Abstract: This invention discloses benzoxazinone and benzothiazinone compounds which display inhibitory effects on serine proteases such as factor Xa, thrombin, and/or factor VIIa. The invention also discloses pharmaceutically acceptable salts of the compounds, pharmaceutically acceptable compositions comprising the compounds or their salts, and methods of using them as therapeutic agents for treating or preventing disease states in mammals characterized by abnornal thrombosis.

Abstract: Antitumor combinations consisting of taxol or Taxotere or analogues thereof combined with at least one therapeutically useful substance for treating neoplastic diseases.

Abstract: This invention provides a method of treating a tumor in a warm-blooded animal, including humans, by administering, in combination, an anti-tumor effective amount of tegafur, uracil, folinic acid or pharmaceutically acceptable salt thereof and cyclophosphamide.

Abstract: Combination therapies are provided for the treatment of proliferative disorders which use a pentafluorobenzenesulfonamide of formula I and an antineoplastic agent such as gemcitabine or paclitaxel.

Abstract: A therapeutic agent for myeloma comprising a combined use of a nitrogen mustard anticancer agent and anti-IL-6 receptor antibody. Thus, a therapeutic agent for myeloma comprising anti-IL-6 receptor antibody for use in combination with a nitrogen mustard anticancer agent; a therapeutic agent for myeloma comprising a nitrogen mustard anticancer agent for use in combination with anti-IL-6 receptor antibody; and a therapeutic agent for myeloma comprising a nitrogen mustard anticancer agent and anti-IL-6 receptor antibody.

Abstract: The disclosed invention is a composition agonists and/or antagonists of V2, V1a or both receptors, in a host, including animals, and especially humans, using a small molecule or its pharmaceutically acceptable salt or prodrug.

Abstract: The present invention provides for improved methods of gene transfer, both in vitro and in vivo. By treating neoplastic cells with a DNA-damaging agent prior to transduction with a transgene, the expression of the transgene is improved up to about 3-fold over the expression seen in the absence of the DNA-damaging agent treatment. This effect is not dependent on the tumor cell type, the method of DNA transduction or type of DNA-damaging agent. The effect is most dramatic when the transduction is performed about 1-3 days following treatment with the DNA-damaging agent.

Abstract: A compound of the general formula I 1

Abstract: This invention provides compositions and methods for increasing cellular respiration of melanized catecholamine neurons, and methods for alleviating symptoms or stopping appearance and/or progression of symptoms of Parkinson's Disease, and methods for preventing symptoms of on-off syndrome associated with treatment with dopamine or a dopamine agonist of a patient suffering symptoms of a disease selected from the group consisting of idiopathic and atypical Parkinson's disease, conditions characterized by nigrostriatal degeneration and multiple system atrophy, said methods comprising administering to said patient an effective amount of a neuromelanin-binding composition having a quinoline ring in a suitable pharmaceutical carrier. Preferably the composition comprises (−)-chloroquine.

Abstract: The present invention provides pharmaceutical compositions and methods for treating cell proliferative disorders, such as tumors, in a subject, utilizing TGF-&agr; or functional fragments thereof. Optionally, a chemotherapeutic agent is administered in combination with TGF-&agr; or fragments thereof.

Abstract: The present invention relates to the use of tachykinin antagonists, including substance P antagonists and other neurokinin antagonists, in the treatment of emesis. Also described are novel tachykinin antagonists of formula (I), processes for their preparation, pharmaceutical compositions containing them and their medical use.

Abstract: Compounds of formula (I) 1

Abstract: 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 possess a &bgr;-lactam pharmacophore. These new inhibitors are fully synthetic, allowing ready access to a wide variety of structurally related analogs. Certain embodiments of these new inhibitors also bind bacterial DD-peptidases, thus potentially acting both as &bgr;-lactamase inhibitors and as antibiotics.

