Abstract: Selected heterocyclecarbonyl 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.

Abstract: This invention relates to compounds of formula (I): ##STR1## which are useful as modulators of D.sub.3 receptors, in particular in the treatment of psychoses.

Abstract: The present invention provides medicinal compounds that are characterized by a cyclic moiety (A) linked through a carboxamido group (more specifically, a carbamate group or a urea group) to another cyclic moiety (B) which is in turn linked to another, N-substituted carboxamido group. These compounds can be used an anti-inflammatory and immunosuppressive agents, as demonstrated by their inhibition of the production of IL-1.beta. in vitro and TNF.alpha. in vivo.

Abstract: The invention relates to the use of carbocyclically and heterocycally fused dihydroyridines as cerebroprotective agents, as agents for treating chronic inflammatory processes and as agents for inhabiting blood clotting, and also relates to new compounds of formula Ie ##STR1##

Abstract: The present invention is directed to novel ketomethylene group-containing inhibitors of cysteine or serine proteases. Methods for the use of the protease inhibitors are also described.

Abstract: The invention relates to sulphonamide compounds of formula (I) or a salt thereof having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of CNS disorders, wherein: Ar is an optionally substituted mono- or bicyclic aromatic or heteroaromatic ring; Ar' is an optionally substituted mono- or bicyclic aromatic or heteroaromatic ring; R.sup.1 is C.sub.1-6 alkyl or together with the group R.sup.3 form a 5-8 membered ring containing one or two heteroatoms optionally substituted by C.sub.1-6 alkyl; R.sup.2 is hydrogen or C.sub.1-6 alkyl; R.sup.3 is hydrogen, C.sub.1-6 alkyl or together with the group R.sup.1 form a 5-8 membered ring containing one or two heteroatoms optionally substituted by C.sub.1-6 alkyl; R.sup.4 is hydrogen or C.sub.1-6 alkyl; R.sup.5 and R.sup.6 are independently hydrogen or C.sub.1-6 alkyl; p is 1, 2 or 3; q is 1 to 3; and r is 1 or 2.

Abstract: Disclosed are compounds of formula (I) or the pharmaceutically acceptable salts thereof wherein: ##STR1## G represents a group of the formula (a), (b) or (c) where R.sub.a and R.sub.b represent hydrogen, or organic or inorganic substituents; A is an optionally substituted alkylene; R.sub.1, R.sub.2, R.sub.3, R.sub.4 represent organic or inorganic substituents; R.sub.5 is hydrogen or lower alkyl; R.sub.6 and R.sub.7 independently represent hydrogen, lower alkyl; or together form a ring of 5-8 members; Z is nitrogen or carbon; and W is optionally susbtituted aryl or heteroaryl. Compounds of the present invention demonstrate high affinity and selectivity in binding to the D.sub.3 receptor subtype.

Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.

Abstract: The present invention relates to certain substituted oxadiazole, thiadiazole, and triazole peptoids that are useful as inhibitors of serine proteases, in particular human neutrophil elastase. Serine protease inhibitors of the invention are useful in the treatment of, for example, adult respiratory distress syndrome, septic shock, and myocardial ischemia-reperfusion injury.

Abstract: Compounds of the invention have the general structure ##STR1## X, Y or Z are, respectively independently, H, F or an isotope thereof, Br or an isotope thereof, I or an isotope thereof, At or an isotope thereof, (R.sub.1)W or (R.sub.2)V and R is --(R.sub.1)W, when W is H or F or an isotope thereof, R.sub.1 is linear or branched alkyl of 1-4 carbon atoms, R.sub.2 is vinyl, V is I or an isotope thereof and at least one of X, Y or Z is not H. The compounds of the invention bind to PK receptors.

Abstract: A method for binding albumin by contacting an aqueous liquid containing an albumin with an albumin-binding compound is selected from albumin-binding compounds containing the scaffold --CO--NH--C(.dbd.C--)--CO--, and conjugates that are capable of binding albumin and exhibiting the scaffold --CO--NH--C(.dbd.C--)--CO--.

Abstract: There are described according to the invention compounds of formula (I) (relative stereochemistry indicated), wherein R.sub.1, R.sub.2, R.sub.3 and X are as defined in the specification, together with processes for preparing them, compositions containing them and their use as pharmaceuticals. Compounds of formula (I) are indicated inter alia for the treatment of chronic bronchitis.

