Abstract: [4S-(4.alpha.,4a.beta.,5.beta.,6.alpha.,7.alpha.,7a.alpha.)]-Octahydro-1H-1 -pyrindine-4,5,6,7-tetrols and [4R-(4.alpha.,4a.alpha.,5.alpha.,6.beta.,7.beta.,7a.beta.)]-octahydro-1H-1 -pyrindine-4,5,6,7-tetrols are useful as inhibitors of alpha-mannosidase and are useful immunostimulants, chemoprotective and radioprotective agents and antimetastatic agents.

Abstract: Adenosine analogues which act selectively at adenosine receptors and which act in general as adenosine antagonists are disclosed. From in vitro studies it is known that specific physiological effects can be distinguished as a result of this selectivity and that adenosine receptor activity in vitro correlates with adenosine receptor activity in vivo.Pharmaceutical preparations of the subject compounds can be prepared on the basis of the selective binding activity of the compounds disclosed herein which will enhance certain physiological effects while minimizing others, such as decreasing blood pressure without decreasing heart rate.

Abstract: The present invention is directed to a group of compounds which are haloethyl substituted steroidal enzyme inhibitors. These compounds are useful as aromatase, 19-hydroxylase, and aldosterone biosynthesis inhibitors and they are prepared from the corresponding epoxide.

Abstract: Substituted (1.alpha.,2.beta.,3.alpha. or .beta.,4.alpha.,5.alpha. or .beta.)-2,3,4-trihydroxy-5-(hydroxymethyl)cyclopentylamines are inhibitors of alpha-mannosidase and alpha-fucosidase and are useful immunostimulants, antiviral and antimetastatic agents.

Abstract: The present invention relates to certain novel 8-substituted purines as selective A.sub.1 -adenosine receptor antagonists which are useful in the treatment of patients suffering from Alzheimer's disease, congestive heart failure or pulmonary bronchoconstriction.

Abstract: The present invention is directed to a group of androstane compounds which contain an ethylene radical bridging the 2- and 19-positions. These compounds are useful as aromatase inhibitors and they are prepared by the cyclization of a 19-[2-(4-toluenesulfonyloxy)ethyl]androst-4-ene-3,17-dione using a strong base.

Abstract: The present invention is directed to 2.beta.,19-(methyleneamino)androst-4-ene-3,17-dione which has the formula ##STR1## and the corresponding 17.beta.-ol which are useful as aromatase inhibitors. The compounds are prepared by the cyclization of an appropriate 19-[N-protected-[(2-methoxyethoxy)methylamino] steroid using titanium tetrachloride followed by, if desired, selective reduction of the 17-ketone.

Abstract: The present invention relates to a group of compounds which are novel squalene derivatives containing the cyclopropyloxy functionality and which act to inhibit the synthesis of cholesterol in mammals and in fungi.

Abstract: The present invention is directed to a group of compounds which are 2,19-methylenoxy or 2,19-methylenethio bridged steroids, and related steroidal compounds. These compounds are useful as aromatase and 19-hydroxylase inhibitors.

Abstract: Adenosine analogues which act selectively at adenosine receptors and which act in general as adenosine antagonists are disclosed. From in vitro studies it is known that specific physiological effects can be distinguished as a result of this selectivity and that adenosine receptor activity in vitro correlates with adenosine receptor activity in vivo. Pharmaceutical preparations of the subject compounds can be prepared on the basis of the selective binding activity of the compounds disclosed herein which can be expected to enhance certain physiological effects while minimizing others, such as decreasing blood pressure without decreasing heart rate.

Abstract: Adenosine analogues which act selectively at adenosine receptors and which act in general as adenosine antagonists are disclosed. From in vitro studies it is known that specific physiological effects can be distinguished as a result of this selectivity and that adenosine receptor activity in vitro correlates with adenosine receptor activity in vivo. Pharmaceutical preparations of the subject compounds can be prepared on the basis of the selective binding activity of the compounds disclosed herein which can be expected to enhance certain physiological effects while minimizing others, such as decreasing blood pressure without decreasing heart rate.

Abstract: The present invention relates to a group of compounds which are novel squalene derivatives containing the cyclopropyloxy functionality and which act to inhibit the synthesis of cholesterol in mammals and in fungi.

Abstract: Xanthine derivative which act selectively at adenosine receptors and which act in general as adenosine antagonists are disclosed. From in vitro studies it is known that specific physiological effects can be distinguished as a result of this selectively and that adenosine receptor activity in vitro correlates with adenosine receptor activity in vivo.Pharmaceutical preparations of the subject compounds can be prepared on the basis of the selective binding activity of the compounds disclosed herein which will enhance certain physiological effects while minimizing others, such as decreasing blood pressure without decreasing heart rate.

Abstract: This invention is directed to a group of compounds which are acyl derivatives of amino substituted triazolopyridazines. They are prepared by the reaction of an aminotriazolopyridazine or an aminotriazolophthalazine with an appropriate acid chloride. These compounds possess bronchodilating and antiallergenic activity.

Abstract: The present invention is directed to a group of compounds which are imidazo[2,1-b]quinazolin-5(3H)-ones, related tricyclic compounds, and pharmaceutically acceptable salts thereof. These compounds are useful as bronchodilators. These compounds are prepared by the reaction of an appropriate hydrazine with an appropriate 1-substituted-2-methyl-2-imidazoline or chemically equivalent compound.

Abstract: 3-(1H-Tetrazol-5-yl)thieno[2,3-d]pyrimidin-4(3H)-ones useful as antiallergic agents are described herein. The compounds are prepared by cyclization of an appropriate substituted amidine using an alkali metal base. The reaction is carried out in an appropriate inert solvent.

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: 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: 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: 2-(Formylamino)-N-(1H-tetrazol-5-yl)benzamide and its pharmaceutically acceptable salts are useful as antiallergic agents. The compounds are prepared by the reaction of 2-amino-N-(1H-tetrazol-5-yl)benzamide with formic acetic anhydride.