Abstract: Methods of promoting allograft survival, by attenuating or preventing allograft rejection, and treating or ameliorating the post-transplantation syndrome complex associated with allograft rejection and immunosuppressive pharmacotherapy used to prevent allograft rejection, are described. These methods comprise administering to an human or animal in need of treatment an effective amount of an insulin-sensitizing compound or and pharmaceutically acceptable salts and solvates thereof, administered alone or in combination with other immunosuppressive drugs.

Abstract: This invention is a method of treating cancer, including carcinomas and sarcomas through the administration of a pharmaceutical composition containing a pyridinylimidazole carbamate.

Abstract: This invention provides methods, formulations and kits to reduce the toxicity of flavopiridol and analogs thereof. Disclosed are therapeutics and treatment methods employing such drugs in combination with agents that increase conjugative enzyme activity or glucuronosyltransferase activity, and agents that decrease biliary transport protein activity, such as cyclosporine A, the resultant effects of which are to decrease the significant side effects previously associated with treatment using these drugs. The invention also characterizes specific isoforms of glucuronyltransferase enzymes involved in glucuronidation of flavopiridols and their analogs.

Abstract: The present invention provides methods for suppressing, reducing or even reversing an immune response. More particularly it concerns anti-CD28 monoclonal antibody compositions and methods for preventing graft-versus-host disease (GVHD), transplant tissue rejection, and treating autoimmune diseases and the like. In particular embodiments, a method of inhibiting an immune response comprises administering an effective amount of a purified anti-CD28 antibody preparation to a subject, wherein the preparation modulates the CD28 receptor thereby inhibiting an immune response.

Abstract: A method is provided for the treatment of neoplastic diseases in a mammal which comprises administering to said mammal a therapeutically effective amount of thalidomide. The method also uses a combination of thalidomide with other anti-neoplastic agents. Additionally, pharmaceutical compositions containing thalidomide and other anti-cancer agents are also provided.

Abstract: A method of lyophilizing an oxazaphosphorin and a preparation produced thereby including dissolving an oxazaphosphorin in water, adding an amino acid to a molar ratio of between 1 to 10 amino acid to 1 oxazaphosphorin to produce a mixture and lyophilizing said mixture to remove said water, is disclosed.

Abstract: Novel cyclic phosphonate ester inhibitors of MTP are provided which have the structure ##STR1## wherein R.sup.2, L.sup.2, A, B, L.sup.1, R.sup.1 and R.sup.5a are as set out herein. These compounds are useful in lowering serum cholesterol and triglycerides.

Abstract: Phospholipid derivatives containing higher elements of the Vth main group (P, As, Sb, Bi), their method of preparation and antineoplastic and antimicrobially active medications that can be prepared from the phospholipid derivatives.

Abstract: A method is provided for preventing and/or treating hypertriglyceridemia, and/or atherosclerosis and/or pancreatitis resulting from hypertriglyceridemia, employing a squalene synthetase inhibitor.

Abstract: Phospholipid derivatives containing higher elements of the Vth main group (P, As, Sb, Bi), their method of preparation and antineoplastic and antimicrobially active medications that can be prepared from the phospholipid derivatives.

Abstract: Phosphonoacetic acid derivatives and their use for treating degenerative joint disorders Compounds of the formula I ##STR1## are suitable for producing pharmaceuticals for the treatment and prophylaxis of degenerative joint disorders, of rheumatic disorders accompanied by cartilage breakdown, such as rheumatoid arthritis, joint trauma and chondrolysis as a consequence of prolonged immobilization of the joint, of inflammations, septic shock, disorders with impaired leukocyte adhesion, disorders caused by an elevated concentration of tumor necrosis factor alpha, such as cachexia or Crohn's disease.

