Abstract: The invention concerns novel [5,6]-cis-1,3-oxathiane derivatives of formula I in which R.sup.1 and R.sup.2 are variously defined as hydrogen, alkyl, trifluoromethyl or phenyl (as set out in the specification), n is 1 or 2, m is 2, 3 or 4, Y is vinylene and Z is carboxy, 1(H)-tetrazol-5-yl or a group of the formula --CO.NH.SO.sub.2 R.sup.3 in which R.sup.3 is alkyl, phenyl or benzyl, and pharmaceutically acceptable salts thereof, for use in conjunction with their pharmaceutical compositions in treating certain pulmonary and/or vascular disorders. The invention also describes various processes and intermediates for the manufacture of the novel compounds.

Abstract: Derivatives of 2-substituted-cycloheptoimidazole are disclosed, which are represented by the following formula: ##STR1## wherein R is a hydrogen atom, a lower-alkyl, acetyl, lower-alkylaminoalkyl or ethylenedioxyethyl group. A represents a phenyl, pyridyl, benzimidazolyl, imidazolyl, thiazolyl, thiadiazolyl, oxazolyl or isoxazolyl group; each of which optionally possesses one substituent or more and m is 0 or 1, and n is 1 or 2. These compounds are useful as anti-ulcerative agents.

Abstract: Aromatic 1,4-benxodiazepines with fused 5- or 6-membered heterocyclic rings which are antagonists of cholecystokinins and/or gastrin, and are useful in the treatment or prevention of CCK-related and/or gastrin-related disorders of the gastrointestinal, central nervous and appetite regulatory systems; compositions comprising these compounds; and methods of treatment employing these compounds.

Abstract: A group of variously methyl-substituted[1,2-c:3,4-c']dipyrazoles, cyclohepta[1,2-c:3,4-c']dipyrazoles, and cyclopenta[1,2-c:3,4-c']dipyrazoles useful as bronchodilators are described herein. The compounds are prepared by reacting a 1,3-diketone with hydrazine or methylhydrazine to give tricyclic products optionally followed by catalytic dehydrogenation and/or alkylation with a strong base and methyl iodide to give various other compounds within the scope of the invention.

Abstract: 1-(Alkylated)-2-(acylated)diazolidinones are intermediates to bicyclic pyrazolidinone antimicrobial compounds. The instant compounds have the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are as defined in the specification.

Abstract: The invention concerns novel pyruvate compounds namely L-lysine pyruvate and L-histidine pyruvate, the method for making these compounds by bringing together pyruvic fluid acid with L-lysine and L-histidine resp., and preparations containing L-lysine pyruvate and/or L-histidine pyruvate.

Abstract: Catalytic transhalogenation of haloaromatics according to the equation:C.sub.z F.sub.a X.sub.b N.sub.e L.sub.1 +C.sub.z F.sub.c X.sub.d N.sub.e L.sub.2 .fwdarw.C.sub.z F.sub.a+1 X.sub.b-1 N.sub.e L.sub.1 +C.sub.z F.sub.c-1 X.sub.d+1 N.sub.e L.sub.2wherein:when C.sub.z is a benzene derivative, a+b=5; e=0; c+d=5; z=6;when C.sub.z is a pyridine derivative, a+b=4; e=1; c+d=4; z=5;when C.sub.z is a naphthalene derivative, a+b=7; e=0; c+d=7; z=10; andwhen C.sub.z is a biphenyl derivative, a+b=9; e=0; c+d=9; z=12;L.sub.1 and L.sub.2, alike or different, are selected from F, Cl, Br, H, CN, C.sub.n F.sub.2n+1, and C.sub.6 F.sub.5 ;X is Cl, Br, or I when C.sub.z is a benzene derivative; andn is 1 to 12. This method is a novel route to known haloaromatic compounds.

Abstract: The present invention is directed to a group of compounds which are variously methylated thiopyranodipyrazoles and to the S-oxides and S-dioxides of such compounds. The compounds are useful as bronchodilators and are prepared by the reaction of appropriately 5-substituted thiopyrano[3,4-c]pyrazol-4-(1H)-one with a hydrazine.

Abstract: Aminoethyl imidazole of formula: ##STR1## in which R.sub.1 is a lower alkyl, R.sub.2 is a phenyl or phenoxy radical, optionally substituted by a halogen atom or a lower alkoxy radical, R.sub.3,R.sub.4 and R.sub.5 are a hydrogen atom or a lower alkyl radical and x, y and z have the value 0 or 1, but the values of y and z cannot be the same, together with their acid addition salts with acids.Cytoprotective medicament.

