.2 --CH.sub.2 --A.sub.5) --N(R.sub.1)--CO--A.sub.6) --N(R.sub.1)--CO--CO--A.sub.7) --N(R.sub.1)--CH.sub.2 --CH.sub.2 --A.sub.8) --O--CH.sub.2 --in which:R.sub.1 is a hydrogen or a (C.sub.1 -C.sub.4)-alkyl; andAm is a nitrogen-containing heterocycle.

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 lining. 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: The present invention provides compounds of formula (I) and the pharmaceutically acceptable salts thereof, wherein R is C.sub.3 -C.sub.7 cycloalkyl, aryl or C.sub.1 -C.sub.6 alkyl, said C.sub.1 -C.sub.6 alkyl, said C.sub.1 -C.sub.6 alkyl being optionally substituted by fluoro, COOH, --COO(C.sub.1 -C.sub.4 alkyl), C.sub.3 -C.sub.7 cycloalkyl, adamantyl, aryl or het.sup.1, and said C.sub.3 -C.sub.7 cycloalkyl being optionally substituted by 1 or 2 substituents each independently selected from C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.1 -C.sub.4 alkoxy, hydroxy, fluoro, fluoro (C.sub.1 -C.sub.4) alkyl and fluoro (C.sub.1 -C.sub.4) Alkoxy; R.sub.1 is phenyl, naphthyl, thienyl, benzothienyl or indolyl, each optionally substituted by 1 or 2 substituents each independently selected from C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halo and trifluormethyl; R.sup.2 is --CO.sub.2 H, --CONR.sup.3 R.sup.4, --CONR.sup.5 (C.sub.3 -C.sub.7 cycloalkyl), --NR.sup.5 (C.sub.2 -C.sub.5 alkanoyl), --NR.sup.

Abstract: Since a compound represented by general formula (1), its pharmaceutically acceptable salt and a hydrate of the pharmaceutically acceptable salt have high antipsychotic activity, they may be used as an active ingredient for preparation of an antipsychotic. ##STR1## Also provided are an optical resolution method of the above compound and an intermediate for preparation of the compound.

Abstract: The invention relates to compounds of the formula ##STR1## wherein Z, R.sub.c, y, m, u, Ar.sub.2, n, X, R.sub.c', l and Ar.sub.2 are as described herein. These compounds are neurokinin antagonists. These compounds are useful in the treatment of chronic airway diseases such as asthma.

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: A description is given of water-soluble or water-dispersible polyaspartic acid derivatives, their preparation and their use in cosmetology, especially in hair cosmetology.

Abstract: Compounds selected from the group of compounds represented by formula I: ##STR1## where: R.sub.10 is represented by the formula (A), (B), or (C): ##STR2## R.sub.20 is represented by the formula (U), (V), or (W): ##STR3## and the other substituents are as defined in the specification; and their pharmaceutically acceptable salts; are inhibitors of prostaglandin G/H synthase and are anti-inflammatory and analgesic agents.

Abstract: The present invention relates to compounds that can maintain, increase, or restore sensitivity of cells to therapeutic or prophylactic agents. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well-suited for treatment of multi-drug resistant cells, for prevention of the development of multi-drug resistance, and for use in multi-drug resistant cancer therapy.

Abstract: The present invention is directed to a compound of the following formula (I) inclusive of its salt ##STR1## ?wherein R.sup.1 represents either carboxy which may be esterified or amidated carboxy which may be substituted; R.sup.2 represents hydrogen or lower alkyl and may be linked to R.sup.3 or R.sup.4 to form a ring; R.sup.3 and R.sup.4 may be the same or different and each represents hydrogen, lower alkyl which may be substituted, or a sulfide group which may be substituted, and R.sup.3 and R.sup.4 may conjoinedly form a ring; R.sup.5 represents a substituted phenyl group of formula (II) ##STR2## (wherein R.sup.6 represents halogen or alkoxy) or a substituted sulfonyl group of formula (III)--SO.sub.2 --R.sup.7 (III)(wherein R.sup.7 represents either aryl which may be substituted by lower alkyl or amino which may be substituted); n is to 0 or 1! and to a method for producing the same compound, which is useful for the treatment of cysteine protease-associated diseases.

Abstract: Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, is effected b ##STR1## its enantiomers, diastereomers, and pharmaceutically acceptable salts and solvates thereof.

Abstract: The present invention relates to novel compounds of the general formula I ##STR1## which can be used for treating medical disorders resulting from a deficiency in growth hormone.

Abstract: The present invention relates to 1,4-disubstituted piperazines of the general formula ##STR1## wherein X, Y, Z, R.sup.1, R.sup.2 and r are as defined in the detailed part of the present description or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation as well as their use for the treatment of indications caused by or related to the secretion and circulation of insulin antagonizing peptides, e.g. non-insulin-dependent diabetes mellitus (NIDDM) and ageing-associated obesity.

