Abstract: The present invention provides a compound represented by the following formula (I): wherein each symbol is as described in the DESCRIPTION, which has a superior peripheral blood lymphocyte decreasing action, and is useful for the treatment or prophylaxis of autoimmune diseases; prophylaxis or suppression of resistance or acute rejection or chronic rejection of transplantation of organ or tissue; treatment or prophylaxis of graft-versus-host (GvH) disease due to bone marrow transplantation; or treatment or prophylaxis of allergic diseases.

Abstract: There are provided, inter alia, derivatives of seriniquinone and methods useful for the treatment of cancer, and in particular treatment of melanoma and prostate cancer.

Abstract: Several classes of in vivo carbon monoxide-releasing compounds are useful for the treatment and/or prevention of diseases, such as chronic inflammatory, e.g., rheumatoid arthritis, and of diseases with a strong inflammatory component, such as atherosclerosis, stroke, coronary disease, and Alzheimers disease. The in vivo carbon monoxide-releasing compounds can be attached to known drug vectors and/or known anti-inflammatory drugs, such as aspirin.

Abstract: The present invention provides a compound represented by the following formula (I): wherein each symbol is as described in the DESCRIPTION, which has a superior peripheral blood lymphocyte decreasing action, and is useful for the treatment or prophylaxis of autoimmune diseases; prophylaxis or suppression of resistance or acute rejection or chronic rejection of transplantation of organ or tissue; treatment or prophylaxis of graft-versus-host (GvH) disease due to bone marrow transplantation; or treatment or prophylaxis of allergic diseases.

Abstract: The present invention provides a protein cross-linking inhibitor containing a compound represented by any of the following formulas (1)-(13), or a pharmaceutically acceptable salt thereof: R3—[—X—B(ZR1)—Y—B(ZR2)—W—]n—R4,??(1) R3—[—X—B(ZR1)—Y—]n—R4,??(2) R3—[—B(ZR1)—Y—B(ZR2)—W—]n—R4,??(3) R3—[—X—B(ZR1)—]n—R4,??(4) R3—[—B(ZR2)—W—]n—R4,??(5) R3—X—B(ZR1)-T[B(ZR2)—W—R4]2,??(6) R3—B(OH)2,??(7) R3—B(ZR1)—X—B(ZR2)—R4,??(8) R3—B(R1)—O—B(R2)—R4,??(9) R3—[—X—B(ZR1)—Y—B(ZR2)—]n—R4,??(10) R3—[—X—B(ZR1)—Y—B(ZR2)—W-Q-]n—R4,??(11) R3—[—P—X—B(ZR1)—Y—B(ZR2)—W—]n—R4,??(12) [R3—X—B(ZR1)—Y]2B(ZR2),??(13) wherein each symbol is as defined in the DESCRIPTION.

Abstract: The invention is directed to TRPM8 antagonists of Formula (I). More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating TRPM8-mediated disorders. Pharmaceutical and veterinary compositions and methods of treating pain and various other disease states or conditions using compounds of the invention are also described.

Abstract: Disclosed herein are stable formulations suitable for the treatment of glaucoma and ocular hypertension.

Abstract: The present invention is directed to a method for treating or ameliorating asthma in a subject in need thereof comprising administering to the subject a therapeutically effective amount of compound 17:

Abstract: This invention provides novel ?-lactamase inhibitors of the aryl- and heteroaryl-sulfonamidomethylphosphonate monoester class having nitrogen-based cations or quarternary ammomium groups. The compounds inhibit three classes of ?-lactamases and synergize the antibacterial effects of ?-lactam antibiotics (e.g., imipenem and ceftazimdime) against those micro-organisms normally resistant to the ?-lactam antibiotics as a result of the presence of the ?-lactamases.

Abstract: The invention is directed to TRPM8 antagonists of Formula (I). More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating TRPM8-mediated disorders. Pharmaceutical and veterinary compositions and methods of treating pain and various other disease states or conditions using compounds of the invention are also described.

Abstract: The present invention is directed to a compound of formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof, and methods for treating inflammatory and serine protease mediated disorders.

Abstract: This invention provides novel ?-lactamase inhibitors of the aryl- and heteroaryl-sulfonamidomethylphosphonate monoester class. The compounds inhibit three classes of ?-lactamases and synergize the antibacterial effects of ?-lactam antibiotics (e.g., imipenem and ceftazimdime) against those micro-organisms normally resistant to the ?-lactam antibiotics as a result of the presence of the ?-lactamases.

Abstract: The present disclosure provides non-naturally occurring polyphenol compounds that upregulate the expression of Apolipoprotein A-I (ApoA-I). The disclosed compositions and methods can be used for treatment and prevention of cardiovascular disease and related disease states, including cholesterol or lipid related disorders, such as, e.g., atherosclerosis.