Abstract: A compound of formula (I) or a salt thereof, or a solvate thereof, wherein either (i) Ra represents a group R.sub.5 which is hydrogen, alkyl or optionally substituted aryl and R.sub.5 represents a moiety of formula (a); wherein X represents a hydroxy or an alkoxy group wherein the alkyl group may be substituted or unsubstituted or X represents a group NR.sub.s R.sub.t wherein R.sub.s and R.sub.t each independently represent hydrogen, alkyl, substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted arylalkyl, an optionally substituted heterocyclic group or an optionally substituted heterocyclylalkyl group, or R.sub.s and R.sub.t together may form a heterocyclic group; R.sub.1 represents an alkyl or a substituted or unsubstituted aryl group; and R.sub.2, R.sub.3 and R.sub.4 each independently represent hydrogen, alkyl, aryl or substituted aryl or (ii) R.sub.a represents a moiety of the above defined formula (a) and R.sub.b represents the above defined R.sub.5 ; R.

Abstract: Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof, wherein: R.sub.1, R.sub.2, R.sub.3, R.sub.4 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, R.sub.2, R.sub.3, R.sub.4 independently represent --CONR'.sub.m, or --NR'.sub.m where m is 0, 1 or 2 and R' is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.5 is hydrogen or C.sub.1 -C.sub.6 alkyl; andR represents an aminoalkyl group,which compounds are useful in the treatment of affective disorders such as schizophrenia, depression, Alzheimer's disease, movement disorders such as Parkinsonism and dystonia, and other disorders which respond to dopaminergic blockade such as substance abuse and obsessive compulsive disorders.

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: Selected heterocyclecarbonyl 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.

Abstract: Described herein is a retroviral protease inhibiting compound of the formula: ##STR1## or a pharmaceutically acceptable salt, prodrug or ester thereof.

Abstract: The invention relates to novel N-(3,5-bis-trifluoromethyl-benzoyl)-2-benzyl-4-(azanaphthoyl-amino)-piperi dines of the formula ##STR1## wherein X and Y are each independently of the other N and/or CH and the ring A is unsubstituted or mono- or poly-substituted by substituents selected from the group consisting of lower alkyl, lower alkoxy, halogen, nitro and trifluoromethyl; and the salts thereof, to the use thereof, to processes for the preparation thereof and to pharmaceutical compositions comprising a compound according to the invention or a pharmaceutically acceptable salt thereof.

Abstract: Compounds of the formula I ##STR1## are suitable for the preparation of pharmaceuticals for the prophylaxis and therapy of disorders involving increased activity of matrix-degrading metalloproteinases.

Abstract: This invention relates to the field of pharmaceutical and organic chemistry and provides benzothiophene compounds, intermediates, formulations, and methods.

Abstract: The present invention provides novel 1,2,3,4-tetrahydroisoquinoline carbamate and thiocarbamate derivatives represented by Formula I ##STR1## wherein: X.sub.1 and X.sub.2 are the same or different from each other and independently represent a a member selected from the group consisting of hydrogen, alkyl, alkoxy, thioalkoxy, halogen, hydroxy, nitro and trifluorocarbon;Y is a member selected from the group consisting of oxygen and sulfur;R.sub.1 is a member selected from the group consisting of hydrogen, alkyl, arylalkyl, and CONHR' where R' is selected from the group consisting of hydrogen, alkyl, arylalkyl and aryl;R.sub.2 and R.sub.3 are the same or different from each other and independently represent a member selected from the group consisting of hydrogen, alkyl, arylalkyl, and cycloalkyl, or R.sub.2 and R.sub.3 may form a 5 to 7-membered ring together with the nitrogen atom to which they are bonded;R.sub.

Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.

Abstract: The present invention is directed to novel benzothiazo and related heterocyclic group-containing inhibitors of cysteine or serine proteases. Methods for using the same are also described.

Abstract: Substituted condensation products of N-benzyl-3-indenylacetamides with heterocyclic aldehydes are useful for inducing or promoting apotosis and for arresting uncontrolled neoplastic cell proliferation, and are specifically useful in the arresting and treatment of neoplasias, including precancerous and cancerous lesions.

Abstract: N-heterocyclic moiety containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Abstract: This invention relates to novel statone antiviral analogs, to the processes and intermediates useful for their preparation and to their use as antiviral agents.

Abstract: Compounds of formula (I) are growth hormone releasing peptide mimetics which are useful for the treatment and prevention of osteoporosis.

Abstract: Disclosed are compounds of the formula ##STR1## or the pharmaceutically acceptable salts thereof wherein: G represents a group of the formula ##STR2## where R.sub.a and R.sub.b represent hydrogen, or organic or inorganic substituents;A is an optionally substituted alkylene;R.sub.1, R.sub.2, R.sub.3, R.sub.4 represent organic or inorganic substituents;R.sub.5 is hydrogen or lower alkyl;R.sub.6 and R.sub.7 independently represent hydrogen, lower alkyl; or together form a ring of 5-8 members;Z is nitrogen or carbon; andW is optionally substituted aryl or heteroaryl. Compounds of the present invention demonstrate high affinity and selectivity in binding to the D.sub.3 receptor subtype.

