Telik, Inc.

Geron Corporation

Bristol-myers Squibb Compnay

The Mclean Hospital Corporation

Michael R Kozlowski

Steven R Schow

Robert T Lum

Songyuan Shi

Wayne R Spevak

Prasad V V S V Manchem

Karen R Prowse

Hugo O Villar

Nam Woo Kim

Susan P Manly

Rachael L Neve

Sharon Wong

Sy-Shi Wang

Junko Aimi

Lawrence M Kauvar

Koji Tomita

Graham Johnson

Graham S Poindexter

Federico C Gaeta

Louise Robinson

Matthew H Lyttle

Pavel E Zhichkin

Yosuke Sawada

Koko Sugawara

Charles P Sloan

Ivo Monkovic

Marc A Bruce

Fanying Meng

Elaine C Stracker

R Jason Herr

Adam Antoni Galan

Ryan Holcomb

Karen LeBoulluec

Thomas Redelmeier

Patricia A Peterli-Roth

Ramakrishna Seethala

Robert W Macsata

Richard Allsopp

Richard Allsop

Micheal M Wick

Jeong Weon Park

Jason R Herr

Pavel Zhichkin

Compounds of formula I are useful for treating conditions associated with hyperglycemia, especially Type II diabetes. These compounds are useful in stimulating the kinase activity of the insulin receptor, activating the insulin receptor, and stimulating the uptake of glucose. Pharmaceutical compositions comprising the antidiabetic compounds are also disclosed.

Naphthalene ureas as glucose uptake enhancers

Pharmaceutical compositions and methods of using them. Lipid formulations of a glutathione analog and methods of manufacturing them. Their use to stimulate hematopoiesis, protect hematopoietic cells from damage caused by radiation or chemotherapy, or potentiate the stimulatory action of one or a combination of cytokines on colony formation by hematopoietic progenitor cells, protect a subject from a destructive effect of a chemotherapeutic agent or irradiation, or to potentiate the effect of a chemotherapeutic agent.

Therapeutic compositions containing glutathione analogs

Methods for treating conditions associated with hyperglycemia, especially Type II diabetes, with novel naphthylsulfonic acids and related compounds. These compounds, as single stereoisomers or mixtures of stereoisomers, or their pharmaceutically acceptable salts, are useful in methods of stimulating the kinase activity of the insulin receptor, enhancing the activation of the insulin receptor by insulin, and stimulating the uptake of glucose into cells. A variety of antidiabetic compounds and pharmaceutical compositions comprising the antidiabetic compounds are also disclosed.

Naphthylsulfonic acids and related compounds as glucose uptake agonists

Bis-(N,N&prime;-bis-(2-haloethyl)amino)phosphoramidates, pharmaceutical compositions containing them, methods of treatment using them, and processes for their preparation. The compounds possess anti-tumor activities or are capable of being modified to have anti-tumor activities; and this invention relates to the use of the compounds in methods for the treatment of tumors and, especially, for the treatment of cancer.

Bis-(N,N'-bis-(2-haloethyl)amino)phosphoramidates as antitumor agents

Methods for treating diseases associated with the activity of the insulin growth factor-1 receptor (IGF-1R), such as cancer, are provided. Methods for inhibiting cell growth and proliferation, especially of tumor cells, and promoting apoptosis are also provided. Each of these methods employs the use of a heteroaryl-aryl urea compound as an antagonist for IGF-1R.

Heteroaryl-aryl ureas as IGF-1 receptor antagonists

The invention provides DNA primase assays suitable for identifying DN primase modulating agents, methods of modulating DNA primase activity, compounds for modulating DNA primase activity, and compositions which modulate DNA primase.

Carboxamide derivatives having aryl and thiazole rings

The invention provides DNA primase assays suitable for identifying DNA primase modulating agents, methods of modulating DNA primase activity and compositions which modulate DNA primase.

Mammalian DNA primase screen and activity modulating agents

The present invention relates to the cloning of .beta.APP-C100 receptor (C100-R), and genetically engineered host cells which express the C100-R. Such engineered cells may be used to evaluate and screen drugs and analogs of .beta.-APP involved in Alzheimer's Disease.

Cloning and expression of .beta.APP-C100 receptor (C100-R)

.beta. APP-C100 receptor

Methods and compositions for the measurement of telomere length have application in medical diagnostic, prognostic, and therapeutic procedures. The methods for measuring telomere length include primer extension-based methods and probe-based methods. The primer extension methods involve elongation of telomeric, linker, and/or subtelomeric based primers under conditions such that the telomere serves as a template for primer extension and that the resultant primer extension products can be compared to standards of known length to provide a measure of telomere length. The probe based methods allow for telomere length measurements using DNA from lysed or whole cells and involve hybridizing an excess of probe to all telomeric repeat sequences in the telomere, measuring the amount of bound probe, and correlating the amount of bound probe measured with telomere length.

