Abstract: The current invention provides methods and pharmaceutical formulations that are useful for inhibiting the loss of bone. These methods and formulations can be used without the associated adverse effects of estrogen therapy, and thus serve as an effective and acceptable treatment for osteoporosis.

Abstract: A method for preparing a new class of protected amino intermediates is provided which utilizes reaction of an imido protected primary amine with a secondary amine. The intermediates thus provided are suitably protected for nucleophilic functionalization on the residue of the primary amine. The desired imido protected amine thus derivatized may be regenerated using acid. Further provided are methods for resolving racemic primary amines. Also provided are .beta.-lactam intermediates protected with the new amino protecting group which are useful in the preparation of .beta.-lactam antibiotics.

Abstract: A method of treating peri-menopasual syndrome comprising administering to a human in need of treatment an effective amount of a compound having the formula ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, --CH.sub.3, ##STR2## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidine and piperidino; or a pharmaceutically acceptable salt of solvate thereof.

Abstract: A process for the preparation of the crystalline monohydrate form of the compound of formula (I) ##STR1## which includes exposing the crystalline dihydrate form of the compound of formula (I) to a temperature of between about 50.degree. and 65.degree. C. and a relative humidity of between about 60 to about 100%.

Abstract: The present invention provides compounds of the formula ##STR1## wherein R is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.3 -C.sub.6 cycloalkyl, or C.sub.1 -C.sub.6 haloalkyl;A and A' are independently hydrogen, C.sub.1 -C.sub.6 alkyl, nitro, amino, a 5-6 membered organic heterocycle containing 1, 2, or 3 hetero atoms selected from nitrogen or sulfur, C.sub.1 -C.sub.6 alkoxy, or phenyl; or A and A' taken together form a group of the formulae ##STR2## wherein X is hydrogen, halo, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkoxycarbonyl, amino, nitro, or carboxy; and Y is nitrogen or carbon; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions and methods of treatment using the above compounds.

Abstract: The invention provides a process for the preparation of the crystalline monohydrate form of the compound of the formula (I) ##STR1## which comprises the step of mixing a form of loracarbef, other than the crystalline monohydrate, such as the ethanol crystal, acetone crystal, crystalline dihydrate, acetonitrile crystal, methanol crystal, propanol crystal, ethyl acetate crystal, methylene chloride crystal, crystalline bis(DMF) and crystalline mono(DMF) form, in water at a temperature between about 30.degree. C. to about 60.degree. C., and preferably at a temperature between 40.degree. C. and 50.degree. C. Conversion may also be accomplished by exposing the loracarbef form to saturated steam at a temperature of between about 90.degree. to about 100.degree. C. Another aspect of the invention is the preparation of the above mentioned crystal forms by slurrying the bis(DMF) solvate form of the compound of formula (I) with the respective solvent.

Abstract: A process for the conversion of a 4-chlorosulfonyl azetidinone (a) to a 3-hydroxy-3-cephem-sulfoxide ester (d) by subjecting an intermediate comprising a tin containing Lewis acid-type Fiedel-Crafts catalyst and 3-exomethylene cepham to ozonolysis.

Abstract: Chiral epoxybutyrates are prepared in high yield from novel dihydro-3R-substituted sulfonyloxy-4R-hydroxy-2-(3H)furanones via based catalyzed alcoholysis. The product chiral epoxy butyrates are useful intermediates for the synthesis of 1-carba-1-dethia cephem antibiotics.

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 and A' together form a group of the formula ##STR3## wherein R.sup.2 is hydrogen or a carboxy-protecting group; X is oxygen; R.sup.1 is hydrogen, hydroxy, halo, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 substituted alkyl, C.sub.1 -C.sub.6 alkylthio, C.sub.1 -C.sub.6 substituted alkylthio, C.sub.7 -C.sub.12 phenylalkyl, C.sub.7 -C.sub.12 substituted phenylalkyl, phenyl or substituted phenyl; a group of the formula--COR.sup.3wherein R.sup.

Abstract: 1-Carba(1-dethia)cephem antibacterial agents possessing a 3-(substituted or unsubstituted)thiazolo group are provided. Further provided is a method for treating bacterial infections in man and other animals and a pharmaceutical formulation utilizing said 1-carba(1-dethia)cephems.

Abstract: .beta.-Hydroxy-.alpha.-amino acids are obtained via serine hydroxymethyltransferase catalyzed condensation of aldehydes with glycine. The predominant product with most aldehydes is the L-erythro diastereomer. For example, succinic semialdehyde methylester is condensed with glycine in the process to provide L-erythro .alpha.-amino hydroxy adipic acid mono methyl ester.

Abstract: Chiral epoxybutyrates are prepared in high yield from novel dihydro-3R-substituted sulfonyloxy-4R-hydroxy-2-(3H)furanones via based catalyzed alcoholysis. The product chiral epoxy butyrates are useful intermediates for the synthesis of 1-carba-1-dethia cephem antibiotics.

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 present invention provides compounds of the formula ##STR1## wherein R.sup.0 is amino or protected amino; A and A' are taken together form a group of the formulae ##STR2## wherein X is hydrogen, halo, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkoxycarbonyl, amino, nitro, carboxy; and Y is nitrogen; or a pharmaceutically acceptable salt thereof.

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 a more desirable protecting group.

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: Disclosed is a process using hydrolysis and hydrogenation for converting enamino .beta.-lactams to their saturated alkyl ester acid salts, key intermediates to 1-carbacephalosporins. Also disclosed are intermediates resulting from the process.

Abstract: Provided is a process for 3' acetylation of 3-hydroxymethylcephalosporins under aqueous conditions.

Abstract: The present invention provides compounds of the formula ##STR1## wherein R is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.3 -C.sub.6 cycloalkyl, or C.sub.1 -C.sub.6 haloalkyl;A and A' are independently hydrogen, C.sub.1 -C.sub.6 alkyl, nitro, amino, a 5-6 membered organic heterocycle containing 1, 2, or 3 hetero atoms selected from nitrogen or sulfur, C.sub.1 -C.sub.6 alkoxy, or phenyl; or A and A' taken together form a group of the formulae ##STR2## wherein X is hydrogen, halo, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkoxycarbonyl, amino, nitro, or carboxy; and Y is nitrogen or carbon; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions and methods or treatment using the above compounds.

Abstract: Chiral epoxybutyrates are prepared in high yield from novel dihydro-3R-substituted sulfonyloxy-4R-hydroxy-2-(3H)furanones via based catalyzed alcoholysis. The product chiral epoxy butyrates are useful intermediates for the synthesis of 1-carba-1-dethia cephem antibiotics.