Abstract: Described herein are compounds and pharmaceutical compositions which inhibit N-acylethanolamine acid amidase (NAAA). Described herein are methods for synthesizing the compounds set forth herein and methods for formulating these compounds as pharmaceutical compositions which include these compounds. Also described herein are methods of inhibiting NAAA in order to sustain the levels of palmitoylethanolamide (PEA) and other N-acylethanolamines (NAE) that are substrates for NAAA, in conditions characterized by reduced concentrations of NAE. Also, described here are methods of treating and ameliorating pain, inflammation, inflammatory diseases, and other disorders in which modulation of fatty acid ethanolamides is clinically or therapeutically relevant or in which decreased levels of NAE are associated with the disorder.

Abstract: A process for making (2S,5R)-5-ethynyl-1-{N-(4-methyl-1-(4-carboxy-pyridin-2-yl)piperidin-4-yl)glycyl}pyrrolidine-2-carbonitrile and salts thereof, and intermediates used in the process are disclosed.

Abstract: Provided is a compound having a D-amino acid oxidase (DAAO) inhibitory action, and useful as for example, a prophylaxis and/or therapeutic agent for schizophrenia or neuropathic pain. The present inventors have studied a compound that inhibits DAAO, and confirm that a dihydroxy aromatic heterocyclic compound has a DAAO inhibitory action, and completed the present invention. That is, the dihydroxy aromatic heterocyclic compound of the present invention has a good DAAO inhibitory action, and can be used as a prophylaxis and/or therapeutic agent for, for example, schizophrenia or neuropathic pain.

Abstract: Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of diseases and disorder such as learning, cognitive activities, and analgesia, particularly in alleviating and/or reducing neuropathic pain. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.

Abstract: Substituted 2-(azetidin-2-on-1-yl)alkoxyalkylalkanoic acids and 2-(azetidin-2-on-1-yl)arylalkylalkanoic acids, and analogs and derivatives thereof are described. Methods for using the described compounds, and pharmaceutical compositions thereof, to treat disease states responsive to antagonism of one or more vasopressin receptors are also described.

Abstract: The invention relates to compounds of formula (I): wherein R1, R2, R3, R4, R5, and R6 as defined herein. The invention also relates to pharmaceutical compositions and methods of treating bacterial infections using compounds of formula (I).

Abstract: The invention relates to compounds of formula (I): wherein R1, R2, R3, R4, R5, and R6 as defined herein. The invention also relates to pharmaceutical compositions and methods of treating bacterial infections using compounds of formula (I).

Abstract: Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of diseases and disorder such as learning, cognitive activities, and analgesia, particularly in alleviating and/or reducing neuropathic pain. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.

Abstract: Substituted 2-(azetidin-2-on-1-yl)alkoxyalkylalkanoic acids and 2-(azetidin-2-on-1-yl)arylalkylalkanoic acids, and analogs and derivatives thereof are described. Methods for using the described compounds, and pharmaceutical compositions thereof, to treat disease states responsive to antagonism of one or more vasopressin receptors are also described.

Abstract: The invention relates to compounds of formula (I): wherein R1, R2, R3, R4, R5, and R6 as defined herein. The invention also relates to pharmaceutical compositions and methods of treating bacterial infections using compounds of formula (I).

Abstract: The invention relates particularly to 2-alkoxy-3,4,5-trihydroxy-alkylamides, preparation thereof, compositions containing them and use thereof as a medicament, particularly as anti-cancer agents.

Abstract: The present invention relates generally to amide group containing pharmaceutical agents, and in particular, to amide containing heterobicyclic metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of heterobicyclic MMP-13 inhibiting and MMP-3 inhibiting compounds, that exhibit an increased potency in relation to currently known MMP-13 and MMP-3 inhibitors.

Abstract: Compounds are provided which have the structure Wherein A, B, C, D, m, Y, Ra, Rc, Rd, and Rd? are as described herein, and which are useful as inhibitors of tryptase, thrombin, trypsin, Factor Xa, Factor VIIa, Factor XIa, and urokinase-type plasminogen activator and may be employed in preventing and/or treating asthma, chronic asthma, allergic rhinitis, and thrombotic disorders.

