Abstract: An environmentally friendly process is described for the preparation of 4-hydroxy-2,2,6,6-tetramethylpiperidine-N-oxyl by the direct hydrogen peroxide oxidation of 4-hydroxy-2,2,6,6-tetramethylpiperidine in the absence of any catalyst.

Abstract: A class of sulforhodamine labeling reagents capable of binding with a biomolecular species to produce a conjugate with fluorescent properties. The sulforhodamine labeling reagents have the structure: ##STR1## The group X is selected from an alkyl, an olefin, a monocyclic aliphatic saturated hydrocarbon, an aryl, or nothing at all. The group Y is selected from an amide, a substituted amide, or nothing at all. The group Z is selected from a monocyclic aliphatic hydrocarbon, an aryl, or an alkyl, as defined with respect to group X, a polyethylene glycol chain of the general form (CH.sub.2 CH.sub.2 O).sub.n, or nothing at all. The alkyl or polyethylene glycol chain may further have inert intermediate amide, ether, or disulfide functionalities. The group X, group Y, and group Z cannot all be nothing at all or non-existent. The group R is an electrophilic moiety suitable for conjugation of the fluorescent labeling reagent with a biomolecular species. Also disclosed is a method of making the reagents.

Abstract: The invention provides a method for synthesizing chiral compounds utilizing novel catalysts which are enantioselective electrophiles via kinetic resolution. The method includes treating a racemic mixture with a reagent which is a chiral DMAP derivative, a chloroformate, a trialkylamine and a Lewis acid to preferentially form a product of one of the enantiomer pair of the mixture. The invention also provides a method for resolving racemic mixture via parallel kinetic resolution.

Abstract: This invention relates to a novel tetracyclic compound represented by formula (I): ##STR1## or its pharmacologically-acceptable salt. The compound of this invention has strong immunosuppressive activity, and is useful as an immunosuppressive agent and as an agent for treating autoimmune disease.

Abstract: A process for preparing substituted 4-methylidenecinnamic acid derivatives of Formula (I). ##STR1## The variables are defined herein. The compounds of Formula (I) can be used, for example, as UV absorbers.

Abstract: Novel 5-HT.sub.3 receptor antagonist compounds having the general formula (I) ##STR1## wherein each of R, R.sub.1 and R.sub.2, which may be the same or different, is hydrogen, halogen, hydroxy, cyano, C.sub.1 -C.sub.6 alkyl, CF.sub.3, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, formyl, C.sub.2 -C.sub.6 alkanoyl, carboxy, C.sub.1 -C.sub.6 alkoxy-carbonyl, nitro, --N(R.sub.4 R.sub.5) in which each of R.sub.4 and R.sub.5 independently is hydrogen, C.sub.1 -C.sub.6 alkyl, formyl or C.sub.2 -C.sub.6 alkanoyl; or a (R.sub.6 R.sub.7)N--SO.sub.2 group, in which each of R.sub.6 and R.sub.7 independently is hydrogen or C.sub.1 -C.sub.6 alkyl; ##STR2## wherein n is an integer of 1 or 2 and R.sub.8 is hydrogen, C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by phenyl, C.sub.2 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl, formyl or C.sub.2 -C.sub.6 alkanoyl; and the pharmaceutically acceptable salts thereof, are provided.

Abstract: The present invention relates to compounds of formula (I), and salts and prodrugs thereof, wherein n is 1 , 2 or 3 and where any carbon atom of (CH.sub.2).sub.n may be substituted by R.sup.4 and/or R.sup.5 ; X represents O or S; R.sup.1 represents optionally substituted (CH.sub.2).sub.q phenyl, wherein q is 0, 1, 2 or 3; R.sup.2 represents optionally substituted aryl, heteroaryl, benzhydryl or benzyl; R.sup.4 and R.sup.5 each independently represent H, halo, C.sub.1-6 alkyl, oxo, CO.sub.2 R.sup.a or CONR.sup.a R.sup.b ; R.sup.6 represents H or C.sub.1-6 alkyl; R.sup.7 represents C.sub.1-6 alkyl or optionally substituted phenyl; R.sup.8 represents H, COR.sup.a, CO.sub.2 R.sup.a, COCONR.sup.a R.sup.b, COCO.sub.2 R.sup.a, C.sub.1-6 alkyl optionally substituted by a variety of substituents, or C.sub.1-6 alkyl, optionally substituted by oxo, substituted by an optionally substituted aromatic heterocycle. The compounds are tachykinin antagonists useful for treating pain or inflammation, migraine or emesis.

