Abstract: A cDNA clone having a base sequence for human tissue factor inhibitor (TFI) has been developed and characterized and the amino acid sequence of the TFI has been determined.

Abstract: Chimeric proteins possessing Kunitz-type domain 1 of TFPI-2 and Kunitz-type domain 2 of TFPI are disclosed, as are muteins of TFPI and TFPI-2. Nucleic acid sequences, expression vectors and transformed host cells encoding and capable of producing the disclosed chimeric proteins and muteins are also disclosed. Finally, methods for prevention and treatment of septic shock using the chimeric proteins and muteins are disclosed.

Abstract: The present invention relates to compounds of the formula wherein X is N3, NH2, NHR, N(R)2, CN, SH, SR, or OR1; R is C1-C4 alkyl or (CH2)n—&phgr;; n is an integer 0, 1, 2, 3 or 4; &phgr; is a phenyl group unsubstituted or substituted with from 1 to 3 substituents, each substituent is independently selected from the group consisting of C1-C4 alkyl, C1-C4 alkoxy, halogen, CF3, OCF3, OH, CN, NO2 or NH2; R1 is C1-C4 alkyl or (CH2)m—NR2R3; m is an integer 1, 2, 3 or 4; R2 and R3 are each independently C1-C4 fluorinated akyl or cycloalkyl; The X substituent on the cyclopentanyl ring is in the TRANS configuration relative to the bicyclic substituent; Y is nitrogen; Z1 and Z2 are each independently hydrogen, halogen or NH2; and ---- represents a singe or double bond; or pharmaceutically acceptable salts thereof, compositions comprising such compounds, and methods of treatment comprising administering of such compounds.

Abstract: This invention relates to Trans cyclopentanyl purine analogs of the formula (1) wherein the substituent in the 3-position on the cyclopentanyl ring is in the Trans configuration relative to the bicyclic substituent, Y3, Y5 Y7, Y9 are each nitrogen and Y8 is a CH group, R is a hydrogen, a C1-C7 alkyl acyl or aryl acyl, Q is NH2, halogen or hydrogen, Z is hydrogen, halogen, or NH2; or a pharmaceutically-acceptable salt thereof, and to their use as immunosuppressants.

Abstract: The present invention relates to novel 9-N-bicyclic nucleoside agents which are useful as selective inhibitors of proinflammatory cytokines.

Abstract: The use of 4-H-1-benzopyran-4-one derivatives as inhibitors of smooth muscle cell proliferation. Smooth muscle cell (SMC) proliferation is a critical component of neointimal formation in many animal models of vascular injury, and in many human lesions as well. Cell cycle inhibition by gene transfer techniques can block SMC proliferation and lesion formation in many animal models, although these methods are not yet applicable to the treatment of human disease. Flavopiridol is a recently identified, potent, orally available cyclin-dependent kinase inhibitor. Given the role of smooth muscle cell (SMC) proliferation in vascular disease, we tested the effects of flavopiridol, a recently identified cyclin-dependent kinase inhibitor, on SMC growth in vitro and in vivo. Flavopiridol (75 nmol/L) potently blocked SMC proliferation, an effect that was associated with downregulation of cyclin-dependent kinase activity and cell cycle-related gene expression.

Abstract: The present invention relates to cyclic peptide analogs containing a pseudo-bond, useful as platelet aggregation inhibitors. An example of a compound of this invention includes Cyclo[Ala.PSI.[CH.sub.2 NH]-Arg-Gly-Asp-.delta.-Glu](NHBn).cndot.CF.sub.3 CO.sub.2 H. These compounds inhibit the binding of fibrinogen to the platelet GPIIb-IIIa integrin receptor which inhibits platelet aggregation and therefore these compounds act as potent antithrombotics.

Abstract: This invention relates to polyfluoroalkyl tryptophan tripeptides and to compositions containing them. The compounds are highly selective thrombin inhibitors which provide anticoagulant effects useful in the treatment of thrombin conditions and in preventing the coagulation of stored whole blood and blood products.

Abstract: A process of converting a hydroxy heteroaromatic compound to an arylamine, comprising the steps of:(1) treating a salt of a hydroxy heteroaromatic compound with an alkylating agent; and(2) treating the reaction mixture with a Smiles solvent system and raising the temperature of the reaction mixture; andA compound made according to the above process.

Abstract: This invention relates to peptide derivatives which are useful anticoagulant agents.

