Abstract: This invention provides novel oxazolidinone derivatives represented by chemical Formula (I), or pharmaceutically acceptable salts thereof: ##STR1## wherein X is NR.sub.1, CR.sub.2 R.sub.3, O, S, SO, or SO.sub.2 ; and Z is NR.sub.4, S, SO, SO.sub.2 or O. The compounds are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci and streptococci, as well as anaerobic organisms such as bacteroides and clostridia species, and acid-fast organisms such as Mycobacterium tuberculosis and Mycobacterium avium.

Abstract: A method is disclosed for the preparation of 9-nitrocamptothecin which involves reacting 20-camptothecin with at least one inorganic nitrate salt and at least one acid effective in catalyzing the formation of a nitronium ion, where the reaction occurs at a temperature and for a time sufficient to form the 9-nitrocamptothecin. Also, methods of further purifying the 9-nitrocamptothecin by column chromatography or by reprecipatation is also disclosed.

Abstract: The present invention relates to compounds of the following formulas: ##STR1## which are endowed with antitumor activity. The invention also relates to methods of treating tumors using these compounds.

Abstract: A novel crystal modification of the compound 2,4-diamino-6-hydroxymethylpteridine hydrobromide and a process for its preparation and its use for preparing methotrexate. The novel crystal modification of 2,4-diamino-6-hydroxymethylpteridine hydrobromide is distinguished in particular by the fact that only one equivalent of the brominating agent triphenylphosphine dibromide is needed for brominating the 6-hydroxymethyl group. No reaction with the amino groups in the 2 and 4 positions takes place. This facilitates the reaction to give 2,4-diamino-6-pteridinyl derivatives such as methotrexate.

Abstract: Novel compounds, formulations and methods of treating patients with cancer are provided for in this invention. The compounds are derivatives of camptothecin, and specifically relate to compounds having novel substitutions at the C-7 position of the camptothecin scaffold B-ring. The formula I compounds are highly lipophilic, lactone stable, do not require metabolic activation, and are potent antineoplastic compounds.

Abstract: A hetero-aromatic (Q) substituted phenyloxazolidinone antimicrobial of Formula (I) wherein Q is a 5-member hetero-aromatic having from one to four nitrogen atoms or alternatively a benzoannulated 5-member hetero-aromatic having from one to four nitrogen atoms where R.sup.1 is independently H, OCH.sub.3, F, or Cl; R.sup.2 is hydrogen, C.sub.1 -C.sub.8 alkyl (optionally substituted with one or more of F, Cl, hydroxy, C.sub.1 -C.sub.8 alkoxy, C.sub.1 -C.sub.8 acyloxy), C.sub.3 -C.sub.6 cycloalkyl, amino, C.sub.1 -C.sub.8 alkylamino, C.sub.1 -C.sub.8 dialkylamino, C.sub.1 -C.sub.8 alkoxy; and each Q is optionally substituted with one or more of H, F, Cl, Br, OR.sup.4, SR.sup.4, S(O).sub.n R.sup.4 (n=1 or 2), CN, O.sub.2 CR.sup.4, NHCOR.sup.4, NHCO.sub.2 R.sup.4, NHSO.sub.2 R.sup.4, CO.sub.2 R.sup.4, CON(R.sup.4).sub.2, COR.sup.4, C.sub.1 -C.sub.8 straight or branched chain alkyl or C.sub.3 -C.sub.

Abstract: Compounds of the Formula I ##STR1## are inhibitors of the 5.alpha.-reductase 1 isozyme, and are useful alone, or in combination with a 5.alpha.-reductase 2 inhibitor, for the treatment of androgenic sensitive disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern baldness, and benign prostatic hyperplasia.