Abstract: This invention provides novel ?-lactamase inhibitors of the aryl- and heteroarylsulfonamidomethylphosphonate monoester class having nitrogen-based cations or quarternary ammonium groups. The compounds inhibit three classes of ?-lactamases and synergize the antibacterial effects of ?-lactam antibiotics (e.g., imipenem and ceftazidime) against those micro-organisms normally resistant to the ?-lactam antibiotics as a result of the presence of the ?-lactamases. Formula (I) or pharmaceutically acceptable salt thereof.

Abstract: The present invention is directed to a compound of formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof, and methods for treating inflammatory and serine protease mediated disorders.

Abstract: The present invention is directed to a compound of formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof, and methods for treating inflammatory and serine protease mediated disorders.

Abstract: The invention is directed to TRPM8 antagonists of Formula (I). More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating TRPM8-mediated disorders. Pharmaceutical and veterinary compositions and methods of treating pain and various other disease states or conditions using compounds of the invention are also described.

Abstract: The present invention relates to compounds of formula I which are prodrugs of caspase inhibitors and pharmaceutically acceptable salts thereof. This invention further relates to the release of caspase inhibitors from these compounds through selective bond cleavage. This invention further relates to pharmaceutical compositions comprising these compounds, which are particularly well-suited for treatment of caspase-mediated diseases, including inflammatory and degenerative diseases. This invention further relates to methods for preparing compounds of this invention.

Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.

Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.

Abstract: The invention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.

Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.

Abstract: The invention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel &bgr;-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic &bgr;-lactamase inhibitors presently available, and which do not require a &bgr;-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.

Abstract: The present invention relates to novel &agr;-substituted-&bgr;-aminoethylphosphonate and &agr;-substituted-&bgr;-aminovinylphosphonate derivatives and their uses for lowering plasma levels of apo (a), Lp(a), apo B, apo B associated lipoproteins (low density lipoproteins and very low density lipoproteins) and for lowering plasma levels of total cholesterol.

Abstract: A class of novel benzo(b)thiophene is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of Inflammatory Diseases such as septic shock.

Abstract: This invention relates to an optically active benzothiepin derivative represented by the formula: wherein R represents a lower alkyl group; R1 and R2 independently represent a lower alkyl group, or may bind together to form a ring, which exhibits excellent osteogenesis-promoting action and is useful as a prophylactic or therapeutic drug for bone diseases.

Abstract: Treatment of warm-blooded animals having a tumor or non-malignant hypervascularation, by administering a sufficient amount of a cytotoxic agent formulated into a phosphate prodrug form having substrate specificity for microvessel phosphatases, so that microvessels are destroyed preferentially over other normal tissues, because the less cytotoxic prodrug form is converted to the highly cytotoxic dephosphorylated form.

Abstract: The invention provides therapeutic and biological uses of chemokine-receptor-binding compounds (including chemokine receptor ligands such as chemokine receptor agonists or antagonists), such as benzopyrone derivatives, including uses in the treatment of disease states mediated by chemokines. The relevant chemokine may for example be interleukin-8 (IL-8), and the relevant chemokine receptors may for example be corresponding chemokine receptors (CXCR-1 and/or CXCR-2). In other aspects, the invention provides corresponding pharamaceutical compositions and therapeutic methods. In one aspect, for example, the invention provides for the use of [7-[benzopyrone-5′(3′-amino)-thiazole]-phenylalanine-benyl ester in the treatment of disease.

Abstract: The present invention provides an antiproliferative compound having a structural formula 1

Abstract: The invention provides compounds of the formula: wherein the ring A is an optionally substituted benzene ring; R1 is an optionally substituted non-aromatic heterocyclic group; R2 and R3 are independently hydrogen atom or an optionally substituted hydrocarbon group; n is an integer of 0-3; or salts thereof, which are useful as medicines having an osteogenesis promoting effect and chondrogensis promoting effect. The present invention relates to an amine compound having an excellent effect of inhibiting production and/or secretion of amyloid-b protein, a production and use thereof. Especially, it is effective for preventing and/or treating, for example, neurodegenerative diseases, amyloid angiopathy, neurological disorders caused by cerebrovascular disorders, and so forth.

Abstract: This invention relates to an optically active benzothiepin derivative represented by the formula: wherein R represents a lower alkyl group; R1 and R2 independently represent a lower alkyl group, or may bind together to form a ring, which exhibits excellent osteogenesis-promoting action and is useful as a prophylactic or therapeutic drug for bone diseases.

