Abstract: A novel bone prosthesis for use in healing a bone fracture is disclosed comprising a strong, rigid non-absorbable structural member and a biologically absorbable element held in use under compression against the structural member. Use of the novel prosthesis combines an excellent initial stabilization of the fixed fracture with a gradual shifting of stress-bearing from the prosthesis to the bone in the fracture region as the fracture heals. Thus, problems associated with stress-shielding during healing are alleviated. The structural member may be, e.g., a bone plate, intramedullary rod or hip nail.

Abstract: A novel formulation of bacampicillin for oral administration is disclosed. Microcapsules comprising an acid addition salt of bacampicillin coated with a mixture of ethyl cellulose:water-soluble or water-permeable filler material are suspended in a buffered vehicle having a pH of at least 6.9. The novel suspension is characterized by palatable taste, surprisingly good stability and enhanced bioavailability after oral administration. The novel suspension is well suited for multiple dose oral administration. The preferred filler material is hydroxypropyl cellulose.

Abstract: Certain novel derivatives of N-(2-pyridyl)-2-methyl-4-hydroxy-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide have been prepared, including N-(2-pyridyl)-2-methyl-4-acetoxy-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide, N-(2-pyridyl)-2-methyl-4-(n-butyryloxy)-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide, N-(6-methyl-2-pyridyl)-2-methyl-4-acetoxy-2H-1,2-benzothiazine-3-carboxami de 1,1-dioxide, N-(2-pyridyl)-2-methyl-4-benzoyloxy-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide, N-(6-methyl-2-pyridyl)-2-methyl-4-benzoyloxy-2H-1,2-benzothiazine-3-carbox amide 1,1-dioxide, N-(2-pyridyl)-2-methyl-4-methanesulfonyloxy-2H-1,2-benzothiazine-3-carboxa mide 1,1-dioxide and N-(6-methyl-2-pyridyl)-2-methyl-4-methanesulfonyloxy-2H-1,2-benzothiazine- 3-carboxamide 1,1-dioxide. All these compounds are useful in therapy as non-steroidal anti-inflammatory agents, especially when administered by the topical route of administration. Methods for preparing these compounds from known starting materials are provided.

Abstract: A series of spiro-imide compounds and their base salts with pharmacologically acceptable cations are disclosed. These particular compounds are useful in therapy as agents for the control of certain chronic diabetic complications. Preferred member compounds include 2,3-dihydro-spiro-[1H-indene-1,3'-pyrrolidone]-2',5'-dione, 2,3-dihydro-spiro-[1H-indene-2,3'-pyrrolidine]-2',5'-dione, 3,4-dihydro-spiro-[2H-naphthalene-1,3'-pyrrolidine]-2',5'-dione, 3,4-dihydro-spiro-[2H-naphthalene-1,3'-piperidine]-2',6'-dione, 6-chloro-2,3-dihydro-spiro-[4H-1-benzopyran-4,3'-pyrrolidine]-2',5'-dione and 6,7-dihydro-spiro-[5H-benzo(b)thiophene-4,3'-pyrrolidine]-2',5'-dione. Methods for preparing these compounds from known starting materials are provided.

Abstract: Novel spiro-oxazolidindiones useful as aldose reductase inhibitors and as therapeutic agents for the treatment of chronic diabetic complications are disclosed. Pharmaceutical compositions containing the novel compounds and a method of treating chronic diabetic complications are also disclosed.

Abstract: A series of substituted phenylacetic acid compounds and their derivatives, including the pharmacologically acceptable base salts of said acids, have been found to be active as oral hypoglycemic agents. Preferred member compounds include 6-ethoxy-1,2,3,4-tetrahydronaphthalene-1-carboxylic acid, 6-benzyloxy-1,2,3,4-tetrahydronaphthalene-1-carboxylic acid, chroman-4-carboxylic acid, p-chlorophenylacetic acid, o-methylphenylacetic acid, o-methoxyphenylacetic acid, p-methoxyphenylacetic acid and .alpha.,.alpha.-di(4-methoxyphenyl)acetic acid. Synthetic routes leading to those member compounds which are novel per se are described in some detail.