Abstract: Disclosed are compounds of the formula: or the pharmaceutically acceptable acid addition salts thereof, wherein:R.sub.1, R.sub.2, R.sub.3, R.sub.4 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, R.sub.2, R.sub.3, R.sub.4 independently represent --CONR'R", or --NR'R" where R' and R" independently represent hydrogen or C.sub.1 -C.sub.6 alkyl;R5 is hydrogen or C.sub.1 -C.sub.6 alkyl; andR represents an aminoalkyl group, which compounds are useful in the treatment of affective disorders such as schizophrenia, depression, Alzheimer's disease, movement disorders such as Parkinsonism and dystonia, and other disorders which respond to dopaminergic blockade such as substance abuse and obsessive compulsive disorders.

Abstract: Novel peptide derivatives, compositions containing them, and their use for treating medical disorders resulting from a deficiency in growth hormone are disclosed. The peptides have the formula (I): ##STR1## wherein a, b, A, R.sup.1, L.sup.1, D, R.sup.3, R.sup.4, R.sup.2, L.sup.2, E and G are as defined in the specification. These peptides exhibit improved resistance to proteolytic degradation, and hence, improved bioavailability.

Abstract: The present invention relates to novel N-substituted amino alcohols, amino acids and acid derivatives thereof in which a substituted alkyl chain forms part of the N-substituent 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.

Abstract: 1,8,8-Trifluoro-5,6,7,8-tetrahydroisoquinoline derivatives, and their use in liquid-crystalline mixtures 1,8,8-Trifluoro-5,6,7,8-tetrahydroisoquinoline derivatives of the formula (I)R.sup.1 (--M.sup.1).sub.a (--A.sup.1 --M.sup.2).sub.b (--A.sup.2 --M.sup.3).sub.c --B(--M.sup.4 --A.sup.3).sub.d (--M.sup.5 --A.sup.4).sub.e (--M.sup.6).sub.f --R.sup.2 (I)in which the symbols and indices have the following meanings:the group B is ##STR1## R.sup.1 and R.sup.2 are, for example, alkyl radicals having 1 to 20 carbon atoms;M.sup.1, M.sup.2, M.sup.3, M.sup.4, M.sup.5 and M.sup.6 are, for example, --O--, --CO--O--, --O--CO-- or a single bond;A.sup.1, A.sup.2, A.sup.3 and A.sup.4 are, for example, 1,4-phenylene, pyrimidine-2,5-diyl or trans-1,4-cyclohexylene, anda, b, c, d, e and f are zero or one, with the proviso that the sum of b, c, d and e is 0, 1 or 2.

Abstract: Guanidine derivatives of formula I ##STR1## wherein R.sup.8 represents hydrogen, halogen, alkyl C1 to 6, nitro, trifluoromethyl, thioalkyl C1 to 6, hydroxy, alkoxy C1 to 6, or a group selected from --NR.sup.4 R.sup.5, --O(CH.sub.2).sub.p Q, --(CH.sub.2).sub.m OQ, --(CH.sub.2).sub.m NR.sup.1 R.sup.2, --O(CH.sub.2).sub.m NR.sup.1 R.sup.2, --NHCO(CH.sub.2).sub.m NH(CH.sub.2).sub.n Q or --(CH.sub.2).sub.p CONR.sup.1 R.sup.2, or R.sup.8 represents the group A--CO--B; R.sup.9 represents hydrogen, halogen, alkyl C1 to 6, nitro or trifluoromethyl;and R.sup.1, R.sup.2, R.sup.4, R.sup.5, n, m, p, Q, A, B, and W are as defined in the specification, are described together with processes for their manufacture and compositions containing them. Compounds of formula I are useful in therapy.

Abstract: Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof, wherein: R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 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, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 independently represent --CONR'R", or --NR'R" where R' and R" independently represent hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.10 is hydrogen or C.sub.1 -C.sub.

Abstract: This invention is directed to novel imidazole and imidazoline derivatives which are selective agonists for cloned human .alpha..sub.2 adrenergic receptors. This invention is also related to the use of these compounds for the treatment of any disease where modulation of the .alpha..sub.2 receptors may be useful. The invention further provides for a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

Abstract: This invention relates to a compound of the Formula IX--C(O)--Y--G--R I(wherein X, Y, G and R have the values defined in the description), or a pharmaceutically acceptable salt thereof, processes and intermediates for the preparation of such a compound or salt, pharmaceutical compositions comprising such a compound or salt and methods of their use as thrombin inhibitors, coagulation inhibitors and agents for the treatment of thromboembolic disorders.

