Abstract: The invention relates to a novel ribosome-binding protein derived from Bougainvillea speotabilis having a molecular weight of about 26,000 daltons by polyacrylamide gel electrophoresis under reducing and non-reducing conditions, a ph of about 9.0, and further comprising a specified amino-terminal amino acid sequence, as well as to a conjugate of said protein with a targeting ligand, such as an antibody, to form an immunotoxin. The protein and the conjugate are useful in therapy, for example in the control of tumour calls or viruses.

Abstract: A mammalian growth factor, displaying homology to both basic and acidic fibroblast growth factor in a single polypeptide chain, is disclosed herein. The growth factor was isolated from cells transfected with the DNA extracted from Kaposi's Sarcoma cells.

Abstract: Compounds are provided that inhibit the interaction of an IGF with any one of its binding proteins and not to a human IGF receptor. These IGF agonist compounds, which include peptides, are useful to increase serum and tissue levels of active IGFs in a mammal.

Abstract: There are described novel 4′ substituted 16-membered macrolides and pharmaceutically acceptable compositions comprising a therapeutically effective amount of a compound of the invention in combination with a pharmaceutically acceptable carrier. Also described are a method for treating bacterial infections by administering to a mammal a pharmaceutical composition containing a therapeutically-effective amount of a compound of the invention, and processes for the preparation of such compounds.

Abstract: The present invention discloses new and novel substituted anthracyclines having a three ring system or other DNA binding moieties. These congeners show high activity in vitro against several tumor cell lines. The invention also describes anthracycline-based DNA alkylators.

Abstract: The present invention relates to a method for introducing molecules in cells by disrupting endosomal and lysosomal membranes using photodynamic treatment, without killing the majority of the cells by the photodynamic treatment. More particularly, this invention includes a method for transferring DNA and/or RNA, such as genes, to cells by photochemically inducing the disruption of endosomes and lysosomes.

Abstract: The present invention provides a method of optimizing therapeutic efficacy and reducing toxicity associated with 6-mercaptopurine drug treatment of an immune-mediated gastrointestinal disorder such as inflammatory bowel disease. The method of the invention includes the step of determining the level of one or more 6-mercaptopurine metabolites in the patient having an immune-mediated gastrointestinal disorder.

Abstract: A method and composition for the treatment of HIV and HBV infections in humans and other host animals is disclosed that includes the administration of an effective amount of a [5-carboxamido or 5-fluoro]-2′,3′-dideoxy-2′,3′-didehydro-pyrimidine nucleoside or a [5-carboxamido or 5-fluoro]-3′-modified-pyrimidine nucleoside, or a mixture or a pharmaceutically acceptable derivative thereof, including a 5′ or N4 alkylated or acrylated derivative, or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable carrier.

Abstract: The invention relates to novel disaccharides of formula (I), wherein R1 is selected from the group consisting of hydrogen, linear or branched (C1-C4) alkyl, phenylalkyl with less than ten carbon atoms and —COCH3; R2 is selected from the group consisting of hydrogen, —COCH3 and SO3M; R3 is selected from the group consisting of hydrogen, linear or branched (C1-C4) alkyl, phenylalkyl with less than ten carbon atoms, —COCH3 and y —COPh, Ph being phenyl; G is selected from amongst —COOR4 and —COOM, R4 is selected from the group consisting of hydrogen, (C1-C2)-alkyl and arylalkyl with less than sixteen carbon atom; A is selected from the group consisting of hydrogen, —SO3H, —SO3M and —COCH3; B is selected from the group consisting of hydrogen, —SO3H, —SO3M and —COCH3, wherein either A or B are necessarily either —SO3H or —SO3M, M being a an organic or metallic cation.

Abstract: Physiologically acceptable aqueous solutions and methods for their use are provided. The subject solutions comprise: electrolytes; a dynamic buffering system and an oncotic agent; and do not comprise a conventional biological buffer. The subject solutions find use in a variety of applications, particularly in those applications where at least a portion of a host's blood volume is replaced with a blood substitute.