Abstract: A methane diphosphonic acid derivative represented by the general formula (I): ##STR1## wherein, X and Y are defined in the specification; m represents an integer of 0 to 3; n represents an integer of 0 to 4; and each X of the (X).sub.m and each Y of the (Y).sub.n may be either identical or different; . . . represents a double bond or single bond; A is --(CH.sub.2)a--(D)b--(CH.sub.2)c-- (wherein D is sulfur, oxygen, NH, alkyl-substituted N, or CH.sub.2, a and c are integers of 0 to 10 and b is 0 or 1), or --(CH.dbd.CH)d.dbd.CH= (wherein d is an integer of 0 to 2, and B does not exist when A represents --CH.dbd.CH)d--CH.dbd.), B refers to a hydrogen atom, alkyl group, amino group, monoalkylamino group, dialkylamino group, acylamino group, hydroxyl group, alkoxy group, trialkylsiloxy group or acyloxy group, and each of R.sup.1, R.sup.2, R.sup.3 and R.sup.

Abstract: The bisphosphonates of formula (III)R.sub.2 --X--(CW).sub.m1 --CR.sub.3 R.sub.4 --CH.sub.2 --CM[PO--(OR.sub.1).sub.2 ].sub.2 (III)bicyclic bisphosphonates (V), and cyclic bisphosphonates (VII) are useful as antiarthritic agents and do not have the side effects of anti-arthritic agents which are prostaglandin synthetase inhibitors.

Abstract: This invention provides a new use of acids, esters, and salts of arylmethylphosphonates of Formula I, ##STR1## or a phosphonic acid of Formula II ##STR2## and derivatives as anti-inflammatory and anti-arthritic agents. Representative compounds include 4-dodecyloxybenzylphosphonic acid dimethyl ester, (2-naphthalenylmethyl)phosphonic acid dimethyl ester, and ([1,1'-biphenyl]-2-ylmethyl)phosphonic acid dimethyl ester.

Abstract: This invention relates to bisphosphoryl hydrazine compounds and to compositions thereof which are useful as pesticides. The compounds of this invention are effective against soil insects, especially the corn rootworm.

Abstract: A method for treating or preventing alopecia which is induced by an antineoplastic compound is disclosed which is based on the administration of a particular tellurium or selenium derivative to a patient prior to the administration of a antineoplastic agent to said patent.

Abstract: Benzoxazinone compounds of general formula (I): ##STR1## useful in the treatment of serotoninergic disorders, especially anxiety and schizophrenia, requiring for their treatment compounds which are 5-HT.sub.1A receptor agonists, wherein R.sub.1, R.sub.2, R.sub.3, and n are as defined in the description, and medicinal products containing the same, are disclosed.

Abstract: Ifosfamide lyophilizate consisting substantially of ifosfamide and 0.1 to 17 parts by weight of a hexitol.

Abstract: Compound of general formula (I): ##STR1## where R.sub.1, R.sub.2, R.sub.3, n, X and A are defined in the description.Medicinal products.

Abstract: Compounds which are inhibitors of cholesterol biosynthesis (by inhibiting de novo squalene biosynthesis), and thus are useful as hypocholesterolemic agents and antiatherosclerotic agents are provided which have the structure ##STR1## and analogs thereof, wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and are H, lower alkyl, a metal ion or a prodrug ester;R.sup.5 is H, halogen or lower alkyl;Zq is substituted alkenyl, substituted alkynyl, mixed alkenyl-alkynyl or substituted phenylalkyl or, phenylalkenyl or phenylalkynyl, or alkyl, including all stereoisomers thereof.New methods for using such compounds to inhibit cholesterol biosynthesis are also provided.

Abstract: The N-phosphorylation of basic nitrogenous drug compounds to produce pro-drugs with enhanced water solubility or lipid solubility, or reduced toxicity, is disclosed. Drugs containing amine, amidine, guadinine, isourea, isothiourea an biguanide functions may be converted to such pro-drugs. The pro-drugs are hydrolyzed in the body, regenerating the original drugs with the release of a salt of phsophoric acid.