Abstract: The present invention describes certain alkyloxyamino-substituted fluorenones which inhibit protein kinase C, as well as pharmaceutical compositions including these compounds and methods of using these compounds to control protein kinase C activity in mammals, including humans. More specifically, the present compounds are useful for the treatment of neoplastic disease states, disorders associated with abnormal blood flow (including hypertension, ischemia, atherosclerosis, coagulation disorders), and inflammatory diseases (including immune disorders, asthma, lung fibrosis, and psoriasis).

Abstract: A method of lowering plasma cholesterol level in a patient with hypercholesterolemia, by administration of a compound of formula (1) ##STR1## wherein: R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each independently a C.sub.1 -C.sub.6 alkyl group;Z is a thio, oxy or methylene group;A is a C.sub.1 -C.sub.4 alkylene group; andR.sub.5 is a C.sub.1 -C.sub.6 alkyl or --(CH.sub.2).sub.n --(Ar)wherein n is an integer 0, 1, 2 or 3; and Ar is phenyl or napthyl unsubstituted or substituted with one to three substituents selected from the group consisting of hydroxy, methoxy, ethoxy, chloro, fluoro or C.sub.1 -C.sub.6 alkyl.

Abstract: The combination of compounds of formula I and II can be used for the treatment of retroviraI infections. The combination can be used to treat AIDS and ARC and other diseases caused by the retrovirus HTV or other related viruses.

Abstract: This invention relates to Trans cyclopentanyl purine analogs of the formula (1) ##STR1## wherein the substituent in the 3-position on the cyclopentanyl ring is in the Trans configuration relative to the bicyclic substituent,Y.sub.3, Y.sub.5, Y.sub.7, Y.sub.8 and Y.sub.9 are each nitrogen,R is a hydrogen, a C.sub.1 -C.sub.7 alkyl acyl or aryl acyl,Q is NH.sub.2, halogen or hydrogen,Z is hydrogen, halogen, or NH.sub.2 ;or a pharmaceutically-acceptable salt thereof, and to their use as immunosuppressants.

Abstract: This invention relates to Trans cyclopentanyl purine analogs of the formula (1) ##STR1## wherein the substituent in the 3-position on the cyclopentanyl ring is in the Trans configuration relative to the bicyclic substituent,Y.sub.3, Y.sub.5 and Y.sub.9 are each nitrogen and Y.sub.7 and Y.sub.8 are a CH group,R is a hydrogen, a C.sub.1 -C.sub.7 alkyl acyl or aryl acyl,Q is NH.sub.2, halogen or hydrogen,Z is hydrogen, halogen, or NH.sub.2 ;or a pharmaceutically-acceptable salt thereof, and to their use as immunosuppressants.

Abstract: This invention relates to novel Trans cyclopentanyl purine analogs of the formula (1) ##STR1## wherein the substituent in the 3-position on the cyclopentanyl ring is in the Trans configuration relative to the bicyclic substituent,Y.sub.3 and Y.sub.8 are CH, Y.sub.5, Y.sub.7 and Y.sub.9 are each independently nitrogen,R is a hydrogen, a C.sub.1 -C.sub.7 alkyl acyl or aryl acyl,Q is NH.sub.2, halogen or hydrogen,Z is hydrogen, halogen, or NH.sub.2 ;or a pharmaceutically-acceptable salt thereof, and to their use as immunosuppressants.

Abstract: Synthetic pulmonary surfactants having antioxidant properties consisting of a complex of a polypeptide of 3-4 amino acid residues, with an antioxidant moiety, and a lipid consisting of one or more of the lipids associated with natural pulmonary surfactant were prepared. These surfactants are useful in the treatment of respiratory distress syndrome.

Abstract: Synthetic pulmonary surfactant consisting of a complex of a polypeptide of 3-4 amino acid residues having alpha-helical structure and a covalently bound long chain acyl group. The peptides are useful when consisting of one or more associated lipids in combination in conditions associated with respiratory distress.

Abstract: Various peptides having affinity for sulfated polysaccharides such as heparin, dextran sulfate and Pentosan polysulfate are bound to resins and used in affinity chromatography to prepare anti-HIV sulfated polysaccharides.

Abstract: A method for controlling the growth of tumor tissues, especially small cell lung. Treatment comprises administering to a patient in need thereof, an effective amount of a bombesin/GRP type inhibitor.Antagonists of bombesin/GRP which are derivatives of naturally occurring bombesin/GRP possessing a thiomethylene or methylene sulfoxide bond connecting the two amino acids on the carboxy terminal end is modified are described. The antagonism is confirmed using conventional competitive binding and biochemical assays as well as conventional physiological tests and the use of these derivatives in a variety of conditions in which bombesin/GRP is implicated is also described.