Abstract: Certain novel schistosomicidal pharmaceutical compositions are disclosed. These compositions involve the concomitant use of two different organic chemical compounds each chosen from a separate class of known schistosomicidal agents. One class of agents involves certain known 2-aminoalkyl-7-substituted-1,2,3,4-tetrahydroquinolines (A), while the other class is primarily concerned with a series of known 2-acyl-4-oxo-1,2,3,6,7,11b-hexahydro-4H-pyrazino[2,1a]isoquinoline derivatives (B). A preferred embodiment involves the use of dl-6-hydroxymethyl-2-isopropylaminomethyl-7-nitro-1,2,3,4-tetrahydroquinol ine (A) in conjunction with 2-cyclohexylcarbonyl-4-oxo-1,2,3,6,7,11b-hexahydro-4H-pyrazino[2,1a]isoqui noline (B). Various methods for administering these compounds in combination and/or in a concomitant manner are provided.

Abstract: An adjustable annular prosthesis for use in the surgical correction of atrioventricular orifice defects is disclosed and claimed.

Abstract: Compounds having the formula ##STR1## wherein ##STR2## R.sub.1 is hydrogen, benzyl or alkanoyl, X is C.sub.2-4 alkylene; andZ-W is alkyl, phenylalkyl or pyridylalkyl which can have an oxygen atom as part of the alkyl chain and their use as CNS agents, antidiarrheals and antiemetics. Processes for their preparation and intermediates therefor are described.

Abstract: Compounds useful for pharmacological and medicinal purposes having the formulae ##STR1## wherein R is H, C.sub.1 -C.sub.5 alkanoyl; R.sub.1 is H, benzyl, C.sub.1 14 C.sub.5 alkanoyl, P(O)(OH).sub.2, --CO(CH.sub.2).sub.2 COOH or a basic acyl group; each of R.sub.2 and R.sub.4 is H, C.sub.1 -C.sub.6 alkyl, phenyl, pyridyl or (CH.sub.2).sub.y C.sub.6 H.sub.5 ; y is 1-4; R.sub.3 is H or CH.sub.3 ; Z is C.sub.1 -C.sub.13 alkylene or --(alk.sub.1).sub.m --O--(alk.sub.2).sub.n --; each of (alk.sub.1) and (alk.sub.2) is C.sub.1 -C.sub.13 alkylene with the proviso that the summation of carbon atoms in (alk.sub.1) plus (alk.sub.2) is not greater than 13; each of m and n is 0 or 1; and W is H, pyridyl, phenyl, fluorophenyl or chlorophenyl; intermediates therefor and methods for their preparation and use.

Abstract: Compounds useful for pharmacological and medicinal purposes having the formulae ##STR1## wherein R is H, C.sub.1 -C.sub.5 alkanoyl; R.sub.1 is H, benzyl, C.sub.1 -C.sub.5 alkanoyl, P(O)(OH).sub.2, --CO(CH.sub.2).sub.2 COOH or a basic acyl group; each of R.sub.2 and R.sub.4 is H, C.sub.1 -C.sub.6 alkyl, phenyl, pyridyl or (CH.sub.2).sub.y C.sub.6 H.sub.5 ; y is 1-4; R.sub.3 is H or CH.sub.3 ; Z is C.sub.1 -C.sub.13 alkylene or --(alk.sub.1).sub.m --O--(alk.sub.2).sub.n --; each of (alk.sub.1) and (alk.sub.2) is C.sub.1 -C.sub.13 alkylene with the proviso that the summation of carbon atoms in (alk.sub.1) plus (alk.sub.2) is not greater than 13; each of m and n is 0 or 1; and W is H, pyridyl, phenyl, fluorophenyl or chlorophenyl; intermediates therefor and methods for their preparation and use.