Abstract: Pharmaceutical compositions and a method for inhibiting the growth of tumor cells by administering a tumor cell growth-inhibiting amount of a bis[bis (diphenylphosphino)hydrocarbon]-, bis[bis(diethylphsophino) hydrocarbon]-, bis[bis(diphenylphosphine-deithylphosphino) hydrocarbon]gold(I), silver(I) or copper(I) complex or a tris[bis(diphenylphosphino)ethane] dicopper(I) complex to an animal afflicted with said tumor cells.

Abstract: Compounds of the formula: ##STR1## and stereoisomers thereof wherein X and Y, which are the same or different, are hydrogen, halogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted alkoxy, optionally substituted aryloxy, optionally substituted heteroaryloxy, optionally substituted arylalkoxy, optionally substituted heteroarylalkoxy, optionally substituted acyloxy, optionally substituted amino, acylamino, nitro, cyano, --CO.sub.2 R.sup.3, --CONR.sup.4 R.sup.5, or --COR.sup.6, except that X and Y are not both hydrogen; R.sup.1 and R.sup.2, which are the same or different, are alkyl or fluoroalkyl; and R.sup.3, R.sup.4, R.sup.5 and R.sup.6, which are the same or different, are hydrogen, alkyl, alkenyl, alkynyl, optionally substituted aryl, optionally substituted aralkyl, or cycloalkylalkyl.

Abstract: Novel pesticidally active cyclic malonylphosphonic diamides of the formula ##STR1## in which X.sup. represents O or S,R.sup.1 represents alkyl, alkenyl, alkinyl, cycloalkyl, aryl or heteroaryl, each of which can be optionally substituted,R.sup.2 represents hydrogen, alkyl, aryl or aralkyl,R.sup.3 represents hydrogen, alkyl, aryl or aralkyl, andR.sup.

Abstract: Through the combined use of a 4-sulfido-oxazaphosphorine of the formula: ##STR1## wherein R.sub.1, R.sub.2, and R.sub.3 are hydrogen, methyl, ethyl, 2-chloroethyl or 2-methanesulfonyloxyethyl and at least two of them are taken from the group consisting of 2-chloroethyl and 2-methanesulfonyloxyethyl, R.sub.4 is hydrogen or methyl, R.sub.5 is a C.sub.2 -C.sub.6 -hydroxyalkyl group or a C.sub.2 -C.sub.6 -mercaptoalkyl group of each of these groups with an additional mercapto group, or R.sub.5 is a carboxy-C.sub.1 -C.sub.10 alkyl group, a carb-C.sub.1 -C.sub.6 -alkoxy-C.sub.1 -C.sub.10 -alkyl group, a 2-amino-2-carboxyethyl group, a 2-amine-2-carb-C.sub.1 -C.sub.6 -alkoxy-ethyl group, a 2-C.sub.2 -C.sub.6 -alkanoylamino-2-carboxyethyl group, the glutathionyl group, a C.sub.2 -C.sub.6 -sulfoalkyl group or a C.sub.2 -C.sub.6 -sulfoalkyl group which contains a mercapto group or a physiologically compatible salt thereof in combination with a thion compound of the formula:R.sub.6 SR.sub.7 IIwhere R.sub.

Abstract: Novel arthropodicidally active compounds of the formula ##STR1## in which R represents amino or optionally substituted radicals from the series comprising alkyl, alkylamino, methyl-alkylamino, alkoxy, alkenyloxy and alkylthio,R.sup.1 to R.sup.8 are identical or different and represent hydrogen or optionally halogen-substituted radicals from the series comprising alkyl, alkenyl, alkoxyalkyl and alkylthioalkyl, or represent halogen, nitro or dialkylaminoalkyl or represent optionally substituted phenyl or benzyl, and two of the radicals R.sup.1 to R.sup.8, together with the carbon atom or atoms to which they are bonded, may furthermore form an optionally substituted monocyclic or bicyclic ring, andn represents zero or 1.intermediates therefor wherein R is replaced by Cl are also novel.