Abstract: The present invention relates to at least one novel anti-dual integrin antibodies, including isolated nucleic acids that encode at least one anti-dual integrin antibody, dual integrin, vectors, host cells, transgenic animals or plants, and methods of making and using thereof, including therapeutic compositions, methods and devices.

Abstract: The present invention provides CDR-grafted antibodies against human tissue factor that retain the high binding affinity of rodent monoclonal antibodies against tissue factor but have reduced immunogenicity. The present humanized antibodies are potent anticoagulants and are thus useful in the treatment and prophylaxis of human thrombotic disease. The invention also provides methods of making the CDR-grafted antibodies and pharmaceutical compositions for the attenuation or prevention of coagulation.

Abstract: The present invention relates to at least one novel anti-alpha-V subunit antibodies, including isolated nucleic acids that encode at least one anti-alpha-V subunit antibody, alpha-V subunit, vectors, host cells, transgenic animals or plants, and methods of making and using thereof, including therapeutic compositions, methods and devices.

Abstract: The invention provides biologically active erythropoietin (EPO) conjugate compositions wherein EPO is covalently conjugated to a non-antigenic hydrophilic polymer covalently linked to an organic molecule that increases the circulating serum half-life of the composition. The invention thus relates to EPO derivatives described by the formula EPO-(X-Y)N where EPO is erythropoietin or its pharmaceutical acceptable derivatives having biological properties of causing bone marrow cells to increase production of reticulocytes and red blood cells, X is PEG or other water soluble polymers, Y is an organic molecule that increases the circulating half-life of the construct more than the PEG alone and N is an integer from 1 to 15. Other molecules may be included between EPO and X and between X and Y to provide the proper functionality for coupling or valency.

Abstract: The present invention relates to at least one novel RSV proteins, antibodies, including isolated nucleic acids that encode at least one RSV protein or antibody, RSV vectors, host cells, transgenic animals or plants, and methods of making and using thereof, including therapeutic compositions, methods and devices.

Abstract: N-substituted amidine and guanidine oxazolidinone compounds of the formula: in which the substituents have the meaning indicated in the description. These compounds are useful as antibacterial agents.

Abstract: This invention provides novel dithiepino[6,5-b]pyridines of the following formulae. These compounds are useful as calcium channel antagonists with cardiovascular, antiasthinatic and antibronchoconstriction activity. Thus, this invention also provides pharmaceutical compositions, as well as methods, for preventing and treating disorders such as hypersensitivity, allergy, asthma, bronchospasm, dysmenorrhea, esophageal spasm, glaucoma, premature labor, urinary tract disorders, gastrointestinal motility disorders and cardiovascular disorders.

Abstract: The invention relates to methods of synthesizing libraries of diverse and complex highly substituted 2,4-dioxopiperidine compounds of the general formula: wherein R1, R2 and R3 are as herein described, novel intermediates useful for synthesizing such 2,4-dioxopiperidine compounds and methods for identifying and isolating the compounds.

Abstract: An oral contraception regimen which comprises sequentially administering two or more progestational agents exhibiting different effects on the human endometrium in combination with an estrogen. The invention is also directed to an extended use oral contraception regimen comprising the sequential administration of two or more progestational agents in combination with an estrogen.

Abstract: A liquid phase process for preparing GnRH peptide analogs of the formula: G-AA1-(A)D-Phe-AA3-AA4-(R2-AA5-AA6-AA7-AA8-Pro-AA10-NH2   Formula 1 which comprises: (a) reacting a peptide of the formula: T-(R2)AA5-AA6-X  where T is (P2) AA4 orP2 and X is AA7-OH or is —OH, with a peptide of the formula: X′-AA8-Pro-AA10-NH2  or acid-addition salt form thereof, where X′ is AA7 when X is absent and X′ is absent when X is AA7-OH;  in a liquid reaction medium in the presence of a peptide coupling reagent and a strong organic amine base to obtain a product of the formula: T-(R2)AA5-AA6-AA7-AA8-Pro-AA10-NH2 (b) removing the P2 protecting group at the N-terminus, and (c) reacting the product of step (b) or an acid addition salt thereof, with a peptide of the formula: G-AA1-(R1)D-Phe-AA3-T′  or acid-addition salt form thereof, where T′ is AA4-OH when T is absent and is absent when T is P2-AA4, in a liquid reaction medium to obtain a GnRH pepti

Abstract: The preparation of 14-membered macrocycles from a resin-bound orthogonally protected lysine residue is described. Reductive alkylation of the a-nitrogen followed by acylation with an Fmoc-aminoacid provides a protected dipeptide precursor. Removal of the Fmoc-group, acylation with a succinic anhydride, methyltrityl-group removal and macrocyclization provides the desired macrocycles, after TFA cleavage, in excellent yield and purity.