Abstract: The efficacy of conventional cancer therapies such as surgery, chemotherapy and radiation is enhanced by the use of a therapeutic material which binds to and interacts with galectins. The therapeutic material can enhance apoptosis thereby increasing the effectiveness of oncolytic agents. It can also inhibit angiogenesis thereby moderating tumor growth and/or metastasis.

Abstract: The invention relates to use of ibandronic acid (1-hydroxy-3-(N-methyl-N-pentyl)aminopropyl-1,1-diphosphonic acid) or physiologically compatible salts or esters thereof for improving the osseointegration of cement-free anchored endoprostheses. Ibandronate or salts thereof is applied for a short time immediately after insertion of an endoprosthesis, with the surprising result that secondary stability of the implant is obtained in only 5 weeks or less after the operation.

Abstract: Use of organophosphorus compounds of general Formula (I) for the therapeutic and prophylactic treatment of infections in humans and animals caused by viruses, fungi and parasites.

Abstract: Methods for the utilization of hypocalcemic vitamin D analogs to inhibit the hyperproliferation of malignant or neoplastic cells without incidence of hypercalcemia.

Abstract: This invention generally pertains to the field of psychiatry. In particular, this invention pertains to the discovery that agents capable of inhibiting the binding of cortisol to its receptors can be used in methods for preventing antipsychotic-induced weight gain. Mifepristone, a potent specific glucocorticoid receptor antagonist, can be used in these methods. The invention also provides a kit for preventing AP-induced weight gain in a human including a glucocorticoid receptor antagonist and instructional material teaching the indications, dosage and schedule of administration of the glucocorticoid receptor antagonist.

Abstract: The present invention provides cryptophycin compounds of Formula I that are useful in the treatment of neoplasms.

Abstract: The present invention is to provide a compound or a salt thereof represented by the formula: wherein R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, the ring A is an optionally substituted divalent nitrogen-containing heterocyclic group, X′ is an optionally substituted alkylene chain, Y is an optionally substituted divalent cyclic group, X is a chemical bond or an optionally substituted alkylene chain, and Z is (1) an optionally substituted amino group, (2) an optionally substituted imidoyl group or (3) an optionally substituted nitrogen-containing heterocyclic group, or a pro-drug thereof, which has activated coagulation factor X inhibitory activity and which are useful as anti-coagulants.

Abstract: An objective of the present invention is to provide carbapenem derivatives which have potent antibiotic activity against MRSA, PRSP, Influenzavirus, and &bgr;-lactamase-producing bacteria and are stable against DHP-1. The compounds according to the present invention are compounds represented by formula (I) or pharmaceutically acceptable salts thereof: wherein R1 represents H or methyl; R2 and R3 represent H, a halogen atom, alkyl or the like; and R4 represents substituted lower alkylthio or the like.

Abstract: Compounds of formula (1) or (2), enantiomers thereof, mixtures thereof, and pharmaceutically acceptable salts thereof: wherein: n is 0, or 1; R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl; and R1 is aryl optionally substituted with alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, nitro, aryl, or a monocyclic 5 to 6-membered heteroaryl group, or R is a monocyclic 5 to 6-membered heteroaryl group optionally substituted with alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, nitro, aryl, or a monocyclic 5 to 6-membered heteraryl group, or R is a bicyclic heteroaryl group composed of a monocyclic 5 to 6-membered heteroaryl group fused to a benzene ring, optionally substituted with alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cy

Abstract: This invention relates to triazine compounds of formula (I): R1 is, aryl, or heteroaryl; each of R2, R4, and R5, independently, is Rc, halogen, nitro, nitroso, cyano, azide, isothionitro, SRc, or ORc; R3 is Rc, alkenyl, alkynyl, aryl, heteroaryl, cyclyl, heterocyclyl, ORc, OC(O)Rc, SO2Rc, S(O)Rc, S(O2)NRcRd, SRc, NRcRd, NRcCORd, NRcC(O)ORd, NRcC(O)NRcRd, NRcSO2Rd, CORc, C(O)ORc, or C(O)NRcRd; n is 0, 1, 2, 3, 4, 5, 6, or 7; X is O, S, S(O), S(O2), or NRc; Y is a covalent bond, CH2, C(O), C═N—Rc, C═N—ORc, C═N—SRc, O, S, S(O), or S(O2); Z is N; and W is O, S, S(O), S(O2), NRc, or NC(O)Rc; in which each of Ra and Rb, independently, is H, alkyl, aryl, heteroaryl; and each of Rc and Rd, independently, is H, alkyl, or alkylcarbonyl.