Abstract: Compounds of formula (I) ##STR1## wherein one of X and Y represents nitrogen, and the other of X and Y represents oxygen, sulphur or N--R.sup.2 ; Q represents a substituted five- or six- membered monocyclic heteroaliphatic ring which contains one nitrogen atom as the sole heteroatom and is linked to the five-membered heteroatomic ring containing the moieties X and Y via a carbon atom; as well as substituted 1,3-dioxopropane precursors thereto, are ligands for dopamine receptor subtypes within the body and are therefore useful in the treatment of disorders of the dopamine system, in particular schizophrenia.

Abstract: Disclosed herein are compounds of Formula I ##STR1## and pharmaceutically acceptable salts thereof which have been found useful in the treatment of nitric oxide synthase mediated diseases and disorders, including neurodegenerative disorders, disorders of gastrointestinal motility and inflammation. These disease and disorders include hypotension, septic shock, toxic shock syndrom, hemodialysis, IL-2 therapy such as in cancer patients, cachexia, immunosuppression such as in transplant therapy, autoimmune and/or inflammatory indications including sunburn or psoriasis and respiratory conditions such as bronchitis, asthma, and acure respiratory distress (ARDS), myocarditis, heart failure, atherosclerosis, arthritis, rheumatoid arthritis, chronic or inflammatory bowel disease, ulcerative colitis, Crohn's disease, systemic lupus erythematosis (SLE), ocular conditions such as ocular hypertension and uveitis, type 1 diabetes, insulin-dependent diabetes mellitus and cystic fibrosis.

Abstract: An environmentally friendly process is described for the preparation of 4-hydroxy-2,2,6,6-tetramethylpiperidine-N-oxyl by the carbonate-mediated hydrogen peroxide oxidation of 4-hydroxy-2,2,6,6-tetramethylpiperidine.

Abstract: Compounds of the formula I ##STR1## wherein R.sup.1 and Y have the meanings indicated herein, and also their physiologically acceptable salts, inhibit the binding of fibrinogen to the corresponding receptor and can be employed for the treatment of thromboses, osteoporoses, oncoses, apoplexy, cardiac infarct, inflammations, arteriosclerosis and osteolytic disorders.

Abstract: A process of preparing 2-cyano-3,5-dimethyl-4-methoxypyridine. The process includes the steps of: acylating 2-methyl-1-penten-1-alkoxy-3-one to obtain 2-alkoxycarbonyl-3,5-dimethyl-4-pyrone; ammonolyzing 2-alkoxycarbonyl-3,5-dimethyl-4-pyrone to obtain 2-carboxamido-3,5-dimethyl-4(1H)-pyridone; methylating 2-carboxamido-3,5-dimethyl-4(1H)-pyridone to obtain 2-carboxamido-3,5-dimethyl-4-methoxypyridine; and dehydrating said 2-carboxamido-3,5-dimethyl-4-methoxypyridone to obtain 2-cyano-3,5-dimethyl-4-methoxypyridine.

Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as selective alpha-1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing orthostatic hypotension. One such tissue is found surrounding the urethral fining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.

Abstract: A process of preparing 2-hydroxymethyl-3,5-dimethyl-4-methoxypyridine including the steps of acylating 2-methyl-1-penten-1-alkoxy-3-one to obtain 2-alkoxycarbonyl-3,5-dimethyl-4-pyrone; ammonolyzing 2-alkoxycarbonyl-3,5-dimethyl-4-pyrone to obtain 2-alkoxycarbonyl-3,5-dimethyl-4(1H)-pyridone; halogenating 2-alkoxycarbonyl-3,5-dimethyl-4(1H)-pyridone to obtain 2-alkoxycarbonyl-4-halo-3,5-dimethylpyridine; methoxylating 2-alkoxycarbonyl-4-halo-3,5-dimethylpyridine to obtain 2-methoxycarbonyl-3,5-dimethyl-4-methoxypyridine; and reducing 2-methoxycarbonyl-3,5-dimethyl-4-methoxypyridine to obtain 2-hydroxymethyl-3,5-dimethyl-4-methoxypyridine.