Abstract: Novel 2-(azetidin-2-on-1-yl)alkanedioic acid derivatives and 2-(azetidin-2-on-1-yl)alkoxyalkanoic acid derivatives are described for use in the treatment of disease states responsive to antagonism of the vasopressin V1a receptor

Abstract: The present invention provides methods for identifying (3-amino-2-oxo-azetidin-1-yl) acetic acid derivatives with anti-PBP2a activity. The method involves the selection of RNA biocatalysts that promote the formation of (3-amino-2-oxo-azetidin-1-yl) acetic acid derivatives with anti-PBP2a activity from component reactants. The invention also provides novel (3-amino-2-oxo-azetidin-1-yl) acetic acid derivatives with anti-PBP2a activity identified by these methods. The invention also provides RNA biocatalysts that are capable of catalyzing the formation of (3-amino-2-oxo-azetidin-1-yl) acetic acid derivatives from component reactants.

Abstract: Novel 2-(azetidin-2-on-1-yl)alkanedioic acid derivatives and 2-(azetidin-2-on-1-yl)alkoxyalkanoic acid derivatives are described for use in the treatment of disease states responsive to antagonism of the vasopressin V1a receptor.

Abstract: The invention provides a compound of Formula (Ia), or a pharmaceutically acceptable salt pro-drug or solvate thereof. The invention also provides a process for the preparation of a compound of Formula (Ia), pharmaceutical compositions of a compound of Formula (Ia) and methods for the treatment or prevention of cancer comprising administering an effective amount of a compound of Formula (Ia).

Abstract: The present discovery consists in new thiazole-substituted ?-lactams of general formula (I), as well as the method for their preparation. R1, R2, R3, R4, R5, R6, R7, and R8 are, independently from each other, a hydrogen atom, a halogen, a hydroxy, amino, nitro, or thiol group, an optionally substituted alkyl, heteroalkyl, aryl, aralkyl, cycloalkyl, cycloaralkyl, heterocycloalkyl, heteroaralkyl, or heteroaryl rest.

Abstract: A novel process for the asymmetric synthesis of an amino-pyrrolidinone of the type shown below from appropriate pyrrolidinones is described.

Abstract: The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, which are for treating a patient suffering from, or subject to, physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.

Abstract: A sulphostin analogue represented by the general formula, wherein n is an integer of from 0 to 3, provided that a case where n is 2 and steric configurations of C* and P* are S and R, respectively, is excluded, or a pharmaceutically acceptable salt thereof.

Abstract: A process for preparing N-acyl, N-sulfonyl and N-phosphoryl substituted isoserine esters in which a metal alkoxide is reacted with a &bgr;-lactam.

Abstract: The present invention relates to compounds of the general formula I wherein A is a group of the formula and Z is an O or S atom, to the further processing thereof to form novel sec-amidoalkylcarbonic acid derivatives and to those sec-amidoalkylcarbonic acid derivatives.

Abstract: The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, for treating a patient suffering from, or subject to, a physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.

Abstract: Organometallic iron complexes containing one or more basic structural components characterizing a molecule with antimalarial properties such as quinine, chloroquinine or mepacrine, as well as one or more iron atoms are described. The complexes of the invention are more particularly characterized in that they contain one or more ferrocene groups.

Abstract: A process for preparing a .beta.-lactam halide compound represented by the formula (2) characterized by halogenating the allenyl group of an allenyl .beta.-lactam compound represented by the formula (1) with a cupric halide and a metal halide to obtain the .beta.-lactam halide compound ##STR1## wherein R.sup.1 is a hydrogen atom or amino or protected amino, R.sup.2 is a hydrogen atom, halogen atom, lower alkoxyl, lower acyl, or lower alkyl having a hydroxyl group or protected hydroxyl group as a substituent, R.sup.3 is a hydrogen atom or carboxylic acid protecting group, and R.sup.4 is a hydrocarbon group which may have a substituent, or the group --S--S(O)n-Ar, n being 0 to 2, Ar being aryl which may have a substituent ##STR2## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same as defined above, X and Y are each halogen atom.

Abstract: This invention provides a process for preparing azetidinones useful as intermediates in the synthesis of penems and as hypocholesterolemic agents, particularly for azetidinones substituted in the C-3 and C-4 positions and optionally substituted at the ring nitrogen, comprising reacting a .beta.-(substituted-amino)amide, a .beta.-(substituted-amino)acid ester, or a .beta.-(substituted-amino)thiolcarbonic acid ester with a silylating agent and a cyclizing agent.

