Abstract: The present invention relates to azacycloalkylalkanoyl peptides and pseudopeptides which inhibit platelet aggregation and thrombus formation thereby being useful in the prevention and treatment of thrombosis associated with disease states such as myocardial infarction, stroke, peripheral arterial disease, and disseminated intravascular coagulation, to methods for the prevention or treatment of thrombosis in a mammal in need of such therapy comprising the administration of a therapeutically effective amount of such compounds, and to pharmaceutical compositions comprising such compounds.

Abstract: Compounds of formula I ##STR1## wherein G, J, L, M, m and D have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of neurokinin A and useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.

Abstract: The present invention relates to compounds of formula (I), ##STR1## wherein A is an optionally substituted phenyl naphthyl, pyridyl, pyrazinyl, pyridazinyl, pyrimidyl, thienyl, thiazolyl, oxazolyl, thiadiazolyl having at least two adjacent ring carbon atoms or a bicyclic ring system, provided that the --CH(R.sup.3)N(R.sup.2)B--R.sup.1 and --OCH(R.sup.4 --)--D linking groups arm positioned in a 1,2 relationship to one another on ring carbon atoms and the ring atom positioned ortho to the --OCHR.sup.4 -- linking group (and therefore in the 3-position relative to the --CHR.sup.3 NR.sup.2 -- linking group) is not substituted; B is an optionally substituted ring system; D is an optionally substituted ring system; R.sup.1 is a variety of group as defined in the description; R.sup.2 is hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, phenylC.sub.1-3 alkyl or 5- or 6-membered heteroarylC.sub.1-3 alkyl; R.sup.3 is hydrogen or C.sub.1-4 alkyl; R.sup.4 is hydrogen or C.sub.1-4 alkyl; and N-oxides of NR.

Abstract: The invention relates to alpha-substituted pyridazino-quinoline compounds of the formula I: ##STR1## wherein Ring A is chosen from an ortho fused aromatic or heteroaromatic five- or six-membered ring; R.sup.1 is selected from a variety of substituents including halogen, (1-4C)alkyl and nitro; R.sup.2 is selected from a group of the formula R2', R2" or R2"' wherein R2' is --CHR.sup.3 (CH.sub.2).sub.n C(O)NR.sup.5 R.sup.6 ; R2" is --CHR.sup.3 (CH.sub.2).sub.n R.sup.4 and R2"' is --CHR.sup.3 (CH.sub.2).sub.n L wherein n is 0-6; R.sup.5 is aryl or substituted aryl; R.sup.6 is (1-6C)alkyl or hydrogen; R.sup.3 is (1-6C)alkyl, (0-6C)alkylCF.sub.3 or (0-6C)alkylCOOR'; R.sup.4 is (1-6C)alkyl, (2-6C)alkyl containing a double or triple bond, or (0-6C)alkylaryl; L is a variety of substituents including phenyl, heteroaryl and CO.sub.2 R'; R' is hydrogen or (1-4C)alkyl; Z is selected from oxo, --OH, H,H--, H, (1-6C)alkyl or (1-6C)alkylaryl; and R.sup.7 is hydrogen or --(CO)R.sup.8 wherein R.sup.

Abstract: This invention relates to substituted and unsubstituted ???(aryl- and heteroaryl-) alkyl-, alkyloxy-, alkylthio-, oxo-, thio-, and alkylamino!- heteroaryl and aryl!- alkylamino-, aminoalkyl-, alkyloxy-, and alkylthio!- aryl and heteroaryl compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof, which are useful as antagonists of the pain enhancing effects of E-type prostaglandins, to processes for the preparation of such compounds, to pharmaceutical compositions comprising such compounds, and to methods for treating pain comprising the administration of such compounds.

Abstract: The invention relates to compounds of the formula (I): ##STR1## wherein A, B and D are various ring systems such as phenyl, R.sup.1 includes carboxy, R.sup.3 is hydrogen or C.sub.1-4 alkyl and Z is a linking group such as --(CH(R.sup.5)).sub.m -- wherein m is 2, 3 or 4, and R.sub.5 includes hydrogen and methyl; and pharmaceutically acceptable salts and in vivo hydrolysable esters or amides thereof, processes for preparing these compounds, pharmaceutical compositions comprising them, and their use in the treatment of pain.

Abstract: The invention relates to aminotetralin derivatives of the formula I: ##STR1## wherein: R.sup.1 is methyl or ethyl; R.sup.2 is hydrogen, halogen, lower-alkoxy or thiolower-alkyl; R.sup.3 is hydrogen, halogen, lower-alkoxy or lower-alkyl; and the chiral center * is in the (S)(-) form; or a pharmaceutically acceptable acid-addition salt thereof, with the proviso that when R.sup.2 and R.sup.3 are both hydrogen, R.sup.1 must be methyl; to pharmaceutical compositions containing them and to methods for the treatment or prevention of movement disorders utilizing them.

