Pharm-eco Laboratories, Inc.

Children's Medical Center Corporation

Other

Harvard College

Interneuron Pharmaceuticals, Inc.

Nuchem Pharmaceuticals Inc.

Ion Pharmaceuticals, Inc.

The United States of America As Represented by the Department of Health

Yesh P Sachdeva

Richard L Gabriel

Siya Ram

Adel M Moussa

Salah A Zahr

Jose Alberto Halperin

Ying-Duo Gao

Minghua Sun

Carlo Brugnara

Richard John Lombardy

Emile Al-Farhan

John J Clifford

Eugene W Kelleher

Reem M Haidar

Heather N Taft

Emile M Bellott

Jaechul Shim

Biman Pal

Rudolf Fluckiger

Bing Cai

Mark Froimowitz

Emile M Bellot, Jr

Falguni M Kher

Kenneth W Locke

Xiaoyong Sun

Kay Jorgenson D'Orlando

Subramaniam Krishnananthan

Michael D Nohrden

Michael H Zeldin

Donna Kaye Wilson

Jurjus Jurayj

David A Swanson

Changhua Liu

Brittany La

Sharon Fitzhenry

Ravi Varma

The present invention provides a class of chemical compounds useful as efficacious drugs in the treatment of sickle cell disease and diseases characterized by unwanted or abnormal cell proliferation, and in particular inflammatory diseases associated with unwanted cellular proliferation. The active compounds are substituted triaryl methane compounds or analogues thereof where one or more of the aryl groups is replaced with a heteroaryl, cycloalkyl or heterocycloalkyl group and/or the tertiary carbon atom is replaced with a different atom such as Si, Ge, N or P. the compounds inhibit mammalian cell proliferation, inhibit the Gardos channel of erythrocytes, reduce sickle erythrocyte dehydration and/or delay the occurrence of erythrocyte sickling or deformation.

Use of triaryl methane compounds for inhibiting unwanted cellular proliferation associated with inflammatory disease

The present invention provides substituted 3,3-diphenyl indole compounds, as well as analogues thereof, which are specific potent and safe inhibitors of mammalian cell proliferation. The compounds can be used to inhibit mammalian cell proliferation in situ as a therapeutic approach towards the treatment or prevention of diseases characterized by abnormal cell proliferation, such as cancer.

Substituted diphenyl indanone, indane and indole compounds and analogues thereof useful for the treatment or prevention of diseases characterized by abnormal cell proliferation

The present invention provides substituted 11-phenyl-dibenzazepine compounds which are specific, potent and safe inhibitors of mammalian cell proliferation. The compounds can be used to inhibit mammalian cell proliferation in situ as a therapeutic approach towards the treatment or prevention of diseases characterized by abnormal cell proliferation, such as cancer.

Substituted 11-phenyl-dibenzazepine compounds useful for the treatment or prevention of diseases characterized by abnormal cell proliferation

The present invention provides substituted 3,3-diphenyl indanone, indane and indole compounds, as well as analogues thereof, which are specific, potent and safe inhibitors of mammalian cell proliferation. The compounds can be used to inhibit mammalian cell proliferation in situ as a therapeutic approach towards the treatment or prevention of diseases characterized by abnormal cell proliferation, such as cancer.

Substituted diphenyl indanone, indane and indole compounds and analogues thereof useful for the treatment of prevention of diseases characterized by abnormal cell proliferation

The present invention provides substituted 11-phenyl-dibenzazepine compounds that are specific, potent and safe inhibitors of mammalian cell proliferation. The compounds can be used to inhibit mammalian cell proliferation in situ as a therapeutic approach towards the treatment or prevention of diseases characterized by abnormal cell proliferation, such as cancer.

Substitute 11-phenyl-dibenzazepine compounds useful for the treatment or prevention of diseases characterized by abnormal cell proliferation

Synthesis of nitroalcohol diastereomers

The present invention provides a class of chemical compounds useful as efficacious drugs in the treatment of sickle cell disease and diseases characterized by unwanted or abnormal cell proliferation, and in particular inflammatory diseases associated with unwanted cellular proliferation. The active compounds are substituted triaryl methane compounds or analogues thereof where one or more of the aryl groups is replaced with a heteroaryl, cycloalkyl or heterocycloalkyl group and/or the tertiary carbon atom is replaced with a different atom such as Si, Ge, N or P, the compounds inhibit mammalian cell proliferation, inhibit the Gardos channel of erythrocytes, reduce sickle erythrocyte dehydration and/or delay the occurrence of erythrocyte sickling or deformation.

Compounds represented by the following structural formula: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are as defined in the specification. The compounds are disclosed as useful in the treatment of various forms of cancer.

2-alkoxy estradiols and derivatives thereof

Amino acid-derived diaminopropanols

Disclosed is a method of preparing a compound represented by the following structural formula: ##STR1## The method comprises reacting bromine (Br.sub.2) and an aliphatic organic acid with a compound represented by the following structural formula: ##STR2## R.sub.1 and R.sub.2 are each independently a hydroxyl protecting group.

Synthesis of 2-alkoxyestradiols

The present invention provides a class of chemical compounds useful as efficacious drugs in the treatment of sickle cell disease and diseases characterized by unwanted or abnormal cell proliferation. The active compounds are substituted triaryl methane compounds or analogues thereof where one or more of the aryl groups is replaced with a heteroaryl, cycloalkyl or heterocycloalkyl group and/or the tertiary carbon atom is replaced with a different atom such as Si, Ge, N or P. The compounds inhibit mammalian cell proliferation, inhibit the Gardos channel of erythrocytes, reduce sickle erythrocyte dehydration and/or delay the occurrence of erythrocyte sickling or deformation.

Triaryl methane compounds and analogues thereof useful for the treatment

The present invention relates to a method for the stereospecific synthesis of an enantiomer of a chiral amine, wherein the chiral amine has the formula R.sup.1 CH(NH.sub.2)R.sup.2. R.sup.1 and R.sup.2 are each independently selected from the group consisting of alkyl, aryl and heterocyclic and radicals. This method is particularly useful for stereospecifically synthesizing S-dolaphenine. The method involves contacting a chiral enantiomer of norephedrine with borane, within an aprotic solvent to form a complex for stereospecifically reducing oximes. The complex is then contacted with an oxime, thereby stereospecifically reducing said oxime to form an enantiomer of a chiral amine.

Stereoselective method for synthesizing dolaphenine

An apparatus for decontaminating a liquid surfactant of a dioxane having a vapor pressure which is higher than the vapor pressure of the surfactant includes an elevated reservoir for dioxane-contaminated liquid surfactant and an elongate inclined conduit, which has an upper portion for receiving a stream of the contaminated liquid surfactant from the elevated reservoir and a lower portion for discharge of decontaminated liquid surfactant. A heat source is suitable for heating contaminated liquid surfactant in the elongate inclined conduit in an amount sufficient to cause the dioxane contaminant of the liquid surfactant to volatilize, thereby decontaminating the surfactant. A gas source is suitable for directing a gas through the inclined conduit to transport volatilized dioxane out of the conduit. A receptacle is connected to the elongate inclined conduit for receiving the decontaminated liquid surfactant discharged from the inclined conduit.

Apparatus for decontaminating a liquid surfactant of dioxane

Growing community of inventors

Concord, MA, United States of America

Yesh P Sachdeva