Abstract: A substituted-amidinobenzene derivative of the following general formula (I) or a salt thereof, and a pharmaceutical composition comprising said derivative or a salt thereof and a pharmaceutically acceptable carrier. ##STR1## (the symbols in the above formula have the following meanings: R.sup.1 : a group which can be converted into an amidino group in vivo;R.sup.2 and R.sup.3 : the same or different and each represents a carboxyl group or a group which can be converted into a carboxyl group in vivo;X.sup.1 and X.sup.2 : the same or different and each represents a lower alkylene group;m: 0, 1 or 2;n: 0 or 1, provided that n=1 when m=0.They have GPIIb/IIIa receptor antagonizing activity and are useful as medicines for ameliorating ischemic cardiac disorders, adminicula in cardiosurgery operations or in vascular surgery operations, medicines for ameliorating cerebrovascular disorders, And medicines for ameliorating peripheral artery disorders.

Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as 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 hypotension. One such tissue is found surrounding the urethral lining. 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 tachykinin receptor antagonist, in particular a neurokinin-1 receptor antagonist, is useful for the treatment or prevention of chronic nonbacterial prostatitis and/or prostatodynia.

Abstract: Supertwist liquid-crystal displays having excellent properties are obtained if the nematic liquid-crystal mixture comprises at least one compound of the formula I: ##STR1## and at least one compound of the formula I.sup.* : ##STR2## in which R.sup.1 is alkyl, alkoxy, alkenyl or alkenyloxy having 1 to 12 carbon atoms,R.sup.2 is alkyl or alkoxy having 1 to 8 carbon atoms,Z is --COO--, --CH.sub.2 CH.sub.2 or a single bond,one of the radicals L.sup.1 and L.sup.2 is F and the other is H,Alkenyl.sup.* is an alkenyl radical having up to 7 carbon atoms,L.sup.* is H or F, andR.sup.* is F or an alkyl group having 1 to 12 carbon atoms which is unsubstituted or non-substituted.

Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.

Abstract: 8a-Azalides are useful in the treatment and prevention of bacterial respiratory and enteric infections in livestock animals, particularly in cattle and swine.

Abstract: The present invention provides a compound of formula I, or a pharmaceutically acceptable salt thereof: ##STR1## wherein Z, E, Q, T, U, V and L are as defined herein; processes for its preparation and its use in the treatment of conditions for which the administration of an agonist selective for the 5-HT.sub.1D.alpha. receptor subtype is indicated, such as migraine.

Abstract: The present invention discloses the isolation and characterization of cDNA molecules encoding two human nuclear receptor proteins, designated nNR1, nNR2 and/or nNR2-1. Also within the scope of the disclosure are recombinant vectors, recombinant host cells, methods of screening for modulators of nNR1, nNR2 and/or nNR2-1 activity, and production of antibodies against nNR1, nNR2 and/or nNR2-1, or epitopes thereof.

Abstract: Compounds having formula I, or salts or prodrugs thereof: ##STR1## are selective agonists of the 5-HT.sub.1D.alpha. receptor and are useful in the treatment of migraine and associated conditions.

Abstract: A class of azetidine, pyrrolidine and piperidine derivatives, substituted by inter alia a phenylmorpholinyl, phenylpiperidinyl or benzimidazolone moiety, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.

Abstract: The present invention is directed to the compound 4-N,N-dimethylaminomethyl-5-formyl-1,2,3-triazole which is a valuable intermediate in the preparation of phamaceutical compounds. The present invention is further directed to a novel convergent process for the preparation of 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)-ethoxy)-4-(5-(dimethylamino) methyl-1,2,3-triazol-4-yl)methyl-3-(S)-(4-fluorophenyl)-morpholine which is a potent and selective substance P (or neurokinin-1) receptor antagonist useful as a therapeutic agent.

Abstract: A class of 2,7-diazabicyclo[3.3.0]octane derivatives represented by formula I are selective agonists of the 5-HT.sub.1D.alpha. receptor. The compounds are useful in the treatment of migraine and related conditions.

Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.

Abstract: The present invention is concerned with a novel linear process for the preparation of 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl) phenyl)-ethoxy)-4-(5-(dimethylamino)methyl-1,2,3-triazol-4-yl)methyl-3-(S) -(4-fluorophenyl)-morpholine which is a potent and selective substance P (or neurokinin-1) receptor antagonist usefull as a therapeutic agent.

Abstract: The compounds of Formula I are useful as immunosuppressive agents.

Abstract: Indolylquinones are useful for the treatment and prevention of diabetes mellitus, and in particular, for the treatment or prevention of hyperglycemia in diabetic patients. Some of the indolylquinones are produced by fermentation of the novel fungus Pseudomassaria sp. ATCC 74411.

Abstract: Vaccine stabilizers, vaccine formulations and lyophilized vaccines with enhanced thermostability are disclosed. The vaccine formulations comprise an increased amount of a 6-carbon polyhydric alcohol (such as sorbitol), an increase amount of a disaccharide (such as sucrose) and an amount of a physiologically active buffer to adjust the pH from about 6.0 to about 7.0.

Abstract: The novel compounds of the present invention are those of structural formula I: ##STR1## or a pharmaceutically acceptable salt, ester, or stereoisomer thereof, which are inhibitors of 5.alpha.-reductase. The compounds of formula I are useful in the oral, systemic, parenteral or topical treatment of hyperandrogenic conditions. Methods of using the compounds of formula I for the treatment of hyperandrogenic conditions such as acne vulgaris, seborrhea, androgenic alopecia, male pattern baldness, female hirsutism, benign prostatic hyperplasia, and the prevention and treatment of prostatic carcinoma, as well as the treatment of prostatitis the treatment of sweat-related conditions such as apocrine gland sweating, hyperhidrosis, and hydradenitis suppurativa, the treatment of polycystic ovary syndrome, the prevention and treatment of bone loss and related diseases, and the prevention and treatment of premature labor are provided, as well as pharmaceutical compositions for the compounds of formula I.

Abstract: A process of synthesizing a carbapenem compound of formula 6: ##STR1## is disclosed using a compound of formula 4': ##STR2## The intermediate compounds that are described herein are also included in the present invention.

Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors .alpha.v.beta.3, .alpha.v.beta.5, and/or .alpha.v.beta.6 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, wound healing, viral disease, tumor growth, and metastasis.