Abstract: A method for blocking platelet adhesion to collagen by contacting platelets with a polypeptide having one of the following sequences:NH.sub.2 (Ch) Ala Arg Gly Asp (Cx) COOH (i)NH.sub.2 (Ch) Ala Ala Gly Asp (Cx) COOH (ii)NH.sub.2 (Ch) Ala Arg Tyr Asp (CX) COOH (iii)NH.sub.2 (Ch) Ala Arg Gly Asp (Cy) Z (iv)wherein Ch, Cx, Cy are defined amino acid sequences or conservatively substituted amino acid sequences, and Z is NH.sub.2 or COOH.

Abstract: A rapidly hydrating welan gum useful for preparing cementitious products. The gum can be dry blended with cement or other dry component and then added to a preformed cement/water pre-mix, thereby alleviating the need for hydrating the gum prior to addition to a cement/water mixture.

Abstract: The new heteropolysaccharide S-657, prepared by fermentation of a new strain of Xanthomonas campestris, ATCC 53159, has valuable properties as a thickening, suspending and stabilizing agent in aqueous solutions and is especially valuable for use in well treating fluids.Heteropolysaccharide S-657 is composed principally of carbohydrate, about 12% protein and about 7% (calculated as O-acetyl) acyl groups, the carbohydrate portion containing about 19% glucuronic acid, and the neutral sugars rhamnose and glucose in the approximate molar ratio of 2:1.

Abstract: Incubation of ##STR1## with a preparation from mammalian organ yields as biotransformation products the 6-hydroxymethyl and 5-(1-hydroxy)ethyl anologs. These products are useful in the prevention or treatment of infection by HIV and the treatment of AIDS.

Abstract: An efficient process for stereoselective preparation of a medicinally significant hydroxyamide compound of structural formula: ##STR1## comprises the addition of metalated amide enolates to chiral .alpha.-amino metalated epoxides. The hydroxyamide reaction products are useful as inhibitors of the HIV protease or of renin, or as intermediates in the preparation of inhibitors of the HIV protease or renin.

Abstract: A novel heteropolysaccharide S-184 is disclosed. The compound is a gum produced under suitable conditions by the novel microorganism Alcaligenes sp. This new heteropolysaccharide is composed primarily of carbohydrate as uronic acid (7% to 16%) and mannose, glucose, and galactose in the molar ratio of 1:3:5. The non-carbohydrate portion contains 12-16% protein and 3-4.5% acyl groups. The compound is used to alter viscosity and rheology of aqueous solutions.

Abstract: A process for the conversion of FK-506 (I,R=allyl;1) to FK-525 (XV) and analogous 23-membered ring macrolides differing in the C.1-N.7 segment of the molecule (e.g. XVI) and is also applicable to the analogs FK-523 (XVII) and FK-520 (XVIII). The overall process consists of three stages: (a) initial degradation of the primary macrolide to an acyclic fragment containing a selectively protected C.10-C.34 framework with a protected aldehyde function at C.10 and a free hydroxyl function at C.26, (b) reacylation of the C.26 hydroxyl function with an appropriately N-protected alpha-amino acid moiety, and (c) reintroduction of the C.8 and C.9 carbons followed by regeneration of the FK-macrolide system.

Abstract: A child resistant unit dose package for medications comprises a container member having concealed locking means, a plurality of cavities along its longitudinal axis for holding medication, each cavity closed with a peel-off seal, and a cover for the container member that requires two operations to open. In another embodiment, a separate drug container is disclosed which does not include a cover.

Abstract: Amino O-alkyl, O-alkenyl and O-alkynylmacrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by alkylation and amination at C-3"/C-4" of the cyclohexyl ring. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases and/or the prevention of rejection of foreign organ transplants. In addition, these macrolide immunosuppressants are useful in the topical treatment of inflammatory and hyperproliferative skin diseases and cutaneous manifestations of immunologically-mediated illnesses. Also, these macrolides are useful in the treatment of reversible obstructive airways disease, particularly asthma.

Abstract: Selected 17.beta.-Polyaroyl-4-aza-5.alpha.-androst-1-en-3-ones as steroidal reductase inhibitors of the formula: ##STR1## wherein R is selected from hydrogen, methyl and ethylR.sup.2 is polycyclic aromatic radical which can be substituted with one or more of: --OH, protected --OH, --OC.sub.1 --C.sub.4 alkyl, C.sub.1 -C.sub.4 alkyl, or nitro, wherein the doted line represents a double bond which can be present, and pharmaceutically acceptable salts or esters thereof, and a pharmaceutical formulation. The above compounds are active as steroidal reductase inhibitors and thus are useful topically for treatment of acne, seborrhea, female hirsutism, and systemically in treatment of benign prostatic hypertrophy.

Abstract: A non-sticky, fat-containing confection which has a smooth texture and which is quick setting, comprising sugar, fat and gellan gum.

Abstract: A process is described for the improved synthesis of the optically pure C.sub.10 -C.sub.18 fragment of the macrolide structure of the immunosuppressant FK-506. This compound is also useful as an intermediate for preparing FK-506 derivatives.