Abstract: Compounds of the formula ##STR1## wherein Q is a hydrazone derivative;R.sup.1 is hydrogen, halogen, alkyl or alkoxy;R.sup.2 is hydrogen, halogen, alkyl, alkoxy, alkenoxy, alkynyloxy, halomethyl, trifluoromethoxy, alkylthio, nitro or cyano; andR.sup.6 is a substituted carboxamide, carbothioamide, phosphonosoamide, or phosphonothioamide,useful as anti-HIV agents.

Abstract: Novel heterocyclic ether compounds of the formula: ##STR1## wherein *, A,B, n, R.sup.1, R.sup.2 and X are specifically defined, or pharmaceutically-acceptable salts or prodrugs thereof, which are useful in selectively activating or inhibiting neurotransmitter release; to therapeutically-effective pharmaceutical compositions of these compounds; and to the use of said compositions to activate or inhibit neurotransmitter release in mammals.

Abstract: Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof wherein: ##STR2## represents an aromatic or alicyclic ring; R.sub.1 and R.sub.2 are the same or different and represent hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, hydroxy, amino, cyano, nitro, trifluoromethyl, trifluoromethoxy, C.sub.1 -C.sub.6 alkoxy, --O.sub.2 CR', --NHCOR', --COR', --SO.sub.m R', where R' is C.sub.1 -C.sub.6 alkyl and wherein m is 0, 1 or 2; orR.sub.1 and R.sub.2 independently represent --CONR'R", or --NR'R" where R' and R" independently represent hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.3 is hydrogen, C.sub.1 -C.sub.6 alkyl, or --COR'" where R'" is C.sub.1 -C.sub.6 alkyl;R.sub.4 is hydrogen or C.sub.1 -C.sub.

Abstract: Diketopiperazines of the formula ##STR1## where one or both of R.sub.1 and R.sub.2, which are different, are chosen from X and a phenyl group substituted by X, C(O)X, OC(O)CH.sub.2 X, OCH.sub.2 CH.sub.2 X, CH.sub.2 X, CONH(CH.sub.2).sub.n X, O(CH.sub.2).sub.n CH(OH)(CH.sub.2).sub.n X ##STR2## and, where appropriate, the other of R.sub.1 and R.sub.2 is a phenyl group optionally substituted by one or more groups selected from halogen, nitro, methoxy, NHC(O)R.sub.12, CO.sub.2 H, O(CH.sub.2).sub.n N(R.sub.12 R.sub.13), C.sub.1 -C.sub.4 alkyl and (CH.sub.2).sub.n C(O)OR.sub.12 ; X is a five- or six-membered heterocyclic ring selected from the group consisting of pyridyl, imidazolyl, furyl, pyrrolyl, pyrrolidinyl, thienyl, piperazinyl, piperidinyl, morpholinyl, quinolyl, isoquinotyl and indolyl, the heteroatom(s) of the said heterocyclic ring, when nitrogen, being optionally substituted by hydrogen, methyl, oxygen, tertiary-butyloxycarbonyl, or SO.sub.

Abstract: This invention is concerned with 2-ureido-benzamide compounds of the formula (1) ##STR1## in which R.sup.1 is H, halogen atom, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy or (C.sub.1 -C.sub.4)dialkylamino and R.sup.2 is H, halogen atom, hydroxy, nitro, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy, (C.sub.3 -C.sub.6) cycloalkylmethoxy, (C.sub.1 -C.sub.4) alkylthio, (C.sub.1 -C.sub.4) alkylsulfinyl, (C.sub.1 -C.sub.4)alkylsulfonyl or ##STR2## wherein j is an integer of from 0 to 2 and R.sup.3 and R.sup.4 are each independently H, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkanoyl, (C.sub.1 -C.sub.4)alkylsulfonyl or (C.sub.1 -C.sub.4)alkylcarbamoyl, NR.sup.3 R.sup.4 can to form a pyrrolidine, piperidine, morpholine, imidazole or pyrazole ring;X is a (C.sub.3 -C.sub.15)alkyl, (C.sub.3 -C.sub.6) cycloalkyl, (C.sub.3 -C.sub.6) cycloalkylmethyl, .omega.-(C.sub.1 -C.sub.4) alkoxy-(C.sub.1 -C.sub.4) alkyl group or ##STR3## wherein k is an integer of from 1 to 4 and R.sup.5 and R.sup.