Abstract: Biphenylylquinuclidine derivatives of formula I, Q--Ar.sup.1 --Ar.sup.2, in which Q is of formula Ia or Ib, ##STR1## in which R.sup.1 and R.sup.2 are independently selected from hydrogen, alkyl, halogeno and hydroxy; or R.sup.1 and R.sup.2 when taken together define an oxo group; Xb is selected from --CH.sub.2 --, .dbd.CH-- and --CH(OH); Xa is selected from --CH.sub.2 --, .dbd.CH--, CO, --O--, and --S(O)n (wherein n=0, 1 or 2); Ar.sup.1 is a phenylene moiety; Ar.sup.2 is phenyl; and wherein one or both of Ar.sup.1 and Ar.sup.

Abstract: A process is provided for preparing intermediates of the structure ##STR1## wherein Rpg is preferably .dbd.CHC.sub.6 H.sub.5 ; and P.G. is a protecting group CBZ or BOC, wherein a protected guanylpyrazole is reacted with an azacycloalkyl, azacycloalkenyl or azaheteroalkyl derivative (such as a piperidine derivative) in the presence of a DBU catalyst. The resulting intermediate may be used as a starting material for preparing thrombin inhibitors.

Abstract: Disclosed are adamantaneospiroheteroaromaticpyrans and adamantanospiro (1.3)oxazines of the general formula ##STR1## whereby R.sub.0 is a substituent from the series H, halogen, O-alkyl, N-alkyl,R.sub.1 -R.sub.4 : is a substituent from the series H, alkyl, aryl, subst. phenyl, naphthyl, heteroaryl, OH, alkoxy (C.sub.1 -C.sub.4), halogen, alkylamino, dialkylamino, cyan and trifluormethyl, orR.sub.1 and R.sub.2 or R.sub.3 and R.sub.4 or R.sub.2 and R.sub.3 are constituents of a condensed aromatic or heteroaromatic ring or an alkane ring with 4-8 C-atoms.

Abstract: The present invention relates to an novel dipiperidine derivative represented by formula (1), or a pharmaceutically acceptable salt thereof; ##STR1## wherein R.sup.1 represents a hydrogen atom or a lower alkyl group; Y represents a single bond or an oxygen atom; n represents 1, 2 or 3; W represents a methylene group or an oxygen atom; R.sup.2 represents a hydrogen atom or a carboxyl modifying group which can be eliminated in vivo; X.sup.1 and X.sup.3 are the same or different and each represents a hydrogen atom or a lower alkyl group.This compound is useful as platelet aggregation inhibitors, cancer metastasis inhibitors, wound remedies or bone resorption inhibitors.

Abstract: The invention concerns compounds of formula ##STR1## in which R, A, R.sub.1 and Y are as defined in claim 1. The instant compounds have an affinity for the fibrinogen receptor: the complex of the glycoproteins IIb/llIa (GP IIb/IIIa); more particularly, the subject of the present invention is new inhibitors of platelet aggregation which are antagonists of the GP IIb/IIIa receptors, of nonpeptide structure, which are active via the parenteral and oral routes.

Abstract: The present invention provides a compound of formula (I) ##STR1## in which R.sub.1 represents a hydrogen atom or a (C.sub.1 -C.sub.4)alkyl group, R.sub.2 represents a hydrogen atom or a straight or branched (C.sub.1 -C.sub.4)alkyl group, R.sub.3 represents a straight or branched (C.sub.1 -C.sub.7)alkyl group, a group --(CH.sub.2).sub.n OCH.sub.3 (where n is 1, 2 or 3) or a group --CH.sub.2 O(C.sub.2 H.sub.4 O).sub.m CH.sub.3 (where m is 1, 2 or 3), R.sub.4 represents a hydrogen atom or a halogen atom, R.sub.5 represents a straight or branched (C.sub.1 -C.sub.4)alkyl group and A represents phenyl or heterocyclic group optionally substituted with one or more substituents independently chosen from halogen atoms and straight or branched (C.sub.1 -C.sub.4)alkyl, straight or branched (C.sub.1 -C.sub.4)alkoxy and trifluoromethyl groups, or a cyclo(C.sub.5 -C.sub.