Abstract: Compounds of formula I ##STR1## where R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, n, and are as defined herein, their use as antiinflammatory, immunosuppressive, and antiallergic agents, pharmaceutical compositions comprising them, and methods for their preparation comprising irradiating compounds of formula II ##STR2## under an inert atmosphere, in the presence or absence of a compound of formula R.sub.3 --S--S(O).sub.m --R.sub.8, where R.sub.7, R.sub.8, and m are as defined herein, and methods for their preparation comprising oxidizing, reducing, halogenating, or alkylating compounds of formula I are disclosed.

Abstract: Antagonists at the NMDA receptor complex which are benz?b!azepines having a hydroxy, alkoxy or amino substituent at the 3-position and a 4-position alkenyl, alkynyl, aryl or heteroaryl substituent for treatment of stroke and/or other neurodegenerative disorders.

Abstract: A novel method for monitoring the success or the yield of chemical reactions involving a reactant bound to a solid phase support, or to forecast the success of such reactions, or to quantify the number of deuterium containing groups present in a solid-phase bound sample, using infrared spectroscopy and deuterium-carbon absorbances, along with novel compounds and intermediates useful for carring out the method.

Abstract: The invention relates to a process for the preparation of intermediates useful in the preparation of (1R,2R)-2-(3-pyridyl)-N-alkyltetrahydro-2H-thiopyran-2-carbothioamide 1-oxides, which possess useful pharmaceutical properties, for example antihypertensive properties, and to intermediates and pharmaceutical products prepared using said process.

Abstract: The present invention relates to compounds, pharmaceutical compositions and methods of using compounds of formula (I) in the treatment and/or prevention of certain diseases or conditions. In formula (I), A is chosen from ortho substituted aryl or heteroaryl species, X is chosen from --OH, --SH, NHR and R.sup.1 or R.sup.2 is chosen from --(CH.sub.2).sub.n L wherein L may be selected from a variety of substituents including aryl, heteroaryl and heterocyclic groups. The compounds are useful in treating and/or preventing neurological disorders associated with excitatory amino acids.

Abstract: Compounds of formula I ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, and Q.sup.4 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of neurokinin A and useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.

Abstract: Compounds of the Formula ##STR1## wherein: K is N or N.fwdarw.O; Q is CH.sub.2 or O; T is ##STR2## or R.sub.3 O--CH.sub.2 ; X is a straight or branched chain alkylene, cycloalkylene or cycloalkenylene group, each of which is optionally substituted by at least one CH.sub.3, CH.sub.3 CH.sub.2, Cl, F, CF.sub.3 or CH.sub.3 O; Y is NR.sub.4, O or S; a=0 or 1; Z is of the formula ##STR3## Z.sub.1 is N, CR.sub.5, (CH).sub.m --CR.sub.5 or (CH).sub.m --N, m being 1 or 2; Z.sub.2 is N, NR.sub.6, O or S, n being 0 or 1; R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are independently H, alkyl, aryl or heterocyclyl; R.sub.a and R.sub.

Abstract: Compounds of formula I ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, and Q.sup.4 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of SP and NKA are useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.

Abstract: The invention relates to new mixtures of sulfated oligosaccharides having the general structure of heparin constitutive oligosaccharides, having an average molecular mass of 6.+-.0.6 kD, a polydispersiveness close to 1 and the capacity of inhibiting the production of thrombin. The invention also relates to their preparation and to pharmaceutical compositions containing them.

Abstract: Compounds of formula I ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, Q.sup.4, and Q.sup.5 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of SP and NKA are useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.

Abstract: The invention relates to new mixtures of sulfated oligosaccharides having the general structure of heparin constitutive oligosaccharides, having an average molecular mass of 6.+-.0.6 kD, a polydispersiveness close to 1 and the capacity of inhibiting the production of thrombin. The invention also relates to their preparation and to pharmaceutical compositions containing them.

Abstract: Compounds of formula I ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, and Q.sup.4 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of neurokinin A and useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.

Abstract: A process is described for the preparation of a compound of formula (IX) from 4-hydroxybutyl 3-pyridyl ketone. The compound of formula (IX) is an intermediate useful in the preparation of (1R,2R)-2-(3-pyridyl)-N-alkyl-tetrahydro-2H-thiopyran-2-carbothioamide 1-oxides which possess useful pharmaceutical properties, for example anti-hypertensive properties.