Abstract: The present invention provides for new 5-amidomethyl, .alpha.,.beta.-saturated and--unsaturated butyrolactone antibacterial agents of formula I ##STR1## characterized by 3-aryl substituents that include, for example, indolinyl and phenyl substituted with zero (0) to two(2) halogen atoms and substituted in the para position with, e.g., piperazinyl, thiomorpholinyl (and corresponding sulfoxide and sulfone), thiazolidinyl (and sulfoxide and sulfone), morpholinyl, azetidinyl, pyrrolidinyl, piperidinyl, pyrrolyl, azepinyl, troponyl, 3,7-diazabicyclo?3.3.0!octan-3-yl, bridged thiazinyl or bridged oxazinyl moieties. In those cases where a ring nitrogen is present, then this is substituted to form an amide, formamide, sulfonamide, urethane, or alkylated with a wide variety of moieties.

Abstract: This invention provides an improved process for producing azetidinones. More particularly, this invention provides the steps of producing an azetidinone represented by the formula I ##STR1## from a carboxylic acid R.sup.2 --D--CH.sub.2 COOH, an aldehyde R.sup.1 --A--CHO and an amine RNH.sub.2, by the steps of: (a) converting a carboxylic acid to the corresponding acid chloride; (b) deprotonating a chiral oxazolidinone and treating the resulting anion with the product of step (a); (c) enolizing the product of step (b) and condensing with an imine; and (d) cyclizing the product of step (c). Steps (c) and (d) of this process are as shown in the following reaction scheme.

Abstract: .beta.-lactam compounds which are reacted with a metal alkoxide for preparing N-acyl, N-sulfonyl and phosphoryl substituted isoserine esters.

Abstract: Pyrimidinyloxy- and triazinyloxy- and pyrimidinylthio- and triazinylthio-butyric acid derivatives of formula I ##STR1## wherein Q is ##STR2## A is hydroxy or a group ##STR3## and the other substituents are as described in patent claim 1, and salts of compounds of formula I, have herbicidal action and are suitable as active ingredients in weed control compositions.

Abstract: Azetidinones of the formula I ##STR1## in which, for example, R.sup.1 is an alkyl or alkenyl radical, R.sup.2 and R.sup.3 are hydrogen or an alkyl or alkenyl radical, Z is hydrogen or (pseudo)halogen, A.sup.1, A.sup.2 and A.sup.3 are a ring system, and M is a spacer group, can be added to liquid-crystal mixtures. Even when admixed in small amounts, they cause considerable twist in the cholesteric and smectic C* phase, which can compensate the pitch of another dope or produce a short S.sub.C * pitch.

Abstract: Provided is a process for diastereoselectively preparing compounds of the formula ##STR1## which includes the step of subjecting a compound of the formula ##STR2## to a salt whose anion is a nucleophilic base whose conjugate acid has a pKa in the range of between about -7 to about 14, or a silylated derivative of the salt; whereinR.sub.1 is said nucleophile;R is hydrogen, or protected amino,R.sub.2 is R.sub.4 as defined herein below;R.sub.3 is a leaving group; andR.sub.4 is hydrogen, C.sub.1 -C.sub.6 alkyl, or a group of the formula--CH.sub.2 --CH.sub.2 --R.sub.6whereinR.sub.6 is 2-furyl, naphthyl, phenyl, phenyl substituted with 1, 2 or 3 substituents selected from C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, nitro, halo, carboxy and amido; orR.sub.6 is a group of the formula--COOR.sub.7or--COSR.sub.7in whichR.sub.7 is selected from C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, benzyl, phenyl, or benzyl or phenyl substituted with 1, 2 or 3 substituents selected from C.sub.

Abstract: The invention provides compounds of the formula ##STR1## wherein R* is a group of the formula ##STR2## wherein R and R.sup.0 are individually C.sub.1 -C.sub.6 alkyl groups or together form a ring consisting of the nitrogen atom to which they are attached and two to seven carbon atoms, said ring optionally substituted by one or more C.sub.1 -C.sub.6 alkyl and/or C.sub.1 -C.sub.6 substituted alkyl groups;Q and Q' are individually hydrogen, C.sub.1 -C.sub.6 alkyl, or when taken together form a divalent radical of the formula --CH.dbd.CH--CH.dbd.CH--;A is C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 substituted alkyl, --S--(C.sub.1 -C.sub.6 alkyl)CO.sub.2 R", or --CH.sub.2 (C.sub.1 -C.sub.6 alkyl) CO.sub.2 R" wherein R"is hydrogen or a carboxy-protecting group;A' is hydrogen, an amide-protecting group, or a group of the formula --CH.sub.2 CO.sub.2 R".

