Abstract: The most thermodynamically stable crystalline form of the benzoic acid salt of 4″-deoxy-4″-epi-methylamino avermectin B1a/B1b as the hemihydrate is obtained by crystallization from organic solvents containing a controlled amount of water.

Abstract: A bioerodible controlled release dosage form is disclosed comprising a polymer formed by condensing beneficial agents having a hydroxyl functionality of two or more with diketene acetals or divinyl ethers which delivers beneficial agents to a biological environment of use. A statistically significant portion of the beneficial agent is covalently bonded within the polymer matrix.

Abstract: Novel avermectin and milbemycin derivatives are disclosed, where the C-24 and C-25 carbon atoms are substituted by hydrogen, alkyl, alkenyl, substituted alkyl or substituted alkenyl groups. These compounds can be further substituted at the 4"-, 5-, 13-, and 23-positions. The new C-24 and C-25 substituted avermect prepared by cleavage of known and suitably protected avermectin and milbemycin compounds. The new compounds are potent anti-parasitic agents, in particular, the compounds are anthelmintic, insecticidal and acaricidal agents.

Abstract: There are disclosed certain novel compounds identified as benzo-fused lactams which 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 increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. The compounds are prepared by substitution of an amino-lactam with a substituted amide function. Growth promoting compositions containing such bezno-fused lactams as the active ingredient thereof are also disclosed.

Abstract: .beta.- or .gamma.-Ketoesters and .beta.- or .gamma.-ketoamides are asymmetrically reduced with a Ru(II)-BINAP derived catalyst at about 40.degree. C. and about 50N/mm.sup.2 of hydrogen in the presence of a strong acid.

Abstract: The present invention comprises analogs of the CAAX motif of the protein Ras that is modified by farnesylation in vivo. These CAAX analogs inhibit the farnesylation of Ras. Furthermore, these CAAX analogues differ from those previously described as inhibitors of Ras farnesyl transferase in that they do not have a thiol moiety. The lack of the thiol offers unique advantages in terms of improved pharmacokinetic behavior in animals, prevention of thiol-dependent chemical reactions, such as rapid autoxidation and disulfide formation with endogenous thiols, and reduced systemic toxicity. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.

Abstract: This invention relates to a the use of new oxodioxolenylmethyl carbamates to produce bioreversible neutral prodrugs from primary and secondary amines.

Abstract: This invention consists of an ophthalmic dispensing tip formed by injection molding, which has a one-piece molded tip to be used with a mating cap, the tip having an internally molded breakaway barrier membrane inside the flow channel, and the cap having a shaped stud fitting inside the tip, so that the final clockwise half-turn of the cap pushes the stud against the barrier and displaces it, thereby creating a restricted path through which the contents are dispensed.

Abstract: Stereospecific (S)-6-bromo-2-tetraol is a key intermediate in the chemical synthesis of the chiral drug candidate, MK499, a ventricular arrythmias suppressant. The yeast strain Trichosporon capitatum (MY 1890) was employed for the bioconversion of 6-bromo-2-tetralone to the corresponding alcohol.

Abstract: A compound of the formula I is disclosed. ##STR1## R.sup.13 represents hydrogen, NH.sub.2, C1-4 alkyl, C1-4 alkylamino or di(C1-4) alkylamino-;Y represents CH or N;Y" represents (a) CR.sup.y' R.sup.z' with R.sup.y' and R.sup.z' hydrogen, C1-6 alkyl, C.sub.3-8 cycloalkyl or C.sub.1-6 alkyl substituted with C.sub.3-8 cycloalkyl, or (b) N substituted with OR.sup.14 with R.sup.14 representing H, C.sub.1-4 alkyl or C.sub.1-4 alkyl substituted with COOH.Ar represents: ##STR2## One of R.sup.1 and R.sup.2 independently represent H, W as defined below or one of the groups (a) through (d) below, and the other represents H or W. Pharmaceutical compositions and methods of use are also included.

Abstract: A class of substituted imidazole, triazole and tetrazole derivatives are selective agonists of 5-HT.sub.1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a selective agonist of these receptors is indicated.

Abstract: A carbapenem antibiotic of the formula I ##STR1## is disclosed. The variable X.sup..crclbar. represents a counterion. Pharmaceutical compositions and methods of use are also disclosed.

Abstract: Compounds of formula (I), and salts and prodrugs thereof ##STR1## wherein: R.sup.1 is H, certain optionally substituted C.sub.1.6 alkyl, or C.sub.3-7 cycloalkyl;R.sup.2 is (CH.sub.2).sub.q -tetrazolyl optionally substituted in the tetrazole ring by C.sub.1-4 alkyl, (CH.sub.2).sub.q -imidazolyl (where q is 0, 1, 2 or 3), CONHSO.sub.2 R.sup.9, SO.sub.2 NHCOR.sup.9 (where R.sup.9 is C.sub.1-6 alkyl, optionally substituted aryl or trifluoromethyl). SO.sub.2 NHR.sup.10 (where R.sup.10 is a nitrogen containing heterocycle), cyclopropyl or (CH.sub.2), CO.sub.2 H, where n is 1 or 2;R.sup.3 is C.sub.1-6 alkyl, halo or NR.sup.6 R.sup.7 ;R.sup.4 is C.sub.1-7 straight or branched chain alkyl; andx is 0, 1, 2 or 3;are CCK and/or gastrin receptor antagonists. They and compositions thereof are useful in therapy.

Abstract: Disclosed is a process for removing by-product phosphorus-containing (PO.sub.x) materials, alendronate and alendronate byproducts from crude mother liquors in an omega amino-1-hydroxy-C.sub.2 -C.sub.6 alkylidene-1,1-bisphosphonic acid synthesis process, e.g. alendronate sodium. Calcium chloride is added first to the crude mother liquors, then calcium oxide to precipitate the PO.sub.x materials, then neutralized to about pH 7 to complete precipitation. Substantially all of the alendronate sodium active ingredient is removed from the precipitate. Following filtration, the PO.sub.x filtercake can then be disposed of by incineration, landfilling or reclamation of usable phosphorus as fertilizer. The remaining filtrate can then be further treated in an environmentally acceptable manner by wastewater treatment or recycling to the process.

Abstract: Substituted heterocycles attached through a methylene bridge to novel substituted phenyl derivatives of the Formula I are useful as angiotensin II antagonists. ##STR1## wherein the substituents are as defined in the claims.

Abstract: This invention relates to compounds represented by formula I: ##STR1## which are agonists of angiotensin II. The invention is also concerned with the use of aforementioned agonists in the treatment of states meditated by angiotensin.

Abstract: The present invention is directed to a process of making 2-aryl carbapenems of formula 1 from a compound of formula A.

Abstract: Novel substituted quinazolinones of the formula (I) are useful as angiotensin II antagonists.

Abstract: Compounds of the general structural formula: ##STR1## or a pharmaceutically acceptable salt, hydrate or crystal form thereof, wherein;X is O or CH.sub.2R.sup.1 is H if R.sup.2 is not H or if R.sup.2 is H then R.sup.1 is ##STR2## R.sup.2 is --H if R.sup.1 is not H or if R.sup.1 is H then R.sup.2 is; ##STR3## and R.sup.3 is ##STR4## are Class HI antiarrhythmic agents.

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 treatment of cancer.