Abstract: Objects of the invention are to provide compounds having excellent activity against interleukin-1&bgr; production and also medicines comprising them as effective ingredients. Pyridazin-3-one derivatives represented by the following formula (1): wherein Ar1 represents a substituted or unsubstituted aromatic group, Ar2 represents a phenyl group having a substituent at least at the 4-position thereof, R1 represents a linear or branched alkyl group, an alkyl group having a cyclic structure, a substituted or unsubstituted phenyl group or a substituted or unsubstituted phenyl(lower alkyl) group, and R2 represents a cyano group, a carboxyl group, a (lower alkoxy)carbonyl group, a substituted or unsubstituted lower alkyl group or a substituted or unsubstituted carbamoyl group, or salts thereof; and medicines comprising them as effective ingredients.

Abstract: This invention relates to novel compounds of Formula (I), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).

Abstract: The present application is directed to compounds having the general formula: and to the use of these compounds in therapeutic methods.

Abstract: The invention relates to novel N-(substituted phenyl)-N′-[&ohgr;-(3-substituted phenyl-4-isoxazolecarbonylamino)alkyl]piperazines, their N-oxides, and pharmaceutically acceptable salts thereof. The compounds are endowed with enhanced selectivity for alpha1-adrenergic receptors and a low activity in lowering blood pressure. The compounds are useful in the treatment of obstructive syndromes of the lower urinary tract, including benign prostatic hyperplasia (BPH), and in the treatment of lower urinary tract symptoms (LUTS) and neurogenic lower urinary tract dysfunction (NLUTD), and other conditions. The compounds may be administered alone or in combination with an anticholinergic compound.

Abstract: The invention relates to the use of derivatives of 3-amidinophenylalanine as urokinase inhibitors for treating malignant tumors and the formation of metastases.

Abstract: Compounds of the formula (I) as well as their pharmaceutically acceptable salts, and pharmaceutical compositions comprising the novel compounds. The novel compounds of the formula (I) are useful in the management of pain.

Abstract: This invention pertains to compounds which specifically inhibit the adenosine A1 receptor and the use of these compounds to treat a disease associated with A1 adenosine receptors in a subject.

Abstract: This invention is directed to dihydropyrimidines which are selective antagonists for human &agr;1a receptors. This invention is also related to uses of these compounds for relaxing lower urinary tract tissue, treating benign prostatic hyperplasia and for the treatment of any disease where the antagonism of the &agr;1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

Abstract: This invention pertains to compounds which specifically inhibit the adenosine A1 receptor and the use of these compounds to treat a disease associated with A1 adenosine receptors in a subject.

Abstract: The present invention provides compositions for controlling plant pests, which contain the compound of the formula (I) in a mixture with fungicidally active compounds, except for cyclopropylcarboxamide derivatives and azolylmethylcycloalkanes.

Abstract: Novel polycyclic compounds of the formula [I], wherein R1, R2, R3, R4, R5, R6, R7, ring A, ring B, X, Y and Z are as defined herein and the pharmaceutically acceptable salts thereof. These compounds have antitumor activity and useful for the treatment of cancer.

Abstract: Crystalline form VII of cabergoline, a pharmaceutical composition containing it and a process for its preparation are disclosed. The process may comprise a slurry procedure using form I or mixture of forms I and VII of cabergoline in a solvent at a temperature above 30° C.

