Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R.sup.1 is a substituted alkylene; C.sub.3 -C.sub.7 cycloalkyl optionally substituted with HO; C.sub.3 -C.sub.6 alkenyl optionally substituted with aryl; C.sub.5 -C.sub.7 cycloalkenyl; or C.sub.3 -C.sub.6 alkynyl; R.sup.2 is H; halo; F.sub.3 C; NC; R.sup.8 R.sup.9 NOC; a substituted alkylene; R.sup.8 R.sup.9 NO.sub.2 S; R.sup.10 S(O).sub.m ; R.sup.12 CON(R.sup.11); R.sup.10 SO.sub.2 N(R.sup.11); R.sup.8 R.sup.9 NOCN(R.sup.11); R.sup.10 O.sub.2 CN(R.sup.11); R.sup.13 (CH.sub.2).sub.n CH.dbd.CH; or R.sup.7 O are selective 5-HT.sub.1 -like receptor agonists useful in the treatment of migraine, cluster headache, chronic paroxysmal hemicrania and headache associated with vascular disorders.

Abstract: Certain 4-aminopyrrolo[2,3-d]pyrimidine compounds, and their pharmaceutically-acceptable salts, are inhibitors of tyrosine kinase enzymes, and are useful for immunoregulation and for the treatment of cancer, angiogenesis and atherosclerosis.

Abstract: Compounds of the formula ##STR1## wherein Z is ##STR2## R.sub.1 is ##STR3## X is O, NH, or S; A, B, D, E, and F are each independently C, N, O, or S; wherein the remaining variables are defined in the specification, and the pharmaceutically acceptable salts thereof. These compounds are useful psychotherapeutics and are potent serotonin (5-HT.sub.1) agonists and may be used in the treatment of depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, migraine, pain, chronic paroxysmal hemicrania and headache associated with vascular disorders, and other disorders arising from deficient serotonergic neurotransmission. The compounds can also be used as centrally acting antihypertensives and vasodilators.

Abstract: Process for the preparation of a dialkyl trans-piperidine-2,5-dicarboxylate from a corresponding dialkyl cis-piperidine-2,5-dicarboxylate via a trans-substituted pyridine derivative of the formula ##STR1## wherein R is a (C.sub.1 -C.sub.3)alkyl group.

Abstract: Compound of formula (I) or salts thereof wherein R.sup.1 is hydrogen, methoxy or formamido; R.sup.2 is an acyl group; CO.sub.2 R.sup.3 is a carboxy group or a carboxylate anion, or R.sup.3 is a readily removable carboxy protecting group or a pharmaceutically acceptable salt-forming group or in vivo hydrolysable ester group; R.sup.4 represents hydrogen or up to four substituents; X is S, SO, SO.sub.2 or CH.sub.2 ; Y is O, S, SO or SO.sub.2 ; n is 0 or 1; m is 1 or 2; and wherein in the (a) ring system the dotted line indicates that one pair of adjacent ring carbon atoms is joined by a C.dbd.C double bond. These compounds have antibacterial activity.

Abstract: A pharmaceutical composition having reduced bitterness consisting of a bitter pharmaceutical agent, a taste-masking component and a pharmaceutically acceptable carrier. The taste-masking component is an alkaline earth oxide, an alkaline earth hydroxide or an alkaline hydroxide and does not interfere with the activity of the pharmaceutical agent.

Abstract: Macrolides of formula (I) and methods of treatment of resistance to transplantation, fungal infections and autoimmune diseases such as rheumatoid arthritis and psoriasis using said macrolides of formula (I), wherein n is 1 or 2; A and B are taken together and form .dbd.O or A and B are taken separately and are each H or A is OH and B is H; R.sup.1 is a 2-aminoglycosyl group; R.sup.2 is OH or a glycosyloxy group; and R.sup.3 is an alkyl or allyl group.