Abstract: Compounds of the formula ##STR1## in which R.sup.1 is Y or Y--C.sub.1-6 alkyl, where Y is carboxy, tetrazolyl, --SO.sub.2 H, --SO.sub.3 H, --OSO.sub.3 H, --CONHOH, or --P(OH)OR', --PO(OH)OR', --OP(OH)OR' or --OPO(OH)OR' where R' is hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or optionally substituted phenyl-C.sub.1-6 alkyl,and R.sup.2, R.sup.3, R.sup.4, X and Z are as defined in the specification, possess affinity for metabotropic glutamate receptors and are useful in the treatment of disorders of the central nervous system.

Abstract: Phosphoramidates and phosphinic amides and related compounds are provided. Also provided are methods that use the compounds for modulating the activity of the endothelin family of peptides are provided. In particular, compounds having formula: ##STR1## in which A, B, R.sup.1 and R.sup.2 are as described are provided. Also provided are methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these compounds or prodrugs thereof. Methods for elucidating the physiological and pathophysiological roles of endothelin, as well as isolating endothelin receptors are also provided.

Abstract: This invention provides a pharmaceutical composition comprising a non-peptide osteogenic promoting substance and a biodegradable polymer, which can be safely used as a prophylactic/therapeutic agent for various bone diseases (e.g., bone fractures).

Abstract: Novel chemotherapeutic agents having utility in treating infectious diseases such as periodontal disease, certain urinary tract infections, and infectious urinary tract stones, are obtained by combining chemically a diphosphonate compound with a therapeutic agent effective against the foregoing diseases.

Abstract: Disclosed are nonpeptides having bradykinin antagonist activity of the formulae (I) and (II) ##STR1## or a pharmaceutically acceptable salt thereof therefor.

Abstract: The present invention discloses a methane diphosphonate derivative, a process for producing said derivative and its pharmaceutical applications, said methane diphosphonate derivative indicated with general formula (1): ##STR1## (wherein, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently a pharmacologically acceptable cation, a hydrogen atom or a straight chain or branched alkyl group having 1-4 carbon atoms, R.sub.5 is a hydrogen atom or a trialkylsilyl group, m is an integer of 0 to 3, n is an integer of 1 to 3, R.sub.6 and R.sub.7 are independently a hydrogen atom or an alkyl group, and X represents a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group or an alkylthio group).

Abstract: Certain substituted semicarbazones, including all geometric and stereoisomers thereof, agricultural compositions containing them and their use as arthropodicides.

Abstract: The invention provides fungicidal compositions containing benzyl-tris(aryl)-phosphonium salts of the general formula ##STR1## in which R.sup.1 represents an optionally substituted alkyl or alkoxy group; R.sup.2 represents a hydrogen atom or an optionally substituted alkyl group; R.sup.3, R.sup.4 and R.sup.5 independently represent a hydrogen or halogen atom or an optionally substituted alkyl or alkoxy group; and A.sup.- represents an anion processes for the preparation of such compounds. Certain of the compounds of formula I are novel and the invention therefore also provides processes for the preparation of such compounds and their use as fungicides.

Abstract: Certain substituted semicarbazones, including all geometric and stereoisomers thereof, agricultural compositions containing them and their use as arthropodicides.

Abstract: This invention provides a method for treating the symptoms of schizophrenia by interacting selectively with presynaptic dopaminergic D.sub.2 receptors without appreciably activating postsynaptic dopamine receptors which comprises administering to a schizophrenic an effective amount of a compound selected from the group consisting essentially of the stereoisomers of mixtures thereof of compounds represented by the general formula: ##STR1## wherein R.sub.1 is selected from the group consisting of pyridyl and ##STR2## X is oxygen or sulfur, Y, if present, is selected from the group consisting of hydroxy, nitro, cyano, azido, amino, acylamino, carboxyamido, trifluoromethyl, sulfate, sulfonamido halogen, hydrocarbyl and hetero atom-substituted hydrocarbyl radicals, wherein said heteroatoms are selected from the group consisting of halogen, nitrogen, oxygen, sulfur and phosphorus and said hydrocarbyl radicals comprise from 1 to 12 carbon atoms, and a is an integer between zero and 3, R.sub.2 is H, R.sub.

Abstract: Phosphine oxide-terminated allene-ene-yne compounds are disclosed that possess DNA-cleaving, antimicobial and tumor growth-inhibiting properties. Methods of making and using those compounds are also disclosed.