Abstract: The present invention relates to novel 8-azabicyclo[3.2.1]oct-2-ene and -octane derivatives which are found to be cholinergic ligands at the nicotinic Acetyl Choline Receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neurodegeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of chemical substances.

Abstract: Compounds of formula [I] in which: W may represent a —(CH2)2—, —(CH2)3—, —CH2—C≡C— or —CH2—CH═CH— group, R2 may in particular represent a piperidyl group, an optionally substituted 1,2,3,6-tetrahydropyridyl group, a hexahydro-1H-azepinyl group, an optionally substituted piperazinyl group or a morpholinyl group, R3 may in particular represent a group —COR1, A may in particular represent an optionally substituted phenyl group, a heterocycle or a cyclopentyl group, and B may in particular represent a pyridyl group, an aminopyrazinyl group, an aminopyridazinyl group, a pyrimidinyl group optionally substituted with an amino group, piperidyl group or an aminopyridyl group optionally substituted on the pyridine with a (C1-C4)alkyl or (C1-C4)alkoxy group, the amino group possibly also being substituted with a (C1-C4)alkyl group, their preparation and their therapeutic application.

Abstract: This invention provides non-immunosuppressive rapamycin dialdehydes, which are useful as neurotrophic agents, in the treatment of solid tumors, and vascular disease.

Abstract: This invention relates to lactam and thiolactam derivatives having useful anesthetic and conscious sedation activity. Particularly useful compounds include the diethyl lactams such as 3,3-diethyl-2-pyrrolidinone. Methods for using these compounds and pharmaceutical compositions containing these compounds are provided.

Abstract: Disclosed is a method for treating a disorder responsive to the positive modulation of AMPA receptors in animals suffering therefrom, comprising administering to an animal in need thereof a compound of Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein: Y is NH2, NHR, and NHCOR; Z is O and S; and R1, R2, R3, R4, and X are defined herein. These compounds can be used as cognitive enhancers, for the treatment of neurodegenerative diseases, including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, Parkinson's disease, AIDS associated dementia and Down's syndrome as well as for the treatment of schizophrenia and myoclonus. Also disclosed are pharmaceutical compositions useful for treating disorders responsive to the positive modulation of AMPA receptors, and novel compounds of Formula I.

Abstract: The present invention relates to novel imidazolidine derivatives of formula I, wherein A, E, Z, R1, R2, R3, R4 and R5 have the meanings indicated in the claims. The compounds of formula I are valuable pharmaceutical active compounds which are suitable, for example, for the treatment of inflammatory diseases, including rheumatoid arthritis, or allergic diseases. The compounds of formula I are inhibitors of the adhesion and migration of leukocytes and/or antagonists of the adhesion receptor VLA-4 belonging to the integrins group. They are generally suitable for the treatment of diseases which are caused by an undesired extent of leukocyte adhesion and/or leukocyte migration or are associated therewith or in which cell-cell or cell-matrix interactions which are based on the interactions of VLA-4 receptors with their ligands play a role.

Abstract: The present invention relates to amlodipine free base in a crystalline form, to pharmaceutical formulations comprising such material, processes of manufacture and its use in therapy.

Abstract: The invention relates to certain indolinone compounds, their method of synthesis, and a combinatorial library consisting of the indolinone compounds. The invention also relates to methods of modulating the function of protein kinases using indolinone compounds and methods of treating diseases by modulating the function of protein kinases and related signal transduction pathways.

Abstract: Novel compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.

Abstract: The present invention provides cyclopentane heptanoic acid, 2 heteroaryl alkyl or alkenyl derivatives which may be substituted in the 1-position with hydroxyl, alkyloxy, amino and amido groups, e.g. 1-OH cyclopentane heptanoic acid, 2 heteroarylalkenyl derivatives. In particular, these derivatives are 7-[5-hydroxy-2-(heteroatom-substituted hydroxyhydrocarbyl)-3-hydroxycyclopentyl] heptanoic or heptenoic acids and amine, amide, ether, ester and alchohol derivatives of said acids wherein one or more of said hydroxy groups are replaced with an ether group. These compounds are potent ocular hypotensive and are particularly suited for the management of glaucoma.