Abstract: The application discloses steroidal glycoside compounds, especially spirostanyl glycosides, which have a glycosyl group O-linked to the C-3 hydroxy radical of the steroid and where the moieties at the C-10 and C-11 positions of the steroid are the same or different and are selected from the group consisiting of methylene, hydroxy and carbonyl. These steroid glycosides are useful as hypocholesterolemic agents and anti-atherosclerosis agents.

Abstract: This invention relates to methods for treating intestinal motility disorders, intestinal ulcerations, including inflammatory bowel disease, ulcerative colitis, Crohn's disease and proctitis, and gastrointestinal ulcerations, depression, prostate disease and dyslipidemia by administering a .beta..sub.3 -adrenoceptor antagonist or agonist.

Abstract: Polypeptides isolated from the venom of the Heteropoda venanoria spider block calcium channels in cells of various organisms and are useful in blocking said calcium channels in cells, per se, in the treatment of calcium channel-mediated diseases and conditions and in the control of invertebrate pests.

Abstract: Compounds of the formula ##STR1## wherein the broken line represents an optional double bond; X is O, S, CH.sub.2 or CH.sub.2 CH.sub.2 ; R.sup.1 is selected from the group consisting of hydrogen, halogen, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkanoyl, C.sub.1 -C.sub.6 alkyl, and C.sub.1 -C.sub.6 alkyl substituted with 1, 2 or 3 halogen atoms; R.sup.2 is selected from the group consisting of phenyl, substituted phenyl, heterocyclic groups, and substituted heterocyclic groups, said substituted phenyl and substituted heterocyclic groups being substituted with 1 or 2 substituents independently selected from the group consisting of C.sub.1 -C.sub.6 alkyl, trifuluoromethyl, and halogen; R.sup.3 and R.sup.4 are independently selected from the group consisting of hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, or trifluoromethyl, or R.sup.3 and R.sup.

Abstract: A compound of formula V: ##STR1## wherein all the R's groups are as defined in the specification, is useful in the treatment of bacterial infections.

Abstract: This invention relates to a process for the removal of an allyl or allyloxycarbonyl group from an allyl or allyloxycarbonyl group protected compound (such as an allylic ester, carbonate, carbamate, O-allyl derivatives or N-allyl derivatives), which comprises contacting the allyl or allyloxycarbonyl group protected compound with a sulfinic acid compound, in the presence of a palladium catalyst in a reaction-inert solvent. Preferably, the sulfinic acid compound is represented by the formula:X--SO.sub.2 M (I)wherein X is C.sub.1-20 alkyl, substituted C.sub.1-20 alkyl (wherein the substituent(s) are independently halo, nitro, sulfo, oxo, amino, cyano, carboxy, hydroxy or moieties derived therefrom), phenyl, substituted phenyl (wherein the substituent(s) are independently C.sub.1-3 alkyl, halo nitro, sulfo, oxo, amino, cyano, carboxy, hydroxy, acetamido or moieties derived therefrom), furyl or thienyl; and M is hydrogen, an alkali metal or ammonium salt residue.

Abstract: Compounds of formula (I): ##STR1## wherein R.sup.1 is hydrogen or methyl, R.sup.2 is hydrogen or (E)-2-methyl 2-butenoyloxy, and R.sup.3 is hydrogen or hydroxy, with the proviso that when R.sup.3 is hydrogen, R.sup.1 and R.sup.2 are both hydrogen, and when R.sup.2 is (E)-2-methyl 2-butenoyloxy, R.sup.1 is methyl; the compound of formula (II): ##STR2## and the compound of formula (III): ##STR3## are obtainable by the fermentation of Streptomyces E225 NCIB 12310 or Streptomyces E225B NCIB 12509. The compounds have antihelminthic utility.

Abstract: This invention relates to compounds of formula (I) wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and X are as defined in the application. These compounds are CCK-B receptor antagonists and are useful in the treatment and prevention of central nervous system and gastrointestinal disorders.

