Abstract:
The present invention is directed to a novel method for preparing a synthetic intermediates for treprostinil. Also described are methods of preparing treprostinil comprising utilizing novel intermediates described herein as well as novel intermediates useful for synthesis prostacyclin derivatives, such as treprostinil.
Abstract:
A locking mechanism (100) and method of fixation, such as the fixation of a fixation device (104) like a bone screw and of a rod (106) to the spine. The locking mechanism (100) includes a body (102), an insert (108, 308), a rod seat (110, 310) and a set screw. The body (102) includes a bottom portion (114) configured to receive the fixation device (104) and the insert (108, 308) but prevents the insert (108, 308) and fixation device (104) from passing therethrough once the insert (108, 308) and fixation device (104) are engaged. The body (102) further includes a side portion (120) configured to receive the rod (106). Between the rod (106) and the insert (108, 308) is a rod seat (110, 310).
Abstract:
A compound of the Formula (I): ##STR1## or pharmaceutically-suitable salts or prodrug forms thereof, wherein: n is 0-1;m is 0;p is 0-1;R.sup.1 is --CO.sub.2 H;R.sup.2 is selected from the group consisting of H, --OH, and --NH.sub.2 ;R.sup.3 is H;R.sup.4 is --C(O)NHR.sup.8 ;R.sup.5 is --NHC(R.sup.6)NH.sub.2R.sup.6 is selected from the group consisting of .dbd.NH, .dbd.NOH, .dbd.NCN, .dbd.O, and .dbd.S; andR.sup.8 is selected from the group consisting of C.sub.1 -C.sub.4 linear or branched alkyl substituted with 0-3 halogens on each carbon.
Abstract:
A method of treating allergy with substituted heterocyclic amines is disclosed wherein the active agents are expressed generally by the formula which includes certain known and certain novel compounds: ##STR1## wherein p is zero, one or two; m is one to six inclusive; A is selected from hydrogen, hydroxy or cyano; d is zero or one; Q is --CH--, --CH.sub.2 -- or ##STR2## n is zero or one and when Q is --CH-- and n is one, a double bond is formed with one of the adjacent carbons but not both at the same time, and when n and d are zero at the same time, a double bond is formed between the .alpha. carbon and a carbon of the central heterocyclic amine ring; Ar, D and R are selected from phenyl, substituted phenyl, pyridinyl, thienyl, furanyl or naphthyl and in addition, R may have the values benzyl, substituted benzyl, cycloalkyl or loweralkyl and D may additionally have the values: 2H-1-benzopyran-2-one, 4-oxo-4H-1-benzopyran-2-carboxylic acid loweralkyl ester, 2,3-dihydro-4H-1-benzopyran-4-one or 1,4-benzodioxan-loweralkyl-2-yl, and the pharmaceutically acceptable salts thereof.
Abstract:
An ophthalmic aspirator-irrigator system for use during cataract surgery is disclosed. The system frees both hands of the surgeon for the surgical tasks and leaves the automatic operation of the system to a single control input operated by a foot pedal. The pedal controls both the aspiration and ejection functions as well as their respective speeds. The ophthalmic aspirator-irrigator system essentially comprises a hand-held device, a control box operable by the foot pedal and a power cord connecting the device with the box. A source of fluid is connected via a tube to the device to effect the irrigation function. The control box includes a power source and a circuit coupled to the source and via the cord to the device. Preferably, the circuit includes a bridge output network controlled by a linear motion slide type potentiometer controlled by the foot pedal. The circuit further includes dual DC amplifiers and a pulse-width modulated gate circuit to operate the device bidirectionally with a smooth, continuous and variable speed. The foot pedal has two zero control positions: in its off, non-depressed position and in its off position about midway through the pedal's downward travel. A vacuum limiting valve assembly permits the system readily to be adapted to posterior capsule polishing following the break-up and removal of the cortex.
Abstract:
Cis and trans-3-aryloxy-4-hydroxypyrrolidines and derivatives thereof having the formula: ##STR1## are disclosed wherein R.sub.1 is hydrogen, loweralkyl, benzyloxycarbonyl and N-loweralkylcarbamoyl; R.sub.2 is hydrogen, lower alkyl, cycloalkyl, phenylalkyl, benzyloxycarbonyl, carbamoyl, N-loweralkylcarbamoyl, N-diloweralkylcarbamoyl and parafluorobenzoyl-lower-alkyl; Ar is phenyl, substituted phenyl, 1-naphthyl, 2-naphthyl, 1-indenyl and 2-indenyl and pharmaceutically acceptable acid addition and quaternary salts thereof. The compounds have antidepressant, antihypertensive and antiarrythmic activity in animals.
Abstract:
Novel 2-amino-3-(alkylthiobenzoyl)phenylacetic acids, esters and metal salts have the formula: ##STR1## wherein R is hydrogen or lower alkyl, R.sup.1 is hydrogen, lower alkyl or pharmaceutically acceptable metal cation, R.sup.2 is hydrogen, halogen, lower alkyl or lower alkoxy, Am is primary amino (--NH.sub.2), methylamino or dimethylamino. The compounds have anti-inflammatory activity; have effective analgesic activity, and inhibit blood platelet aggregation.
Abstract:
Novel 2-amino-3-benzoyl-phenylacetamides are provided having the formula: ##STR1## wherein R represents hydrogen or lower alkyl, R.sup.1 and R.sup.2 represent hydrogen, lower alkyl, cycloalkyl, phenyl and phenyl substituted by lower alkyl, lower alkoxy, halogen, nitro and trifluoromethyl, and R.sup.1 and R.sup.2 when taken together with the adjacent nitrogen may form a heterocyclic residue; X represents hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; Y represents hydrogen, lower alkyl, lower alkoxy, halogen, trifluoromethyl, lower alkylthio, lower alkyloxythio or lower alkyldioxythio; Am is primary amino (--NH.sub.2), methylamino or dimethylamino, and n is 1 to 3 inclusive. The compounds exhibit anti-inflammatory, antipyretic, anti-blood platelet aggregation and analgetic pharmacological activities.
Abstract:
Trans isomers of 1-substituted-3-arylthio-4-hydroxypyrrolidines and derivatives thereof having the formula: ##STR1## are disclosed wherein R.sub.1 is hydrogen, lower-alkyl, --C(O)NH-lower-alkyl and --C(O)-NH-phenyl; R.sub.2 is lower-alkyl, cycloalkyl and phenylalkyl; Ar is phenyl and substituted phenyl and the pharmaceutically acceptable addition salts thereof. The compounds have antidepressant activity in animals.
Abstract:
This present invention relates to an improved process to prepare prostacyclin derivatives. One embodiment provides for an improved process to convert benzindene triol to treprostinil via salts of treprostinil and to purify treprostinil.