Methods for measuring telomere length

Methods and compositions for treating cancer and other diseases in which inhibition of telomerase activity can ameliorate disease symptoms or prevent or treat the disease relate to compounds that are derivatives of pyrido�b!thiophenes, pyrido�b!furans, pyridine ethers or pyridine thioethers. Such compounds are characterized by the following structure: ##STR1## X.sub.3 is oxygen or sulfur; and the double dashed lines between X.sub.4 and X.sub.5 indicate an optional double bond, which, when present, forms a fused, bicyclic pyrido�b!furan or pyrido�b!thiophene ring system, depending upon whether X.sub.3 is oxygen or sulfur, respectively. When the double bond is not present, the compound is a monocyclic pyridine ether or thioether, again depending upon whether X.sub.3 is oxygen or sulfur. X.sub.4 is --CH.sub.2 R.sub.21 or --CR.sub.21 --, where R.sub.21 is selected from the group consisting of aryl, heteroaryl, aralkyl, heteroaralkyl, alkylcarbonyl, arylcarbonyl, heteroalkylcarbonyl, heteroaralkylcarbonyl, aralkylcarbonyl, aminocarbonyl, alkylaminocarbonyl, arylaminocarbonyl, dialkylaminocarbonyl, diarylarninocarbonyl, arylalkylaminocarbonyl, carboxyl, alkoxycarbonyl, aryloxycarbonyl, sulfo, alkylsulfonyl and arylsulfonyl; and X.sub.5 is hydrogen, alkyl, hydroxyl, alkoxyl, aryloxyl, halogen, cyano, amino, alkylamino, arylamino, dialkylamino, diarylamino, arylalkylamino, aminocarbonyl, alkylaminocarbonyl, arylaminocarbonyl, dialkylaminocarbonyl, diarylaminocarbonyl, arylalkylaminocarbonyl, carboxyl, alkoxycarbonyl, aryloxycarbonyl, sulfo, alkylsulfonyl, arylsulfonyl or --CR.sub.22 -- where R.sub.22 is selected from the group consisting of hydrogen, amino, alkylamino, arylamino, dialkylamino, diarylamino, arylalkylamino, aminocarbonyl, alkylaminocarbonyl, arylaminocarbonyl, dialkylaminocarbonyl, diarylaminocarbonyl, arylalkylaminocarbonyl, hydroxyl, halogen, cyano, carboxyl, alkoxycarbonyl and aryloxycarbonyl. When X.sub.4 is --CR.sub.21 --, X.sub.5 is --CR.sub.22 --, and X.sub.4 and X.sub.5 are joined by the above-mentioned double bond, to form thereby a fused, bicyclic pyrido�b!thiophene (X.sub.3 is sulfur) or pyrido�b!furan (X.sub.3 is oxygen) ring system. When X.sub.4 is --CH.sub.2 R.sub.21, X.sub.5 is not --CR.sub.22 --, thereby forming a pyridine ether (X.sub.3 is oxygen) or thioether (X.sub.3 is sulfur). R.sub.18 and R.sub.19 are selected independently from the group consisting of hydrogen, halogen, hydroxy, aryloxy, alkoxy, lower alkyl, aryl, heteroaryl, aralkyl and heteroaralkyl. R.sub.20 is selected from the group consisting of alkoxymethyl, dialkoxymethyl, arylalkylaminomethyl, arylaminomethyl, alkylaminomethyl, aminomethyl, diarylaminomethyl, dialkylaminomethyl, hydroximinyl, iminyl, aldehyde, alkylcarbonyl, arylcarbonyl, alkyliminyl, aryliminyl, aralkyliminyl, alkoximinyl, aryloximinyl, heterocycleimninyl, alkoxycarbonyl, aryloxycarbonyl, carboxyl, alkene, --HC.dbd.NNHR.sub.23 where R.sub.23 is selected from the group consisting of hydrogen, alkyl, aryl, aralkyl, heterocycle, heterocyclealkyl, and --C(X.sub.6)NHR.sub.24 where X.sub.6 is oxygen or sulfur and R.sub.24 is selected from the group consisting of hydrogen, aryl, arylsulfonyl, aralkyl, heterocycle and heterocyclealkyl.

Telomerase inhibitors

Methods are provided for the determination of telomere length. These methods can be used for diagnosis of cancer and the staging of cancer, and diagnosis of senecesence in cells. Also, the instant methods can be used to determine stages of diseases such as atherosclerosis or HIV infection, and can be used to diagnose infertility.

A series of non-peptidergic antagonists of NPY have been synthesized and are comprised of piperazine and homopiperazine derivatives of 4-phenyl-1,4-dihydropyridines of Formula (I). ##STR1## As antagonists of NPY-induced feeding behavior, these compounds are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.

Dihydropyridine npy antagonists: piperazine derivatives

Disclosed are active compounds BU-4726G-A and BU-4726G-B which contain a quinone chromophore and hydroquinone chromophore, respectively. The compounds are produced by fermentation of Streptomyces exfoliatus AA4510. The compounds possess antimicrobial, and K.sub.ATP channel blocking activities.

Compounds produced by a strain of Streptomyces exfoliatus

Growing community of inventors

Palo Alto, CA, United States of America

Michael R Kozlowski