Abstract: A composition and its method of use are disclosed for controlling rheology of an aqueous dye, which composition comprises 1-30 parts of a gum selected from the group consisting of xanthan gum, rhamsan gum, welan gum and mixtures thereof and 70-99 parts of a water soluble polysaccharide having aliginate equivalent rheology, preferably an alginate. Also disclosed is a color imparting composition for fabric or carpet printing which comprises 99-99% of an aqueous dye component and 1-10% of the rheology control component. The polysaccharide is preferably an alginate, starch, cellulosic polymer or guar gum or mixtures thereof.

Abstract: Specific 17.beta.-thiobenzoyl-4-aza-5.alpha.-androst-1-en-3-ones as antiandrogenic agents of the formula: ##STR1## wherein R is selected from hydrogen, methyl and ethyl andR.sup.2 is phenyl substituted with one or more of: --SH, --SC.sub.1 --C.sub.4 alkyl, --SO--C.sub.1 --C.sub.4 alkyl, --SO.sub.2 --C.sub.1 --C.sub.4 alkyl, --SO.sub.2 N--(C.sub.1 -C.sub.4 alkyl).sub.2, C.sub.1 -C.sub.4 alkyl, --(CH.sub.2).sub.m SH, --S(CH.sub.2).sub.n OCOCH.sub.3, where m is 1-4, n is 1-3, and providing C.sub.1 -C.sub.4 alkyl is only present when one of the above sulfur-containing radicals is present, wherein the dotted line can represent a double bond, and pharmaceutically acceptable esters and salts thereof. Also included is a pharmaceutical formulation thereof. The above compounds are active as antiandrogenic agents and thus are useful topically for treatment of acne, seborrhea, female hirsutism, and systemically in treatment of benign prostatic hypertrophy.

Abstract: 17.beta.-Acyl-4-aza-5.alpha.-androst-1-en-3-ones of the formula: ##STR1## wherein R is selected from hydrogen, methyl and ethyl andR.sup.2 is a monovalent radical selected from straight and branched chain alkyl of from 1-12 carbons, or monocyclic aryl optionally containing 1 or more lower alkyl substituents of from 1-2 carbon atoms and/or 1 or more halo (Cl or Br) substituents, aralkyl selected from benzyl and phenethyl and heterocyclic selected from 2- or 4-pyridyl, 2-pyrrolyl, 2-furyl or thiophenyl;and R', R" and R'" are each selected from hydrogen and methyl and pharmaceutical formulation of the above compounds are active as testosterone 5.alpha.-reductase inhibitors and thus are useful topically for treatment of acne, seborrhea, female hirsutism, and systemically in treatment of benign prostatic hypertrophy.

Abstract: Peptide analogues of human humoral hypercalcemic factor (hHCF) that contain a lactam bridge act as inhibitors of the naturally occurring peptide. A lactam bridge between Lys and Asp situated five residues (inclusive) apart confers rigidity to that region of the peptide, and enhances the helical nature and metabolic stability of the peptide analogue.

Abstract: Described is a process for producing a new immunosuppressant, a C-31 desmethyl, C-19/C-22 cyclic hemiketal biotransformation analog (Compound I) of FR-900520, under novel fermentation conditions utilizing the novel microorganism, Streptomyces, lavendulae ATCC No. 55209. Also disclosed is the C-31 methylated devivative (Compound II) of Compound I produced by enzymatic methylation using 31-O-desmethylimmunomycin O-methyl transferase, (DIMT), a methyl transferase enzyme. The macrolide immunosuppressants are useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow, liver, lung, kidney and heart transplants.

Abstract: Macrolides of the general structural Formula I: ##STR1## have been prepared. These macrolides are antagonists of FK-506-type immunosuppressants and are useful for modifying dosages of FK-506-type immunosuppressants in the treatment of autoimmune diseases, infectious diseases and/or the prevention of rejection of foreign organ transplants. Furthermore, the compounds of the present invention may have utility as antidotes for overdoses of FK-506-type immunosuppressants. In addition, these macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases and/or the prevention of rejection of foreign organ transplants.

Abstract: Novel C-3" and C-4" halogen-substituted macrolides of FK-506 type structural Formula I: ##STR1## are described. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases (such as juvenile-onset diabetes melitus, multiple sclerosis and rheumatoid arthritis), infectious diseases and/or the prevention of rejection of foreign organ transplants, e.g. bone marrow and heart transplants. In addition, these macrolide immunosuppressants are useful in the topical treatment of inflammatory and hyperproliferative skin diseases and cutaneous manifestations of immunologically-mediated illnesses such as: psoriasis, atopical dermatitiis, contact dermatitis and further eczematous dermatitises, seborrhoeic dermatitis, Lichen planus, Pemphigus, bullous Pemphigoid, Epidermolysis bullosa, urticaria, angioedemas, vasulitides erythemas, cutaneous eosinophilias, Lupus erythematosus or Alopecia areata.

Abstract: A class of 5-membered heterocyclic compounds having at least one heteroatom, substituted on the heterocyclic ring by an imidazolyl moiety, are useful in the treatment of psychotic disorders (e.g. schizophrenia and mania); anxiety; alcohol or drug withdrawal or dependence; pain; gastric stasis; gastric dysfunction (such as occurs with dyspepsia, peptic ulcer, reflux oesophagitis and flatulence); migraine, nausea and vomiting; movement disorders; and presenile and senile dementia.