Abstract: There are disclosed preparation and compounds of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are hydrogen or lower alkyl or taken together are a --CH.sub.2 -- group to form a cyclopropane ring.X is ##STR2## wherein R.sup.5, R.sup.6, R.sup.7, and R.sup.8 are hydrogen or alkyl,p and q are independently either 0 or 1;R.sup.3 is alkyl, alkenyl, cycloalkyl, alkoxy, thiopyridyl, adamantyl, --NR.sup.9 R.sup.10 or --Ar--NR.sup.9 R.sup.10 whereinR.sup.9 and R.sup.10 are hydrogen or alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, adamantyl, aryl, benzyl, diphenylmethyl, norbornyl, or taken together with the nitrogen to form 4 to 8 atom heterocyclic group, ##STR3## optionally substituted with alkyl groups; Ar is aromaticR.sup.4 is hydrogen or methyl;Z is --O--, --NH--, --N(lower alkyl), --S--, --SO--, --SO.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, CO, CO.sub.2, O.sub.2 C, --N.dbd.N--, --CH.dbd.N--, or --N.dbd.CH--,and n and m are 0, 1 or 2.

Abstract: A pneumatic apparatus for withdrawing goods from defective blister packages on a blister packaging machine and comprising a pair of spaced-apart and laterally shiftable vacuum heads reciprocally mounted above the carrier strip between the detection station and the sealing station of the blister packaging machine so that when one head is in vertical registration with the carrier strip the other head is laterally offset from the carrier strip. Each vacuum head comprises a plurality of suction elements depending from the bottom thereof which are adapted to selectively engage a predetermined plurality of goods on the carrier strip.

Abstract: The present Invention includes synthetic steps and intermediates involved in the following reaction scheme a of converting compounds of Formula (II) to the diarylmethanes of Formula (I): ##STR1## wherein: Y is oxygen or sulfur;A, B, C, D, and E are carbon or 1, 2 or 3 of A, B, C, D, and E are independently nitrogen, and the others are carbon; andwhereinR.sup.1 through R.sup.10 are selected independently from the group consisting of: hydrogen, hydroxy, alkyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.3 -C.sub.8 cycloalkyl alkyl, alkenyl, hydroxy alkyl, alkoxy alkyl, perhalo-alkyl, amino, nitro, nitrile, halo, carboxyl, sulfonyl, acyl, formyl, carbamoyl, trifluoromethyl, aminomethyl, azido, amido, hydrazino, aryl, aryloxy, heteroaryl, or aryl or heteroaryl, mono, di, or tri substituted with one or more hydrogen, hydroxy, alkyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.3 -C.sub.

Abstract: The present invention relates to an aerosol dispensing apparatus, more particularly to aerosol dispensing valves incorporating a controlled metered dispensing function wherein the metering chamber holding the next aerosolized dose is in fluidic communication with the reservoir allowing homogenous mixing of the next aerosolized dose to be dispensed.

Abstract: A breath-actuated dry powder medicament inhalator device having a housing and a conduit mounted within the housing defining an air passageway therethrough having an aperture in the sidewall thereof. A blister-type strip of sealed containers arranged in a matrix of rows and columns wherein the columns extend generally diagonally to the longitudinal axis of the strip is secured in a two-piece cage adapted for being rotatably mounted around the conduit of the inhalator device. Advancement means are provided for rotatably moving the two-piece cage and blister strip contained thereby in a generally helical pathway relative to the conduit so as to successively advance each of the sealed containers of the blister strip into registration with the conduit aperture.

Abstract: The present invention comprises a bi-layer, pharmaceutical tablet having one layer formulated for the immediate release (IR) of ranitidine and a second layer formulated for sustained release (SR) of ranitidine with the ratio of ranitidine in the IR layer to that in the SR in the range of from about 30:70 to about 60:40.

Abstract: Novel piperidinyl intermediates as set forth below wherein R, R.sup.1 and Ar are as set forth in the specification and W is either hydrogen or benzyloxycarbonyl. The intermediates are useful in the preparation of N-phenyl-N-(4-piperidinyl) amides having potent analgesic activity.

Abstract: CCK modulators, e.g. agonists or antagonists, of the following formula (I): ##STR1## or a base-addtion salt thereof.

Abstract: A method of making a stabilized aerosol drug formulation is disclosed, along with the formulations so produced and metered drug inhalers containing the same. The method comprises combining a solid particulate drug composition with a fluoropolymer in a liquid fluorocarbon aerosol propellant to form a stable suspension. Further stabilization can be achieved by cooling the suspension for a time and to a temperature sufficient to adsorb the fluoropolymer to the solid particulate drug composition in the liquid fluorocarbon aerosol propellant. Preferred propellants for carrying out the invention are 1,1,1,2-tetrafluoroethane, heptafluoropropane, and mixtures thereof, and preferred fluoropolymers for carrying out the invention are fluoropolyethers.

Abstract: The present invention relates to the synthesis of water soluble, camptothecin derivatives of formula (I), ##STR1## wherein: n represents the integer 1 or 2;R.sup.1 represents independently, hydrogen, lower alkyl, (C.sub.3-7)cycloalkyl, (C.sub.3-7)cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, lower alkoxy lower alkyl; andR.sup.2 represents hydrogen andthe pharmaceutically acceptable salts thereof.

Abstract: Synthesis of the triol of the following formula (I) from an alcohol of the formula (IV): ##STR1## via steps including protecting and then cyanating the alcohol to yield a cyanide, isomerization of the double bond, hydrolysis followed by reduction of the cyanide back to an alcohol and cis-dihydroxylation of the double bond.