Abstract: A process for preparing a compound of formula (I) ##STR1## wherein R is a methylthio, methylsulfoxy, methylsulfonyl or a nitro group; andX4 is --OH, fluorine or --O--SO.sub.2 R6 where R6 is methyl, trifluoromethyl, phenyl or p-methylphenyl which comprises contacting of a compound of formula (III) ##STR2## where R2 is C.sub.1-4 alkyl; and R and X4 have the above mentioned meanings, with a strong base selected from the group consisting of alkali earth metal alcoholates, alkaline earth metal alcoholates, and tertiary amines in an aprotic solvent, to obtain the compound of formula (I).

Abstract: N-Benzylazolium derivatives of the general formula (I), ##STR1## wherein Q is the remainder of an azole compound of the formula II ##STR2## possessing antifungal activity; Z is nitrogen or methine;R.sup.1 and R.sup.2 are each independently a hydrogen atom or a group --OY ?in which Y is a group easily hydrolyzable under physiological condition!;R.sup.3 and R.sup.4 are each independently a hydrogen or halogen atom, lower alkyl, lower alkoxy, lower alkylthio, (lower alkylcarbonyl)thiomethyl, carboxy or methoxycarbonyl; andX.sup.- is a pharmaceutically acceptable anion,as well as salts, hydrates or solvates of the compounds of the general formula (I) have antifungal properties.

Abstract: The present invention refers to basic oxazoline-amide derivatives of GE 2270 and GE 2270-like antibiotics of general formula (I), wherein the group GE represents the antibiotic core molecule. The amide derivatives of antibiotic GE 2270 of formula (I) are antimicrobial agents mainly active against gram positive bacteria.

Abstract: Compounds of the formula ##STR1## are inhibitors of 5.alpha.-reductase and are useful alone or in combination with other active agents for the treatment of hyperandrogenic disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern baldness, and benign prostatic hyperplasia.

Abstract: New morphinane derivatives of the formula (I) ##STR1## their pharmaceutically acceptable salts, a process for their preparation and their use in therapy. The variables in the above structure are as follows: R.sub.1 is selected from the group consisting of C.sub.1 -C.sub.6 alkyl and hydrogen;R.sub.2 is selected from the group consisting of hydrogen; hydroxy; C.sub.1 -C.sub.6 alkoxy; C.sub.7 -C.sub.16 arylalkyloxy, wherein the aryl is C.sub.6 -C.sub.10 aryl and the alkyloxy is C.sub.1 -C.sub.6 alkyloxy;R.sub.3 is a C.sub.1 -C.sub.6 alkyl;R.sub.4 is a hydrogen; hydroxy; or a C.sub.1 -C.sub.6 alkoxy;R.sub.5 and R.sub.6 each and independently are selected from the group consisting of hydrogen; and C.sub.1 -C.sub.6 alkyl;X is NR.sub.9, wherein R.sub.9 is selected from the group consisting of hydrogen; and C.sub.1 -C.sub.6 alkyl;and wherein any aryl group in the compound may be unsubstituted or mono-, di-, or tri-substituted independently with hydroxy; halo; nitro; cyano; thiocyanato; trifluoromethyl; C.sub.1 -C.

Abstract: The invention relates to new 1,3,4-oxadiazine derivatives of the formula (I) ##STR1## in which Ar.sup.1 represents in each case optionally substituted aryl or hetaryl,Ar.sup.2 represents in each case optionally substituted aryl or hetaryl andX represents the group --(CHR.sup.1).sub.m --(CHR.sup.2).sub.n in whichR.sup.1 represents hydrogen or alkyl,R.sup.2 represents hydrogen or alkyl,m represents 0 or 1 andn represents 0 or 1,to a plurality of processes for their preparation, and to their use for combating animal pests.

Abstract: The present invention provides benzoxazole derivatives and nonlinear optical (NLO) materials obtained therefrom as a novel organic NLO material having following general formula (I), which can be used as optical devices such as electro-optic modulator, optical switch, or the like for treating optical signal in optical communication industry. In order to obtain more stable NLO material, benzoxazole group having high thermal resistance is substituted as a .pi. conjugated unit instead of conventional stilbene or azobenzene group. A variety of NLO materials can be prepared by the synthetic process according to the present invention. ##STR1## wherein D and Ar have the same meaning as defined in the aforementioned.