Abstract: HIV protease inhibitors, obtainable by chemical synthesis, block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and possibly other anti-viral agents as ingredients, are thus suitable for the treatment of the HIV virus known to cause AIDS.

Abstract: Compound of general formula I ##STR1## wherein A is a benzo or thieno group;R.sub.1 is (C.sub.4-6)cycloalkyl, (C.sub.4-6)cycloalkyl-(C.sub.1-5)alkyl or ##STR2## R.sup.2, m, R.sup.3, R.sup.4, R and u are defined as in the specification, and pharmaceutical preparations containing this compound and the new pharmaceutical uses thereof.

Abstract: A process for producing 2-?3(S)-amino-2-(R)-hydroxyl-4-phenyl butyl!-N-tert,butyl decahydro-(4aS,8aS)-isoquinoline-e(S)-carboxamide of the formula (I) via 3(S)-?lower alkoxy carbonyl amino, phenoxy carbonyl amino or benzyl oxycarbonyl amino!-2-hydroxy-4-phenyl butyric acid and process for producing said acid.

Abstract: The instant invention is concerned with acetylphenols which are useful as antiobesity and antidiabetic compounds. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering or modulating triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility or for treating atherosclerosis are also disclosed.

Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.

Abstract: The present invention is directed to (D)-amino acid containing inhibitors of cysteine or serine proteases. Methods for the use of the protease inhibitors are also described.

Abstract: Disclosed are a phenol compound represented by the formula (1): ##STR1## wherein R.sup.0 represents H, alkyl or alkyloxy; R.sup.1 represents alkyl; R.sup.2 represents alkyl or alkyloxy; OR.sup.3 represents OH; R.sup.4 represents H, lower alkyl or acyl, each of the above substituents may be substituted; W represents O, S or NR.sup.7 ; where R.sup.7 represents H, alkyl, aryl, OH or alkyloxy, a group of the formula (2): ##STR2## represents an amino which may be mono- or di-substituted or heterocyclic group containing N atom,or a pharmaceutically acceptable salt thereof, and a process for preparing the same.

Abstract: (Z)-1?1-(4-Methoxybenzylidene)-1,2,3,4,5,6,7,8-octahydro-isoquinolin-2-yl!a lkanones of the formula ##STR1## wherein R is lower alkanoyl, can be produced under specific reaction conditions in a one-pot process in an advantageous manner by a Bischler-Napieralski cyclization of N-(2-cyclohex-1-enylethyl)-2-(4-methoxyphenyl)-acetamide and subsequent lower-alkanoylation of the resulting 1-(4-methoxybenzyl)-3,4,5,6,7,8-hexahydro-isoquinoline of the formula ##STR2## under an inert gas atmosphere and, if desired converted to dextomethorphan in a known manner.

Abstract: Novel cholecystokinin antagonists useful as agents in the treatment of obesity, hypersecretion of gastric acid in the gut, gastrin-dependent tumors, or as antipsychotics are disclosed. Further, the compounds are antianxiety agents and antiulcer agents. They are agents useful for preventing the response to the withdrawal from chronic treatment with use of nicotine, diazepam, alcohol, cocaine, coffee, or opioids. The compounds of the invention are also useful in treating and/or preventing panic. Also disclosed are pharmaceutical compositions and methods of treatment using the antagonists as well as processes for preparing them and novel intermediates useful in their preparation. An additional feature of the invention is the use of the subject compounds in diagnostic compositions.

Abstract: A process for the manufacture of the .alpha.,.alpha.'-diaminoalcohol of formula ##STR1## is via N-protected L-phenylalanine lower alkyl esters, corresponding N-protected .alpha.-amino-.alpha.'-haloketones, and .alpha.-amino-.alpha.'-haloalcohols.

Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1.beta. converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against interleukin-1 mediated diseases, including inflammatory diseases, autoimmune diseases and neurodegenerative diseases. This invention also relates to methods for inhibiting ICE activity and methods for treating interleukin-1 mediated diseases using the compounds and compositions of this invention.

Abstract: A compound of formula I ##STR1## wherein A denotes a benzo, indolo or thieno group;R.sup.1 denotes thienyl or the group ##STR2## wherein R.sup.7, R.sup.8 and R.sup.9 independently of one another may represent methyl, ethyl, propyl, phenyl or benzyl, while not more than 2 of the substituents can simultaneously represent phenyl or benzyl;R.sup.2, m, R.sup.3 and R.sup.4 are defined as in the specification, as well as pharmaceutical preparations containing this compound and the new pharmaceutical uses thereof.

Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.

Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.