Abstract: New substituted azetidinones of the general formula (A') which have been found to be potent elastase inhibitors and thereby useful anti-inflammatory and antidegenerative agents are described.

Abstract: Disclosed herein are processes for preparing a compound of the formula ##STR1## in which a novel compound of the formula ##STR2## is reacted with a beta lactam of the formula ##STR3## by treatment with a base, wherein the symbols are as defined in the specification.

Abstract: The present invention provides a process for protecting an amino group in a compound exposed to nucleophilic reaction conditions in which the imido group used for protection is reacted with a secondary amine to form an acyl group which protects the amino group during exposure to the nucleophilic reaction conditions, after which the acylamino group may be reacted with an acid to reform the imido group so that the compound may then undergo non-nucleophilic manipulations. Also provided is a resolution method in which diasteriometric compounds having the acylamino group as described above are reacted with acid, and as these diasteriomers react at different rates to form the imido group, the reaction may be monitored so as to isolate the desired product at the appropriate point to maximize optical purity.

Abstract: N-tetrazolyl beta-lactams of the Formula: ##STR1## and the pharmaceutically acceptable salts thereof wherein R.sup.2 is hydrogen, alkyl having 1 to 6 carbon atoms or carboalkoxy having 2 to 7 carbon atoms; andZ is ##STR2## and W is ##STR3## thus forming a zwitterion, or Z is ##STR4## wherein R.sup.1 is benzyl, phenyloxymethyl or ##STR5## wherein Y is alkoxy or substituted alkoxy having 1 to 6 carbon atoms wherein the substituent on the alkoxy group is --COOH; andW is ##STR6## wherein R.sup.3 is H, M or --CH.sub.2 COOM, wherein M is a pharmaceutically acceptable cation are disclosed. The compounds are useful as antibiotics.

Abstract: A process for preparing 3-4-cis-.beta.,.beta.-(4)-substituted and 3-4-trans,.beta.,.alpha.-(4)-substituted azetidinones is provided. Also provided are novel 4,4-disubstituted azetidinones.

Abstract: Novel intermediates for preparing 2-oxo-1-[[(substituted sulfonyl)-amino]carbonyl]azetidines are disclosed. These intermediates have the formula ##STR1## wherein Prot is as defined herein.

Abstract: Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof and possessing antibacterial activiy, and intermediates to compounds of formula I having the formula ##STR2##

Abstract: Benzopyran derivatives of the general formula I ##STR1## are disclosed. The compounds are therapeutic active compounds.

Abstract: This invention presents novel 2-azetidinone compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and are hydrogen (C.sub.1 -C.sub.12) alkyl, (C.sub.2 -C.sub.8) alkenyl, (C.sub.2 -C.sub.8) alkynyl, (C.sub.3 -C.sub.10) cycloalkyl, phenyl optionally substituted with from one to 3 substituents selected from the group consisting of halogen, hydroxy, amino, nitro, (C.sub.1 -C.sub.4)alkyl, and (C.sub.1 -C.sub.4)alkoxy, benzyl optionally subsituted with from one to 3 substituents selected from the group consisting of halogen, hydroxy, amino, nitro, (C.sub.1 -C.sub.4)alkyl, and (C.sub.1 -C.sub.4)alkoxy, --CH.sub.2 --O--CO--CH.sub.2 --NHR.sub.4, --CH.sub.2 --O--CO.sub.2 --R.sub.5, --CH.sub.2 F, or --CHF.sub.2 ; wherein R.sub.4 is hydrogen, --CHO or --CO--O--C(CH.sub.3).sub.3 ; wherein R.sub.5 is --(C.sub.1 -C.sub.8)alkyl, --(CH.sub.2) .sub.2 NH--CO--O--C(CH.sub.3).sub.3, --(CH.sub.2).sub.2 N(CH.sub.3)--CO--O--C(CH.sub.3).sub.3, --(CH.sub.2).sub.2 OC(O)NH.sub.2, --(CH .sub.2).sub.