Abstract: There is provided by the present invention liquid injectable and oral solid pharmaceutical dosage forms containing a mixture of cladribine (2-chloro-2′-deoxyadenosine; 2-CdA) and cyclodextrin.

Abstract: A matrix for containing drugs for transdermal delivery systems is disclosed. The matrix, formed of a skin-adhesive acrylate copolymer, attains high rates of drug delivery without the addition of drug delivery rate enhancers. In preferred embodiments the matrix is used to administer steroids, in particular estradiol. Water-soluble polymers may be added as well.

Abstract: A method for preparing liposomal suspensions which comprises preparing a solution of a poorly soluble protein or other poorly soluble compound and an encapsulating amount of a suitable lipid in an alcoholic solvent, injecting the resulting solution into an aqueous solution of appropriate ionic strength, and removing the alcoholic solvent by thin-film evaporation at the transition temperature of the liposomal suspension. This process is suitable for continuous production on an industrial manufacturing scale. It is of particular application in the preparation of KL4 pulmonary surfactant composition, wherein the thin film evaporation is conducted within the transition temperature range of the surfactant (approximately 35-50.degree. C.), thereby enhancing the KL4 peptide insertion into the lipid bilayer and leading to a product with reduced viscosity and enhanced surface tension lowering properties.

Abstract: This invention is directed to certain 1,3- and 2,3-diarylpyrazole antiinflammatory compounds of the general formulae: ##STR1## wherein R.sub.1 and R.sub.2 are independently selected from the group consisting of hydrogen, halogen, (C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkoxy, nitro, amino, hydroxy, trifluoro, --S(C.sub.1 -C.sub.6)alkyl, --SO(C.sub.1 -C.sub.6)alkyl and --SO.sub.2 (C.sub.1 -C.sub.6)alkyl and the fused moiety Q is a group selected from the group consisting of an optionally substituted cyclohexyl and cycloheptyl group as herein described, pharmaceutical compositions containing the compounds, processes for their production and use as COX-2 inhibitor and antiinflammatory agents.

Abstract: This invention relates to the use of compounds of formula I as selective COX-2 inhibitors and antiinflammatory agents: ##STR1## wherein: X and Y are selected from hydrogen, halogen, alkyl, nitro, amino or other oxygen and sulfur containing functional groups such as hydroxy, methoxy and methylsulfonyl.

Abstract: Compounds of Formula I ##STR1## wherein, R.sub.1 through R.sub.7 are described herein. These compounds inhibit the production of arachidonic acid products associated with 5-lipoxygenase and cyclooxygenase and are useful in the treatment of inflammatory disorders.

Abstract: The invention relates to improved liquid phase processes for the preparation of the 21 residue protein component, (Lys-Leu.sub.4).sub.4 -Lys, of the pulmonary surfactant KL-4. These process are amenable to large scale synthesis and one process employs a method of saponifying an ester which reduces the inherent racemization of the .alpha.-carbon.

Abstract: A liquid phase process for preparing GnRH peptide analogs of the formula:G-AA.sub.1 -(A)D-Phe-AA.sub.3 -AA.sub.4 -(R.sub.2)-AA.sub.5 -AA.sub.6 AA.sub.7 -AA.sub.8 -Pro-AA.sub.10 -NH.sub.2Formula 1which comprises:(a) reacting a peptide of the formula:T-(R.sub.2)AA.sub.5 -AA.sub.6 -Xwhere T is (P.sub.2)AA4 orP.sub.2 and X is AA.sub.7 --OH or is --OH, with a peptide of the formula:X'-AA.sub.8 -Pro-AA.sub.10 -NH.sub.2or acid-addition salt form thereof, where X' is AA.sub.7 when X is absent and X' selected from P-Ala, Gly, GABA, the D- and L- isomers of Ala, amino isobutyric acid, 6-amino-hexanoic acid, Ser, Thr, His, Tyr, Asn, and Gln' is absent when X is AA.sub.7 --OH;in a liquid reaction medium in the presence of a peptide coupling reagent and a strong organic amine base to obtain a product of the formula:T-(R.sub.2)AA.sub.5 -AA.sub.6 -AA.sub.7 -AA.sub.8 -Pro-AA.sub.10 -NH.sub.2(b) removing the P.sub.

Abstract: Liquid antacid compositions containing a tri- or di-ester buffer have a reduced final product pH providing for a more efficacious preservative system and better tasting product without compromising to acid neutralization capacity of the antacid.