Abstract: An anticoagulant agent which comprises, as an active ingredient, an aromatic amidine derivative represented by the following general formula (1) or a salt thereof: ##STR1## wherein the group represented by ##STR2## is a group selected from indolyl, benzofuranyl, benzothienyl, benzimidazolyl, benzoxazolyl, benzothiazolyl, naphthyl, tetrahydronaphthyl and indanyl; X is a single bond, an oxygen atom, a sulfur atom or a carbonyl group; and Y is a saturated or unsaturated 5- or 6-membered heterocyclic moiety or cyclic hydrocarbon moiety optionally having a substituent group, an amino group optionally having a substituent group or an aminoalkyl group optionally having a substituent group.The inventive compound has a high anticoagulant capacity based on its excellent FXa inhibition activity.

Abstract: Piperazine derivatives of the formula ##STR1## their esters and salts are useful as modulators of multiple drug resistance.

Abstract: The present invention is directed to piperazine-2,3-dione compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.

Abstract: Piperazine derivatives of formula (A): ##STR1## wherein .sub.-------- denotes an optional bond, provided that either .sub.----.sup.a.sub.---- and .sub.----.sup.c.sub.---- are both bonds and .sub.----.sup.b.sub.---- and .sub.----.sup.d.sub.---- are not bonds, or .sub.----.sup.b.sub.---- and .sub.----.sup.d.sub.---- are both bonds and .sub.----.sup.a.sub.---- and .sub.----.sup.c.sub.---- are not bonds; each of R.sub.14 and R.sub.15 is independently selected from hydrogen and C.sub.1 -C.sub.6 alkyl which is unsubstituted or substituted by an organic functional group; and each of R.sub.1 to R.sub.10, which may be the same or different, is independently hydrogen or an organic functional group; and the pharmaceutically acceptable salts and esters thereof have utility as modulators of multiple drug resistance (MDR).

Abstract: Disclosed are compounds represented by the following chemical formula (I) and pharmacologically acceptable salts thereof which are novel compounds useful as anticancer agents, antiviral agents or antimicrobial agents.

Abstract: A compound of formula (I): ##STR1## In which: R.sub.1 represents linear or branched (C.sub.1 -C.sub.6) alkyl,X represents oxygen or sulfur,R.sub.2 represents optionally substituted alkyl, alkoxy, optionally substituted phenyl, optionally substituted cycloalkyl, 4-(2,3-dithiacyclopent-1-yl)butyl, pyridyl or optionally substituted amino or any one of the groups as defined in the description,R.sub.3 represents hydrogen or cycloalkyl, formyl, optionally substituted phenyl, pyridyl or optionally substituted alkyl,the isomers thereof, the addition salts thereof with a pharmaceutically acceptable acid or base, and medicinal compounds containing them are useful for the treatment of chronic or cellular ischemia.

Abstract: A biphenyl derivative represented by the following formula (I) or a pharmacologically acceptable salt thereof: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.5 are defined in the specification, is clinically useful for treating and ameliorating mental disorders such as cerebrovascular disorder, aggressive behavior due to senile dementia, mental excitation, poriomania, delirium, hallucination, hyperkinesia, schizophrenia, emotional disturbance, depression, neurosis, psychophysiologic disorder and anxiety neurosis. The compounds exhibit dopamine 2 receptor antagonism and/or serotonin 2 receptor antagonism.

Abstract: A class of 1,4-disubstituted piperazine derivatives, further substituted on one of the carbon atoms of the piperazine ring, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, while eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.

Abstract: Compound represented by the structural formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein: a is 0, 1, 2 or3;b, d and e are independently 0, 1 or 2;R is H, C.sub.1-6 alkyl, --OH or C.sub.2 -C.sub.6 hydroxyalkyl;A is an optionally substituted oxime, hydrazone or olefin;X is a bond, --C(O)--, --O--, --NR.sup.6 --, --S(O)e--, --N(R.sup.6)C(O)--, --C(O)N(R.sup.6)-- --OC(O)NR.sup.6 --, --OC(.dbd.S)NR.sup.6 --, --N(R.sup.6)C(.dbd.S)O--, --C(.dbd.NOR.sup.1)--, --S(O).sub.2 N(R.sup.6)--, --N(R.sup.6)S(O).sub.2 --, --N(R.sup.6)C(O)O-- or --OC(O)--;T is H, phthalimidyl, aryl, heterocycloalkyl, heteroaryl, cycloalkyl or bridged cycloalkyl;Q is --SR.sup.6, --N(R.sup.6)(R.sup.7), --OR.sup.6, phenyl, naphthyl or heteroaryl;R.sup.6a, R.sup.7a, R.sup.8a, R.sup.9a, R.sup.6 and R.sup.7 are H, C.sub.1-6 alkyl, C.sub.2 -C.sub.6 hydroxyalkyl, C.sub.1 -C.sub.6 alkoxy-C.sub.1 -C.sub.6 alkyl, phenyl or benzyl; or R.sup.6 and R.sup.7, together with the nitrogen to which they are attached, form a ring;R.sup.

