Abstract: Amine-carboxyboranes (boron analogues of amino acids) which demonstrate sificant antitumor and antihyperlipidemic (cholesterol and /or triglyceride lowering) activities are disclosed.

Abstract: A method of synthesizing boron analogues of choline and choline related mrials is disclosed. The method comprises reacting N,N dimethylethanolamine with hydrogen chloride or an acid chloride to form an ester hydrochloride. The resulting aminoalcohol hydrochloride or ester hydrochloride is further reacted with tetraethyl NBH.sub.4.Also disclosed are pharamaceutically interesting compounds of acetylcholine.

Abstract: Ester analogues of boron analogues of amino acid are disclosed. Also disced is a method of forming the ester analogues in high yield by condensation of the corresponding acids and alcohols with dicylohexylcarbodiimide at room temperature in dichloromethane. The disclosed compounds have shown interesting biological activities, in particular, hypolipidemic activity as well as significant antitumor and antiarthritic activities.

Abstract: This invention involves amine-carbamoylborane compounds of the formulaR.sub.1 R.sub.2 NH.BH.sub.2 C(O)NHR.sub.3wherein R.sub.1 and R.sub.2 are hydrogen or certain alkyl moieties and R..3 is an alkyl. A process for their preparation involving an amine displacement reaction is also described. A method of use and pharmaceutical compositions containing the subject compounds are also described.

Abstract: A compound of the formula[Cu(R.sub.3 NBH.sub.2 CO.sub.2).sub.2. R.sub.3 NBH.sub.2 CO.sub.2 H].sub.2wherein each R independently represents H, C.sub.1 -C.sub.10 alkyl, or phenyl and L represents a non-toxic Lewis base capable of forming a coordinate bond with the copper with the provisos that any two or three R attached to the same nitrogen may represent a C.sub.4 -C.sub.5 alkylene group containing up to 2 non-cumulative double bonds optionally having 1 or 2 carbons replaced by oxygen or nitrogen, that any 3 R attached to the same nitrogen when taken together with the nitrogen may represent a 6-membered aromatic ring containing 1, 2 or 3 nitrogen atoms, and that any R containing a carbon atom may be substituted with a hydroxyl, ether, ester, carboxyl, or amino functional group is disclosed along with methods of making these compounds and methods of using these compounds as antihyperlipidemic agents and antineoplastic agents.

Abstract: The use of a mine boranes to inhibit the inflammation process is disclosed. hese boranes, which are boron analogs of .alpha.-amino acids, effectively block the following: general inflammation, induced arthritis, and the writhing reflex associated with inflammation pain. The inflammation associated with pleurisy is also inhibited. The boron analogs are shown in vitro to inhibit the release of lysosomal enzymes from liver and polymorphonuclear neutrophils (PMNs). Further, prostaglandin synthesis is blocked by these compounds at a low concentration, viz., 10.sup.-6 M.Liver oxidative phosphorylation processes are also uncoupled by these compounds, but PMN migration is unaltered at 10.sup.-4 M. The elevation of cyclic adenosine monophosphate in PMNs correlates positively with in vivo antiarthritic activity. Studies in rodents demonstrate that these boron analogs may be used at safe therapeutic doses. Several compounds per se are included within the scope of the invention.

Abstract: The use of amine boranes to inhibit the inflammation process is disclosed. These boranes, which are boron analogs of .alpha.-amino acids, effectively block the following: general inflammation, induced arthritis, and the writhing reflex associated with inflammation pain. The inflammation associated with pleurisy is also inhibited. The boron analogs are shown in vitro to inhibit the release of lysosomal enzymes from liver and polymorphonuclear neutrophils (PMNs). Further, prostaglandin synthesis is blocked by these compounds at a low concentration, viz, 10.sup.-6 M.Liver oxidative phosphorylation processes are also uncoupled by these compounds, but PMN migration is unaltered at 10.sup.-4 M. The elevation of cyclic adenosine monophosphate in PMNs correlates positively with in vivo antiarthritic activity. Studies in rodents demonstrate that these boron analogs may be used at safe therapeutic doses. Several compounds per se are included within the scope of the invention.

Abstract: Preparation of the crystalline complex [Na{NH.sub.3.BH.sub.2 -(CN)}.sub.6 from NMe.sub.3.BH.sub.2 I and NaCN in liquid NH.sub.3 is disclosed. Structural details of this novel octahedral complex are obtained by single-crystal X-ray analysis. Evidence indicates that the complex is a valuable antiarthritic agent, since it completely inhibits bacteria-induced chronic arthritis in rats with no evidence of toxic effects. The complex also possesses analgesic and anti-inflammatory activity.