Abstract: The invention features compounds having anti-arthritic activity and having the formula ##STR1## wherein X is an alkyl group having between 1 and 8, inclusive, carbon atoms and Y is a hydroxyalkylamino group having between 2 and 8, inclusive, carbon atoms; a dialkylamino group having between 2 and 12, inclusive, carbon atoms; a carboxyalkylamino group having between 2 and 9, inclusive, carbon atoms; a heterocycloalkyl group having between 2 and 5, inclusive, carbon atoms and having nitrogen as a hetero atom; an alkylthioalkylamino group having between 3 and 10, inclusive, carbon atoms; or a heteroarylalkylthioalkylamino group having between 5 and 14, inclusive, carbon atoms and having ntrogen as a hetero atom.

Abstract: Compounds of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and Y have the indicated meanings, their physiologically tolerated acid addition salts, and a process for the preparation of these compounds, are described. The compounds inhibit thromboxane synthetase and can thus be used as medicaments.

Abstract: 2,2,6,6-tetramethyl-4-oxopiperidine is prepared from acetone and ammonia in the presence of catalytic amounts of active halogen compounds selected from sulfonylhalides, sulfurylhalides, N-haloamides, N-haloimides, .beta.-haloesters, .alpha.-haloketones, .alpha.-halohydroxy compounds, and .beta.-halonitriles.

Abstract: The present invention is directed to a group of methylated tetrahydro cyclohepta[1,2-c:4,3-c']dipyrazoles and benzo[1,2-c:4,3-c']dipyrazoles useful as bronchodilators. The compounds are prepared by the reaction of an appropriate hydrazine with an appropriate 1,3-diketone or with a compound that is chemically equivalent to a 1,3-diketone.

Abstract: 1-Alkylated diazolidinones are intermediates to bicyclic pyrazolidinone antimicrobial compounds. The instant compounds have the formula ##STR1## wherein R.sub.1, R.sub.2, and R.sub.3, have the meanings as defined in the specification.

Abstract: 4-Amino-3-imidazolin-2-one and (2-methoxy-2-iminoethyl) urea are valuable intermediates for the production of pharmacologically active compounds.

Abstract: Herbicidally active 5-acylamido-1-aryl-pyrazoles of the formula ##STR1## in which R.sup.1 represents hydrogen, halogen or nitro,R.sup.2 represents hydrogen or alkyl,X represents oxygen or sulphur,Y represents oxygen, sulphur, a sulphinyl group or a sulphonyl group,A represents a straight-chain or branched, optionally substituted alkylene bridge,Ar.sup.1 represents in each case optionally substituted aryl or heteroaryl, andAr.sup.2 represents in each case optionally substituted phenyl or pyridyl.

Abstract: The invention relates to novel substituted N-phenyl-N'-acylisothioureas of the formula ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.5 alkyl,R.sub.2 is hydrogen or C.sub.1 -C.sub.5 alkyl,R.sub.3 is hydrogen, halogen, C.sub.1 -C.sub.5 alkyl, phenoxy or phenoxy which is substituted by 1 or 2 identical or different members selected from the group consisting of halogen atoms, C.sub.1 -C.sub.5 alkyl or trifluoromethyl radicals,R.sub.4 is C.sub.1 -C.sub.5 alkyl or propargyl,R.sub.5 is C.sub.1 -C.sub.5 alkyl, C.sub.3 -C.sub.6 cycloalkyl, allyl or propargyl, andR.sub.6 is a radical selected from --CO--R.sub.7, --CO--CO--R.sub.8, --SO.sub.2 --R.sub.7 or --CO--OR.sub.7, whereinR.sub.7 is C.sub.1 -C.sub.5 alkyl, phenyl or phenyl which is substituted by 1 or 2 halogen atoms or methyl groups, andR.sub.8 is C.sub.1 -C.sub.10 alkoxy or C.sub.1 -C.sub.5 dialkylamino.

Abstract: Substituted 2-benzyl-mercapto-imidazoles and analogs were prepared from the nucleophlic substitution of an appropriately substituted benzoxyacetate with a 2-imidazole mercapto anion or an analog thereof. These compounds were found to be anti-inflammatory agents.

Abstract: 3-(3-Halophenyl)-3,4-diazatetracyclo-[6.3.1.1.sup.6,10.0.sup.1,5 ]tridec-4-en-2-ones are useful as anti-hypoxia agents.

Abstract: Azido-, 4-nitro and 2,4-dinitrophenylhydrazones as well as 4,4'-dihydroxybenzophenone-hydrazone and other hydrazones are disclosed which have antiestrogenic activity useful in treating estrogen-requiring tumor cells. The described hydrazones bind to estrogen receptors in the cytoplasm of tumor cells. The azido-, 4-nitro- and 2,4-dinitro-phenyl branches of the molecules appear to bind to the receptors and prevent translocation of estrogenic information into the nucleus, thereby blocking the synthesis of necessary macromolecules such as proteins. Absence of geometric isomerization from antiestrogenic to estrogenic forms of the drug minimizes estrogenic side-effects.