Abstract: A series of novel spiro-imidazolone compounds and their pharmaceutically acceptable acid addition salts are disclosed. These particular compounds are useful in therapy as agents for the control of certain chronic diabetic complications. 3',4'-Dihydro-spiro-[imidazolidine-4,1'(2'H)naphthalene]-5-one represents a typical and preferred member compound. Methods for preparing all these compounds from known hydantoin starting materials are provided.

Abstract: Erythromycylamine 11,12-carbonate, its 2'-acetyl-, 2'-propionyl- and 2'-(3-carbethoxypropionyl)-derivatives; N-(carbobenzoxy)-derivatives and pharmaceutically acceptable acid addition salts of said compounds; their use as antibacterial agents; and processes for their preparation.

Abstract: A series of phenylguanidine base compounds and their pharmaceutically acceptable acid addition salts have been found to be active as oral hypoglycemic agents. Preferred member compounds include N,N'-diphenyl-1-pyrrolidinocarboxamidine, N-phenyl-N'-methyl-N'-phenyl-1-pyrrolidinocarboxamidine and N-phenyl-N'-(p-chlorophenyl)-1-pyrrolidinocarboxamidine, and their hydrohalide acid addition salts. Synthetic routes leading to these compounds are described.

Abstract: A series of novel 4-amino-6,7-di(lower alkoxy)-2-(4-substituted piperazino)quinazoline derivatives have been prepared, including their pharmaceutically acceptable acid addition salts. These derivatives all possess a benzo-oxacycloalkanoyl moiety located at the 4-position of the piperazine ring. Such compounds are useful in therapy as highly potent antihypertensive agents. 4-Amino-2-[4-(chroman-2-carbonyl)piperazino]-6,7-dimethoxyquinazoline represents a typical and preferred member compound. Methods for preparing all these compounds from known starting materials are provided and the principal synthetic route leading to the desired final products is described in some detail.

Abstract: A novel combination of a bone implant, e.g. a bone staple, and a tissue retention element in sliding relation therewith is disclosed. The tissue retention element is provided with a multiplicity of teeth capable of piercing and holding in place adjacent soft tissue when the implant is driven into the bone structure of a patient. Since the tissue retention element is separable from the implant, the same element can be used in combination with different bone implants.

Abstract: Magnetic material comprising magnetic iron oxide modified with at least about 0.5 weight % cobalt, based on the weight of total product which when combined with a binder at a 75% by weight loading forms a magnetic recording member having an orientation ratio and coercivity value that corresponds to a coordinate value equal to or above the coordinate values on the FIGURE and an M-factor value between about -1.0 and +1.0. The magnetic material is preferred in which the amount of cobalt present is from about 0.5 to about 5.0 weight % based on the weight of total product and in which chromium is also present in an amount of from about 0.1 to about 0.3 weight percent based on the weight of total product. A magnetic impulse record member having such a magnetic material dispersed in a binding medium is also claimed.

Abstract: 5-Keto-L-ascorbic acid-5,5-dimethyl ketal, alkali metal and alkaline earth metal salts thereof; process for the preparation thereof; its use as an antioxidant and intermediate for production of 5-keto-L-ascorbic acid and L-ascorbic acid. 5-Keto-L-ascorbic acid and its 5,5-dimethyl ketal exhibit antiscorbutic activity.

Abstract: Novel 3-(1-Imidazolylalkyl)indoles and the pharmaceutically acceptable acid addition salts thereof are disclosed. The novel compounds are useful in selectively inhibiting the action of the thromboxane synthetase enzyme without significantly inhibiting the action of the prostacycline synthetase or cyclooxygenase enzymes and are thus of value as therapeutic agents for the treatment of ischaemic heart disease, stroke, transient ischaemic attack, thrombosis, migraine and the vascular complications of diabetes.

Abstract: Novel guanylamidines and the pharmaceutically acceptable acid addition salts thereof having activity as hypoglycemic agents are disclosed.