Abstract: A method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells is disclosed. The method comprises the administration of a compound of Formula 1.0: ##STR1## to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being. Novel compounds of formulas 5.0, 5.1 and 5.2, wherein R is --C(R.sup.20)(R.sup.21)(R.sup.46), and 5.3, 5.3A and 5.3B, wherein R is --N(R.sup.25)(R.sup.48), are disclosed. Also disclosed are processes for making 3-substituted compounds of Formulas 5.0, 5.1, 5.2 and 5.3. Further disclosed are novel compounds which are intermediates in the process for making 3-substituted compounds of Formulas 5.0, 5.1, 5.2 and 5.3.

Abstract: A compound represented by formula (I) and a salt thereof, and a hydrate and solvate thereof: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 represent independently, for example, hydrogen atom, hydroxyl group, or C.sub.1-3 alkoxy group; R.sub.4 represents, for example, C.sub.1-7 alkyl group or C.sub.3-7 cycloalkyl group; R.sub.5 and R.sub.6 represent independently, for example, hydrogen atom or C.sub.1-3 alkyl group; Y represents C.sub.1-3 alkyl group, a heterocyclic group containing 1 to 4 nitrogen atoms and 5 or 6 ring-membered atoms, or C.sub.6-10 aryl group; k represents an integer of 1 to 3; and l represents an integer of 2 to 4. These urea compounds have excellent inhibitory activities against ACAT and are useful as active ingredients of medicines for preventive and/or therapeutic treatment of hyperlipemia and atherosclerosis.

Abstract: The invention relates to compounds of the formulas ##STR1## wherein Z, R.sub.c, y, x, l.sub.1, l.sub.2, l.sub.3, u, R.sub.4, R.sub.c', n, R.sub.1, R.sub.2, and R.sub.3, are as described herein. These compounds are neurokinin antagonists. These compounds are useful in the treatment of chronic airway diseases such as asthma.

Abstract: The invention relates to compounds of the formula ##STR1## These compounds are neurokinin antagonists. These compounds are useful in the treatment of chronic airway diseases such as asthma.

Abstract: This invention relates to novel compounds which inhibit platelet aggregation, pharmaceutical compositions containing the compounds, and methods of using the compounds.

Abstract: A sulfonamide derivatives of formula (I) ##STR1## a non-toxic salts, an acid addition salts or a solvates thereof which has an inhibitory effect on elastase.

Abstract: The invention relates to compounds of the formula ##STR1## wherein Z, R.sub.c, y, m, u, Ar.sub.2, n, X, R.sub.c', I and Ar.sub.2 are as described herein. These compounds are neurokinin antagonists. These compounds are useful in the treatment of chronic airway diseases such as asthma.

Abstract: Disclosed are compounds of the formula: ##STR1## wherein: A represents arylalkyl, aryl or heteroaryl; X is nitrogen or CH; and R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent organic or inorganic substituents;and the pharmaceutically acceptable salts thereof;useful for treating disorders of the central nervous system.

Abstract: The present invention relates to a mercaptopyrrolidinyl derivative of the following formula ##STR1## suitable for the preparation of carbapenem compounds.

Abstract: Compounds of the formula X--Y--R, or the pharmaceutically acceptable salts and esters thereof, wherein X is ##STR1## Y is --SO.sub.2 --, --(CH.sub.2).sub.p -- or --CO--(CH.sub.2).sub.p --; R is unsubstituted or substituted phenyl where said substitutents are one or more of R.sup.5, R.sup.6 or R.sup.7 ; R.sup.1 is hydrogen, cyano, phenyl, --CONHR.sup.2, --CONR.sup.2 R.sup.2, --(CH.sub.2).sub.m --OR.sup.2, --(CH.sub.2).sub.p --S(O).sub.r --R.sup.2, --(CH.sub.2).sub.m --CO.sub.2 R.sup.2, --(CH.sub.2).sub.m --N.sub.3, --(CH.sub.2).sub.m --NH.sub.2 or --(CH.sub.2).sub.m --NR.sup.2 R.sup.2 ; R.sup.2 is hydrogen, C.sub.3-8 cycloalkyl or C.sub.1-5 alkyl; R.sup.5 and R.sup.6 are each independently selected from hydrogen, C.sub.1-5 alkoxy, halogen or --(CH.sub.2).sub.n --N(R.sup.2)--C(O)--R.sup.18 ; R.sup.7 is hydrogen or ##STR2## R.sup.11 is selected from hydrogen, C.sub.1-5 alkyl-carbonyl, --Z--R.sup.13, ##STR3## or substituted C.sub.

Abstract: Selected amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.