Abstract: Indazole compounds that modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction and thereby modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer and other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.

Abstract: Compounds of the formula: (where R1, R2 and R3 are defined in the specification) are inhibitors of AICARFT. These compounds, as well as their pharmaceutically acceptable salts, solvents, prodrugs, and pharmaceutically active metabolites, are useful in pharmaceutical compositions for treating diseases such as cancer.

Abstract: A method of treating, preventing or inhibiting a disorder selected from the group consisting of cardiovascular or heart related diseases such as stroke, hypertension, tachycardia, and congestive heart failure, osteoporosis, premature birth, psychosocial dwarfism, stress-induced fever, ulcer, diarrhea, post-operative ileus, and colonic hypersensitivity associated with psychopathological disturbance and stress, comprising administering to a mammal, including a human, in need of such treatment a therapeutically effective amount of a compound of the formula or a pharmaceutically acceptable salt thereof, wherein A, B, D, E, Y, Z, R3, R4, and R5 are as defined herein.

Abstract: The invention relates to compounds of the formula I and to pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formula I, methods of using said compounds of formula I in the treatment of infections, and methods of preparing said compounds of formula I.

Abstract: The invention relates to the compounds of the formula 1 and to pharmaceutically acceptable salts thereof, wherein R1, R2, R3, X and Y are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formula 1, methods of using said compounds of formula 1 in the treatment of infections, and methods of preparing said the compounds of formula 1.

Abstract: The invention relates to crystalline 9-E-(O-methyl)oxime of 11,12-dideoxy-3-de(2,6-dideoxy-3-C-methyl-3-O-methyl-&agr;-L-ribohexopyranosyloxy)-6-O-methyl-12,11-(iminocarbonyl-(2-(3-(4-(3-pyridinyl)-1H-imidazol-1-yl)propyl)hydrazono))-3-oxoerythromycin wherein said crystalline compound is as the free base of said compound, the hemihydrate of said compound or the mesylate (methanesufonic acid) salt of said compound. The invention also relates to pharmaceutical compositions containing the foregoing crystalline compound and to methods of treating bacterial and protozoa infections by administering said crystalline compound.

Abstract: Antibacterial quinolone carboxylic acids and naphthyridone carboxylic acids, having an external amino group attached to their 7-substituent are prepared without the use, and subsequent removal, of blocking groups on the external amino group. In a preferred embodiment, the naphthyridone carboxylic acid is the antibiotic trovafloxacin.

Abstract: The invention relates to a monohydrate polymorph PII.M of a compound of the formula ##STR1## exhibiting the following X-ray powder diffraction pattern______________________________________ Peak No. 1 2 3 4 5 6 7 8 ______________________________________ 2.sub.-- .theta..sub.-- (.degree.) Cu 3.6 7.3 13.7 14.5 17.1 21.) 23.6 26.7 d space 24.2 12.2 6.5 6.1 5.2 4.2 3.8 3.3 ______________________________________The invention also relates to methods of preparing the above compound, pharmaceutical compositions containing the above compound, and methods of treating bacterial infections by administering the above compound.

Abstract: The invention relates to a non-hygroscopic polymorph of the following compound ##STR1## and to pharmaceutical compositions containing the above compound, methods of treating bacterial infections by administering the above compound, and to methods of preparing the above compound and related compounds.

Abstract: The invention relates to compounds of the formula (I) ##STR1## and pharmaceutically acceptable salts thereof, wherein Ar, Z and Het are as defined herein. The compounds of formula (I) possess activity as antifungal agents. The invention also relates to pharmaceutical compositions containing said compounds of formula (I) and to methods of treating fungal infections by administering said compounds of formula (I).

Abstract: The invention relates to the trihydrate of the mesylate salt of (1S,2S)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidin-1-yl)-1-propano l, pharmaceutical compositions containing said compound and methods of treating disorders of the central nervous system by administering said compound.