Abstract: Compounds of formula (I) wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are each H or C.sub.1 -C.sub.4 alkyl; R.sup.5 is (CH.sub.2).sub.m NHSO.sub.2 R.sup.6 or (CH).sub.m NHCOR.sup.6 ; R.sup.6 is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl optionally substituted by aryl, aryl or heteroaryl; R.sup.7 is H, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halo, CF.sub.3, OCF.sub.3, CN, CONH.sub.2, or S(O).sub.n (C.sub.1 -C.sub.4 alkyl); X is CH.sub.2, CHCH.sub.3, CH(OH), C(OH)CH.sub.3, C.dbd.CH.sub.2, CO or O; m is 0 or 1 and n is 0, 1 or 2, and their pharmaceutically acceptable salts and biolabile esters, are antagonists of thromboxane A.sub.2 of utility, particulary in combination with a thromboxane synthetase inhibitor, in the treatment of atherosclerosis and unstable angina and for prevention of reocclusion after percutaneous transluminal angioplasty.

Abstract: Compounds of formula I, ##STR1## wherein R.sup.1 represents hydrogen; R.sup.2 represents hydrogen, halogen, cyano, OR.sup.4, --(CH.sub.2).sub.m CONR.sup.5 R.sup.6, --(CH.sub.2).sub.m SO.sub.2 NR.sup.5 R.sup.6, --(CH.sub.2).sub.m NR.sup.7 COR.sup.8, --(CH.sub.2).sub.m S(O).sub.x R.sup.8, --(CH.sub.2).sub.m NR.sup.7 CONR.sup.5 R.sup.6, --(CH.sub.2).sub.m NR.sup.7 COOR.sup.9 or --CH.dbd.CH(CH.sub.2).sub.y R.sup.10 ; R.sup.3 represents hydrogen or C.sub.1-6 alkyl; R.sup.4 represents hydrogen, C.sub.1-6 alkyl or aryl; R.sup.5 and R.sup.6 are independently represent hydrogen, C.sub.1-6 alkyl, aryl or (C.sub.1-3 alkyl)aryl; or R.sup.5 and R.sup.6 taken together may form a 4-, 5- or 6-membered ring; R.sup.7 and R.sup.8 independently represent hydrogen, C.sub.1-6 alkyl, aryl or (C.sub.1-3 alkyl)aryl; R.sup.9 represents hydrogen, C.sub.1-6 alkyl, aryl or (C.sub.1-3 alkyl)aryl; R.sup.10 represents --CONR.sup.5 R.sup.6, --SO.sub.2 NR.sup.5 R.sup.6, --NR.sup.7 COR.sup.8, --NR.sup.7 SO.sub.2 R.sup.8, --NR.sup.7 CONR.sup.

Abstract: The present invention relates to novel substituted benzothiazepines and benzoxazepines of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.7, R.sup.8, R.sup.9 and X are as defined below, and to novel intermediates used in the synthesis of such compounds.Such compounds are useful in the treatment and prevention of gastrointestinal disorders, pain and anxiety disorders.

Abstract: Compounds of formula ##STR1## where R is 5-indanyl or a carboxylic acid protecting group, or an amine salt thereof, are prepared by hydrogenating an (E)-allylic ether of formula ##STR2## in the presence of a stereoselective rhodium or ruthenium biphosphine catalyst and a protic solvent.

Abstract: A test apparatus for the in situ, non destructive, integrity testing of hydrophobic filters and/or their housings that is less sensitive to error from system pressure leaks. The apparatus comprises a pressurizable system including a pipe having an upstream end and a downstream end and a hydrophobic filter housing disposed inbetween. The hydrophobic filter housing has a hydrophobic filter disposed therein. The hydrophobic filter housing has an inlet which is in fluid communication with the upstream end of the pipe and the hydrophobic filter housing is closed to the downstream end of the pipe, but a fluid pathway to the downstream end of the pipe exists through the hydrophobic filter. The system has a second inlet including a flowmeter and the second inlet is disposed upstream of the downstream end of the pipe. An overflow outlet is disposed upstream of the hydrophobic filter and second inlet and is in fluid communication with a flow measurement device.