Abstract: Aminobutanoic acids of the following formula (I): ##STR1## where R.sup.1 -R.sup.5 are a variety of substituents, novel intermediates, a pharmaceutical composition for treating inflammatory diseases, demyelinating diseases, and tumor metastasis, methods for such treatment and processes for preparing compounds of formula (I).

Abstract: A bottle having an inserted tube in its neck to effectively reduce its interior volume and allow a large surface area for the bottle exterior, e.g. for supporting a large label or to allow oversized print, with a relatively small interior volume, e.g. to prevent abrasions caused by the interior contents moving excessively against each other.

Abstract: The present invention relates to certain substituted tetracyclic fused quinoline derivatives of formula (I): ##STR1## wherein: R.sup.1 is hydrogen, hydroxy, fluoro, chloro, bromo, iodo, methoxy or amino;R.sup.2 is hydrogen, hydroxy, methoxy or amino;R.sup.3 is hydrogen, hydroxy, methoxy, methoxymethoxy, amino, --OCONH.sub.2, [2(5H)-3,4-dihydro-3-oxyfuranone], 2-hydroxyethoxy, 2-aminoethoxy, 3-hydroxypropoxy or 3-aminopropoxy; or taken together with R.sup.2 or R.sup.4, methylenedioxy or ethylenedioxy;R.sup.4 is hydrogen, hydroxy or amino;Z is --CH.sub.2 --, --O-- or --NH--; anda) X.sup.1 is hydrogen;X.sup.2 is hydrogen, hydroxy, fluoro, chloro, bromo, iodo or methoxy; andX.sup.3 is hydrogen or hydroxy; orb) X.sup.2 taken together with X.sup.3 is methylenedioxy or ethylenedioxy, and X.sup.1 is hydrogenor a pharmaceutically acceptable salt thereof provided that:i) at least one of R.sup.1 through R.sup.4 is other than hydrogen.

Abstract: The present invention relates to certain substituted 17 .beta.-substituted carbonyl-6-azaandrost-4-en-3-ones of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 arei) independently hydrogen or lower alkyl and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single or a double bond, orii) taken together are a --CH.sub.2 -- group to form a cyclopropane ring, and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single bond;X is ##STR2## wherein R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are independently hydrogen or lower alkyl,p and q are independently either 0 or 1;R.sup.3 is lower alkyl, lower alkenyl, lower cycloalkyl, lower alkoxy, thiopyridyl, adamantyl, --NR.sup.9 R.sup.10 or --Ar--NR.sup.9 R.sup.10whereinR.sup.9 and R.sup.

Abstract: The present invention comprises a method for measuring the amount, i.e., mass, of a volatile liquid which comprises passing the mass over a heat loss measuring device, calculating the amount of heat loss accompanying the vaporization of the mass and correlating the heat loss to measurement of heat loss of known liquid aerosol mass made with the same device.

Abstract: Compounds of the following formula (I): ##STR1## where R.sup.1 and R.sup.2 are alkyl or cycloalkyl, which may be substituted, R.sup.4 is aryl such as phenyl which may be substituted, L is a direct bond or an oxygen containing linking group, R is a hydrogen, alkyloxy, alkyl, halogen or haloalkyl and Het is a pyridinyl or pyridazinyl group. The compounds can be used antihypertensives or myocardial relaxants. Also part of the invention are pharmaceutical compositions, intermediates and methods of synthesis.

Abstract: Compounds are described of the formula ##STR1## wherein: R.sup.1 is C.sub.3-6 alkyl or C.sub.1-3 alkylthioC.sub.1-3 alkyl;R.sup.2 is an optionally substituted C.sub.1-6 alkyl or C.sub.1-6 alkoxy group, aryl, heteroaryl, arylC.sub.1-4 alkyl, heteroarylC.sub.1-4 alkyl or a side-chain of a natural .alpha.-amino acid;R.sup.3 is hydrogen, C.sub.1-6 alkyl, CHR.sup.4 COR.sup.5 (where R.sup.4 is a side-chain of a natural .alpha.-amino acid and R.sup.5 is hydroxyl, C.sub.1-6 alkoxy or NHR.sup.6 where R.sup.6 represents a hydrogen atom or a C.sub.1-6 alkyl group) or a group (CH.sub.2).sub.n X (where n is 1 to 6 and X is hydroxyl, C.sub.1-4 alkoxy, heteroaryl or a group NR.sup.7 R.sup.8 where R.sup.7 and R.sup.8 are each hydrogen or C.sub.1-6 alkyl or the group NR.sup.7 R.sup.

Abstract: This invention relates to the new process for preparing the 1R-cis isomer of carbovir, (1R-cis)-amino-1,9-dihydro-9-[4-(hydroxymethyl)-2-cyclopenten-1-yl]-6H-pur in-6-one, an antiviral agent and intermediates of the formula (Vlb) use in that process ##STR1## wherein X is chloro, bromo or iodo and R is (C.sub.1-6) alkyl.

Abstract: A breath actuated dry powder medicament inhalator has a primary air passageway therethrough defining a venturi in the medial portion thereof. A secondary air passageway is provided which includes a compound deaggregating swirl chamber and is fluidly connected to the venturi of the primary air passageway. A dry powder compound storage chamber and cooperatively associated metering plate act to introduce a predetermined amount of compound into the swirl chamber upon actuation of the metering plate. The primary air passageway is configured within the inhalator apparatus so as to create an optimized air flow trajectory through the mouth of the user to minimize dry powder compound impingement upon the outside radius of the throat.