Abstract: This invention presents novel 2-azetidinone compounds of the formula ##STR1## wherein R.sub.10 and R.sub.15 are the same or different and are (a) hydrogen, (b) (C.sub.1 -C.sub.12) alkyl, (c) (C.sub.2 -C.sub.8) alkenyl, (d) (C.sub.2 -C.sub.8) alkynyl, (e) --CH.sub.2 OCOCH.sub.2 NHR.sub.4, (f) --CH.sub.2 OCO.sub.2 R.sub.30, (g) --CH.sub.2 F, or (h) --CHF.sub.2 ; wherein R.sub.4 is hydrogen or --COH; wherein R.sub.30 is (C.sub.1 -C.sub.8)alkyl; wherein R.sub.20 is an acyl group derived from a carboxylic acid; wherein A is oxygen or sulfur; and wherein R.sub.70 is (a) hydrogen, (b) (C.sub.1 -C.sub.8) alkyl, (c) phenyl, (d) --OH, or (e) --SH; where each member of b or c may optionally be substituted by 1 to 2 substituents selected from the group consisting of halogen, hydroxy, and amino.These compounds are useful as antibacterial agents to eradicate or control susceptible microbes. Intermediates and processes for making these compounds are also disclosed.

Abstract: This invention presents novel 2-azetidinone compounds of the formula ##STR1## wherein R.sub.80 is --CO.sub.2 R.sub.5 or --CONR.sub.6 R.sub.7 ; wherein R.sub.5 is hydrogen or (C.sub.1 -C.sub.4) alkyl; and wherein R.sub.6 and R.sub.7 are the same or different and are hydrogen, (C.sub.1 -C.sub.4 alkyl), or --OH with the proviso that when R.sub.6 is --OH, R.sub.7 is other than --OH. These compounds are useful as antibacterial agents to eradicate or control susceptible microbes. Intermediates and processes for making these compounds are also disclosed.

Abstract: A process for preparing 3-4-cis-.beta.,.beta.-(4)-substituted and 3-4-trans,.beta.,.alpha.- (4)-substituted azetidinones is provided. Also provided are novel 4,4-disubstituted azetidinones.

Abstract: A method for preparing 2-amino-.beta.-lactams which are substituted by readily-removed protecting groups is provided. According to this invention, an acyl-2-amino-.beta.-lactam is further acylated with a different acyl group and is subsequently treated with base to provide a protected 2-amino .beta.-lactam with allyloxycarbonyl, t-butoxycarbonyl, naphthyloxycarbonyl, trichloroethyloxycarbonyl, p-nitrobenzyloxycarbonyl, benzhydryloxycarbonyl, p-methoxybenzyloxycarbonyl, or o-nitrobenzyloxycarbonyl.

Abstract: An improved process for making compounds having the formula ##STR1## includes subjecting an intermediate of the formula ##STR2## to hydrogenolysis in the presence of a ketonic solvent so as to simultaneously remove both Z-protecting groups from compound II while selectively reprotecting the --A.sub.1 --NH.sub.

Abstract: This invention presents novel 2-azetidinone compounds which are useful as antibacterial agents to eradicate or control susceptible microbes of the formula ##STR1## wherein R.sub.401 and R.sub.402 are the same or different and are (a) hydrogen, (b) (C.sub.1 -C.sub.12) alkyl (c) (C.sub.2 -C.sub.8) alkenyl, (d) (C.sub.2 -C.sub.8) alkynyl, (e) (C.sub.3 -C.sub.10) cycloalkyl, (f) phenyl optionally substituted with from one to 3 substituents selected from the group consisting of halogen, hydroxy, amino, nitro, (C.sub.1 -C.sub.4) alkyl, and (C.sub.1 -C.sub.4) alkoxy, (g) benzyl optionally substituted with from one to 3 substituents selected from the group consisting of halogen, hydroxy, amino, nitro, (C.sub.1 -C.sub.4) alkyl, and (C.sub.1 -C.sub.4) alkoxy, (h) --CH.sub.2 --O--CO--CH.sub.2 --NHR.sub.420, (i) --CH.sub.2 --O--CO.sub.2 --R.sub.430, (j) --CH.sub.2 F, or (k) --CHF.sub.2 ; wherein R.sub.420 is (a) hydrogen, (b) --COH, or (c) --CO--O--C(CH.sub.3).sub.3 ; wherein R.sub.430 is (C.sub.1 -C.sub.8) alkyl, --(CH.