Abstract: An acidic polycyclic ether antibiotic, having structure established by X-ray crystallography, is formed by fermentation of a novel microorganism, Streptomyces sp. ATCC 55028. This novel antibiotic is useful as an anticoccidial in chickens, in the prevention or treatment of swine dysentery, as a growth promotant in cattle and swine, and as an anthelmintic in mammals, particularly in dogs, cats, sheep, cattle and swine.

Abstract: This invention provides processes for producing quinolone compounds which comprise cultivating Amycoa sp. FERM BP-4785, and then isolating quinolone compounds from the fermentation broth. The compounds produced by these processes include compounds of formula (I) wherein R.sup.1 is H, R.sup.2 is (a) and R.sup.3 is CH.sub.3 ; R.sup.1 is CH.sub.3, R.sup.2 is (a) and R.sup.3 is CH.sub.3 ; or R.sup.1 is CH.sub.3, R.sup.2 is (b) and R.sup.3 is CH.sub.3 ; and the like. The present invention also relates to a pharmaceutical composition comprising the same, which is useful in the treatment of diseases, disorders and adverse conditions caused by Helicobacter pylori and is particularly useful in the treatment of gastroduodenal disorders, diseases and adverse conditions caused thereby.

Abstract: An infection with Helicobacter may successfully be treated with a compound of the formula ##STR1## wherein R.sub.1 is hydrogen or methyl and R.sub.2 is hydrogen or L-alanine-L-alanyl, and the pharmaceutically acceptable acid additive salts thereof. These compounds are useful in the treatment of gastric and duodenal ulcers.

Abstract: A compound of the formula ##STR1## or a pharmaceutically acceptable salt thereof; W is hydrogen, (C.sub.1 -C.sub.6)alkyl optionally substituted with from one to three fluorine atoms, --S(O).sub.v --(C.sub.1 -C.sub.6) alkyl wherein v is zero, one or two, halo, benzyloxy or (C.sub.1 -C.sub.6)alkoxy optionally substituted with from one to three fluorine atoms;R.sup.1 is a 4, 5 or 6 membered heterocyclic ring containing from one to three heteroatoms selected from oxygen, nitrogen and sulfur, wherein said heterocyclic ring contains from zero to three double bonds and is optionally substituted with one or two substituents independently selected from (C.sub.1 -C.sub.6) alkyl optionally substituted with from one to three fluorine atoms and (C.sub.1 -C.sub.6) alkoxy optionally substituted with from one to three fluorine atoms;R.sup.2 is hydrogen or --CO.sub.2 (C.sub.1 -C.sub.10)alkyl;R.sup.

Abstract: A method of treating tinnitus in a mammal in need of such treatment, in which the method comprises administering a therapeutically effective amount of a compound of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.1 14 R.sup.4 are as defined herein.

Abstract: Polypeptides isolated from the venom of the Filistata hibernalis spider block calcium channels in cells of various organisms and are useful in blocking said calcium channels in cells, per se, in the treatment of calcium channel-mediated diseases and conditions and in the control of invertebrate pests.

Abstract: The invention relates to compounds of the formula ##STR1## and to pharmaceutically acceptable salts thereof, wherein R.sup.1 is hydrogen, fluoro, or chloro, and R.sup.2 is hydrogen or methyl. The above compounds are lipoxygenase inhibitors. The invention also relates to pharmaceutical compositions containing the above compounds, and to methods of treating inflammatory and allergic conditions by administering the above compounds.

Abstract: The invention provides antifungal compounds of the formula: ##STR1## and pharmaceutically acceptable salts thereof, whereinR is phenyl substituted by 1 to 3 substituents each independently selected from halo, --CF.sub.3 and --OCF.sub.3 ;R.sup.1 is C.sub.1 -C.sub.4 alkyl;R.sup.2 is H or C.sub.1 -C.sub.4 alkyl;X is CH or N; andY is F or Cl.

Abstract: Polypeptides isolated from the venom of the Geolycosa riogrande spider form pores in the plasma membrane of cells and are effective in mobilizing intracellular calcium ions in cells. These polypeptides are useful in such areas as drug delivery, cancer chemotherapy and immunotherapy, as well as in the physiological study of cells.