Abstract: Disclosed are pharmaceutical compositions that comprise gallium complexes of 3-hydroxy-4-pyrones. These compositions provide enhanced gallium bioavailability particularly when orally administered as compared to the gallium bioavailability achieved by use of pharmaceutical compositions containing gallium salts. Compositions included in this invention are useful in providing gallium to humans and other mammals for a wide variety of medical and veterinary applications, including the treatment, prevention, or diagnosis of hypercalcemia, certain cancers, certain disorders of calcium homeostasis, and certain bone diseases including osteoporosis, osteopenia, and Paget's disease.

Abstract: A process for preparing 3-alkoxy-5-alkylpyrazin-2-amines of the general formula: ##STR1## wherein R.sup.1 is a C.sub.1-4 -alkyl group or an aryl group and R.sup.2 is a C.sub.1-4 -alkoxy group or an aryloxy group, starting either from aminomalononitrile or from aminoacetonitrile.

Abstract: The present invention relates to the derivatives of formula: ##STR1## and to their use in therapeutics, especially as drugs with anti-inflammatory and analgesic properties.

Abstract: The present invention is directed to (R)-(-)-4,5-dihydro-5-methyl-6-?4-?(2-propyl-3-oxo-1-cyclohexenyl)amino!ph enyl!-3(2H)-pyridazinone, the crystalline form thereof and a method for manufacturing the said compound and the said crystalline form.The compound of the present invention has excellent inhibitory effect on platelet aggregation while giving less side effect, and therefore, it is useful to utilize the compound as an antithrombotic drug. In addition, the compound of the present invention has bronchodialatic effect as well, and it is therefore useful to utilize the compound for chemotherapy of chronic obstructive lung disease, such as asthma and bronchitis.Moreover, the compound of the present invention is useful for chemotherapy of the diseases relating to the concentration of cAMP in cells, such as hypertension, ulcer, diabetes mellitus and cancer.Again, crystalline form of the said compound is the most suitable form in order to supply stable and homogeneous bulk thereof.

Abstract: The present invention relates to substituted camptothecin derivatives of formula (I) wherein the symbol - - - - represents a single or double bond; R.sub.1, R.sub.2 and R.sub.3 are as defined under (a) or (b) below: (a) R.sub.1 and R.sub.2 are, each independently, hydrogen; C.sub.1 -C.sub.4 alkyl; C.sub.3 -C.sub.7 cycloalkyl; phenyl C.sub.1 -C.sub.6 alkyl; an optionally substituted phenyl ring; --NR.sub.5 R.sub.6 wherein one of R.sub.5 and R.sub.6 is hydrogen, C.sub.1 -C.sub.6 alkyl or benzyl and the other is hydrogen, C.sub.1 -C.sub.6 alkanoyl, an optionally substituted C.sub.1 -C.sub.6 alkoxycarbonyl, an optionally substituted benzoyl, phenyl C.sub.1 -C.sub.6 alkanoyl, an optionally substituted C.sub.1 -C.sub.6 alkoxycarbonyl, an optionally substituted phenoxycarbonyl or phenyl C.sub.1 -C.sub.6 alkoxycarbonyl, or R.sub.5 and R.sub.6, combined together with the nitrogen atom to which they are linked, form a 4-7 membered saturated, optionally substituted, heteromonocyclic ring residue; COOR.sub.8 wherein R.

Abstract: Organic materials normally subject to gradual degradation in the presence of oxygen are stabilized by inclusion of an aromatic fluorophosphite having at least one benzene group bonded through oxygen to phosphorus and at least one fluorine atom bonded directly to the same phosphorus. Stabilization is improved by also including a conventional phenolic antioxidant. Many of the aromatic fluorophosphites are new compounds.