Abstract: Benzoheterocyclylalkylaminoalkanediphosphonic acids of formula I ##STR1## wherein R.sub.1 and R.sub.2, independently of one another, are hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl, R.sub.3 is hydrogen or lower alkyl, X and Y, independently of one another, are oxy or thio, alk.sub.1 and alk.sub.2 are identical or different lower alkylene radicals, n is 0 or 1 and m and m', independently of one another, are 0, 1 or 2, the sum of n, m and m' being 1, 2 or 3, and their salts exhibit a pronounced regulatory action on the calcium metabolism of warm-blooded animals. They are prepared, for example, as follows: in a compound of the formula ##STR2## wherein R.sub.1, R.sub.2, n, m, m', X, Y, alk.sub.1 and alk.sub.2 are as defined above, R'.sub.3 is one of the groups R.sub.3 mentioned above or is an amino-protecting group R.sub.0, Z.sub.1 is a functionally modified phosphono group, and Z.sub.2 is a free or functionally modified phosphono group, converting functionally modified phosphono Z.sub.

Abstract: Cyclophosphamides possessing anti-tumor activity and having the formula ##STR1## and salts thereof; wherein R is lower alkyl, aryl, aryl-lower alkyl or a nitrogen, sulfur or oxygen containing heterocyclic or heterocyclic lower alkyl, andR' is hydrogen, hydroxy or OOH with the proviso that when R' is hydrogen, R is other than methyl or phenyl and when R' is hydroxy, R is other than methyl.

Abstract: A sulfur-containing hetrocyclic compound of the formula (I) ##STR1## wherein the ring A is an optionally substituted benzene ring, R is a hydrogen atom or an optionally substituted hydrocarbon residue, B is a carboxyl group which may be esterified or amidated, X is --CH(OH)-- or --CO--, and n is an integer of 0, 1 or 2, or its salt, which is useful in the prevention or treatment of osteoporosis.

Abstract: Compounds of the formula: ##STR1## wherein R.sub.1 is C.sub.2- C.sub.12 linear or branched unsubstituted alkyl; C.sub.1- C.sub.12 linear or branched substituted alkyl; C.sub.2 -C.sub.12 linear or branched monoalkenyl; C.sub.2 -C.sub.12 linear or branched alkynyl; C.sub.7 -C.sub.20 aralkyl, wherein the alkyl chain is linear or branched C.sub.1- C.sub.8 and the aryl moiety is C.sub.6- C.sub.12 ; C.sub.4- C.sub.10 cycloalkylalkyl; C.sub.3- C.sub.7 cycloalkyl; wherein these values for R.sub.1, other than C.sub.2- C.sub.12 linear or branched unsubstituted alkyl, can be substituted by one or more of C.sub.1 -C.sub.4 alkoxy, C.sub.3- C.sub.6 cycloalkyloxy, C.sub.3- C.sub.6 cycloalkylthio, C.sub.6- C.sub.12 aryloxy, C.sub.1- C.sub.4 alkylthio, C.sub.6- C.sub.12 arylthio, C.sub.7- C.sub.10 aralkyloxy, C.sub.7- C.sub.16 aralkyl-thio; and R.sub.5 is H or C.sub.1- C.sub.12 linear or branched alkyl; C.sub.2- C.sub.12 linear or branched monoalkenyl; C.sub.7- C.sub.

Abstract: The present invention provides a sulfur-containing heterocyclic compound of the formula (I) ##STR1## wherein ring A is a benzene ring which may be substituted; R is a hydrogen atom or a hydrocarbon group which may be substituted; B is a carboxyl group which may be esterified or amidated; X is --CH(OH)-- or --CO--; k is 0 or 1; and k' is 0, 1 or 2 or a pharmaceutically acceptable salt thereof.Also, it provides a process for producing the compound (I) or a salt thereof and a pharmaceutical preparation for use in the treatment of osteoporosis comprising the compound (I) or salt thereof.The compounds (I) and salts thereof show excellent bone resorption inhibitory activity.

Abstract: Angiostatic compounds are potentiated by collagen matrix metabolism modulators including:a) proline analogs which inhibit proline hydroxylation when substituted for proline in collagen;b) inhibitors of proline hydroxylase;c) inhibitors of collagen cross-linking; andd) all trans-retinoic acid.In methods and therapeutic compositions for inhibiting angiogenesis in a mammal, the collagen matrix modulator is administered with an angiostatic steroid or with heparin (including angiostatic heparin fragments of six or more sugar units, and synthetic fragments).

Abstract: A compound of the formula: ##STR1## wherein R.sup.1 -A- is a group of the formula: ##STR2## in which R.sup.1 is aryl or a heterocyclic group, each of which may be substituted with substituent(s) selected from the group consisting of lower alkyl, lower alkoxy, lower alkylthio, halo(lower)alkyl, acyl, acylamino and halogen, or lower alkyl which may be substituted with a heterocyclic group optionally substituted with acyl, andX is O or S, andR.sup.2 is hydrogen or lower alkyl, provided that when R.sup.1 is lower alkyl, thenR.sup.1 -A- is a group of the formula: ##STR3## in which R.sup.1 and X are each as defined above, processes for the preparation thereof and pharmaceutical composition comprising the same.

Abstract: Novel labdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.