Abstract: This disclosure describes new antibiotic Cytosporacin having the structure: The invention relates to a new antibiotic designated Cytosporacin, to its production by fermentation, to methods for its recovery and concentration from the crude solutions, and to process for its purification. The invention includes within its scope the agent in dilute form, as a crude concentrate, and in pure form. The invention also relates to the use of the compound according to the invention in antimicrobial compositions and as antiseptics or disinfectants.

Abstract: A process for making an N1-(2′-pyridyl)-1,2-alkanediamine sulfamic acid of formula II by reacting a compound of formula I with NH2R′ wherein R and R′ are as defined in the specification. The invention also includes the compound of formula II, and optical isomers thereof. The compound of formula II is an intermediate useful for making chiral piperazine derivatives which are active at the 5-HT1A receptor.

Abstract: The present invention provides methods of treating an autoimmune pathology in a mammal, comprising administering an agent with estrogen receptor &agr; agonist activity in particular a selective estrogen receptor modulator, to the mammal in an amount sufficient to decrease production of TH-1 and/or TH-2 cytokines. Also provided is a method of selecting compounds useful for the treatment of multiple sclerosis, comprising selecting a compound which has estrogen receptor &agr; agonist activity.

Abstract: This invention provides parenteral formulations of rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid (CCI-779).

Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.

Abstract: This invention provides compound of formulae I or II having the structure 1

Abstract: The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor.

Abstract: This invention provides methods of using a pharmacological combination of a biguanide agents, such as metformin, and one or more PTPase inhibiting agents and, optionally, one or more sulfonlylurea agents, including glyburide, glyburide, glipizide, glimepiride, chlorpropamide, tolbutamide, or tolazamide, for treatment in a mammal of Syndrome X, type II diabetes or metabolic disorders mediated by insulin resistance or hyperglycemia. Further included in this invention is a method of modulating blood glucose levels in a mammal utilizing the combination of one or more PTPase inhibiting agents and one or more sulfonlylurea agents.

Abstract: Compounds of the formula are useful for treating the cognitive deficits due to aging, stroke, head trauma, Alzheimer's disease or other neurodegenerative diseases, or schizophrenia and are also useful for the treatment of disorders such as anxiety, aggression and stress, and for the control of various physiological phenomena, such eating disorders, disorders of thermoregulation, and sleep and sexual dysfunction.

Abstract: There is provided a process for the preparation of 7-substituted-3-quinolinecarbonitriles and intermediates useful in a process to prepare 7-substituted-3-quinolinecarbonitriles and pharmaceutically acceptable salts is described. Where 7-fluoro-4-oxo-1,4-dihydro-3-quinolinecarbonitrile is converted in three steps to 7-substituted-3-quinolinecarbonitriles which inhibit the action of certain protein kinases and are useful in the treatment of cancer.

Abstract: This invention provides compounds and methods using them to provide neuroprotection and prevent or limit processes of neurodegeneration in mammals, including Alzheimer's Disease, Huntington's Disease, Parkinson's Disease, AIDS dementia, retinal disease, diabetic peripheral neuropathy, multiple sclerosis, stroke, acute thromboembolic stroke, focal ischemia, global ischemia, transient ischemic attack, ischemia resulting from surgery, head trauma, spinal trauma, hypoxia, fetal hypoxia, and neuroprotection.

Abstract: This invention provides a compound of Formula (I): 1

Abstract: This invention provides compounds of the formulae: wherein: R1 is hydrogen, —C(O)CH3 or alkyl of 1-6 carbon atoms; R2 and R3 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, cycloalkyl, alkoxy of 1-6 carbon atoms, —CH2OH, fluoroalkyl, alkyl sulfonamide of 1-6 carbon atoms, alkyl amide of 1-6 carbon atoms, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl moiety, fluoroalkoxy of 1-6 carbon atoms, acyl of 2-7 carbon atoms, aryl, or aroyl; R4 and R5 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, halogen, fluoroalkyl, —CN, alkyl sulfonamide of 1-6 carbon atoms, alkyl amide of 1-6 carbon atoms, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl moiety, fluoroalkoxy of 1-6 carbon atoms, acyl of 2-7 carbon atoms, or aroyl; R6 and R7 are each independently hydrogen, C1-C6 alkyl or cycloalkyl; or a pharmaceutically acceptable salt thereof, as well as pharmaceut

Abstract: The present invention provides an efficient method of making O-desmethylvenlafaxine.

Abstract: The invention provides new substantially pure antibiotics designated AC-98-1, AC-98-2, AC-98-3, AC-98-4 and AC-98-5 derived from the microorganism Streptomyces hygroscopicus.

Abstract: This Invention provides a compound of the Formula: 1

Abstract: This invention comprises antibodies to rapamycin effector proteins, and preparations thereof. Novel Rapamycin-FKBP12 binding proteins, nucleic acids and their fragments are also described, as are related methods and therapeutic uses of the proteins, nucleic acids, and antibodies.

Abstract: The present invention relates, at least in part, to polypeptides which include Bcl-xL binding domains, novel Bcl-xL binding domains of Pablo polypeptides, nucleic acid molecules encoding such polypeptides, and uses thereof. For example, such polypeptides and nucleic acid molecules are useful in modulating apoptosis, particularly in neural cells, as well as in the treatment or prevention of disorders that can benefit from modulation of cell death.

Abstract: This invention provides estrogen receptor modulators of formula I, having the structure wherein R, R′, A, A′, X, Y, and Y are as defined in the specification, or a pharmaceutically acceptable salt thereof.

Abstract: Methods of treatment and pharmaceutical combinations are provided for the treatment of acute leukemia, such as acute myelogenous leukemia, and myelodysplastic syndrome. The methods of treatment and pharmaceutical combinations employ an anti-CD33 cytotoxic conjugate in combination with at least one compound selected from the group consisting of an anthracycline and a pyrimidine or purine nucleoside analog. Preferred methods of treatment and pharmaceutical combinations employ gemtuzumab ozogamicin, daunorubicin, and cytarabine.