Abstract: Compounds having therapeutic utility are of formula (I) B—X—(CH2)n—CR2R3—CR4R5—COY  (I) wherein n=0-1; X is S(O)0-2; Y is OR1 or NHOH; R2 and R4 are independently H or a group (optionally substituted with R10) selected from C1-6 alkyl, C2-6 alkenyl, aryl, C1-6 alkyl-aryl, heteroaryl, C1-6 alkyl-heteroaryl, heterocycloalkyl, C1-6 alkyl-heterocycloalkyl, cycloalkyl and C1-6 alkyl-cycloalkyl; and R1, R3 and R5 are independently H or C1-6 alkyl, provided that not more than two of R2, R3, R4 and R5 are H; or any of CR2R3, CR4R5 and CR2—CR4 is a cycloalkyl or heterocycloalkyl ring optionally substituted with R10 or a group (optionally substituted with R10) selected from C1-6 alkyl, aryl, C1-6 alkyl-aryl, heteroaryl and C1-6 alkyl-heteroaryl; B is heterocycloalkyl (optionally substituted by R6 or R7) bonded through carbon to X, or C1-6 alkyl-heterocycloalkyl (optionally substituted with R6 or R7), or a group (substituted with R6) selected from C1-8 alkyl

Abstract: 15-fluoro substituted analogs of PGF2&agr; and methods of their use in treating glaucoma and ocular hypertension are disclosed.

Abstract: This invention provides a drug combination comprised of a thyroid hormone receptor beta agonist with a fibrate in therapeutically effective amounts, which is useful for reducing cholesterol synthesis, lowering plasma cholesterol levels and lowering plasma triglyceride levels.

Abstract: Atorvastatin and pravastatin may be destabilized by the environmental factors, their degradation may also be accelerated by interactions with other pharmaceutical ingredients, such as fillers, binders, lubricants, glidants and disintegrating agents, therefore the pharmaceutical ingredients and the process for preparation of the pharmaceutical formulation should be meticulously chosen to avoid the aforementioned undesired interactions and reactions. The present invention relates to a stable solid pharmaceutical formulation for the treatment of hypercholesterolemia and hyperlipidemia. More precisely, the present invention relates to the new stable solid pharmaceutical formulation containing as an active ingredient, an HMG-CoA reductase inhibitor, such as atorvastatin and pravastatin and pharmaceutically acceptable salts thereof.

Abstract: The invention provides for methods of monitoring the proliferation of cultured prostate cancer cells in the presence of quercetin, methods of treating an individual with prostate cancer or at risk of developing prostate cancer, and methods of reducing the risk of recurrence of prostate cancer in an individual who had previously been treated for prostate cancer. Methods of the invention further include treating an individual with benign prostatic hyperplasia (BPH) with quercetin as well as methods of screening for compounds that inhibit the proliferation of prostate cancer cells. The invention provides for compositions and articles of manufacture containing quercetin in particular formulations, and quercetin with a second compound that also exerts an effect on the androgen receptor.

Abstract: The instant invention is a method of using certain analogs of glutamic acid and gamma-aminobutyric acid to relieve the pain associated with renal colic.

Abstract: The present invention relates to a method of treating hair loss comprising administering a composition having a cardiac-sparing compound characterized by the structure: and pharmaceutically acceptable salts, hydrates, and biohydrolyzable amides, esters, and imides thereof. In this compound, n may be an integer from 1 to 3; R1 and R2 may each, independently, be a hydrogen or lower alkyl; R4 may be hydrogen, lower alkyl or cycloalkyl; R6 and R9 may each, independently, be hydrogen or lower alkyl; R7 and R8 may each, independently, be hydrogen, lower alkyl, substituted phenyl, or substituted benzyl; R10 may be hydrogen, lower alkyl, cycloalkyl, or acyl; and R11 may be hydrogen, lower alkyl, or cycloalkyl.

Abstract: The present invention relates to new substituted salicylic acid salts of salmeterol, processes for preparing them and their use