Abstract: [4,5]-Fused-1,3-disubstituted-1,2-diazine-6-one derivatives with nitrogen-containing substituents in position one are useful for inducing or promoting apoptosis and for arresting uncontrolled neoplastic cell proliferation, and are specifically useful in the arresting and treatment of neoplasia, including precancerous and cancerous lesions.
Type:
Grant
Filed:
August 14, 1998
Date of Patent:
January 30, 2001
Assignee:
Cell Pathways, Inc.
Inventors:
Xiaojing Wang, Gerhard Sperl, Paul Gross, Rifat Pamukcu, Gary A. Piazza
Abstract: Substituted condensation products of N-benzyl-3-indenylacetamides with heterocyclic aldehydes are useful for inducing or promoting apotosis and for arresting uncontrolled neoplastic cell proliferation, and are specifically useful in the arresting and treatment of neoplasias, including precancerous and cancerous lesions.
Type:
Grant
Filed:
January 24, 2000
Date of Patent:
December 26, 2000
Assignee:
Cell Pathways, Inc.
Inventors:
Gerhard J. Sperl, Paul Gross, Klaus Brendel, Gary A. Piazza, Rifat Pamukcu
Abstract: 1,3,6-Trihydro-6-Aza-3-Oxapentalen-2-One Derivatives of Formula I are useful for inducing or promoting apoptosis and for arresting uncontrolled neoplastic cell proliferation, and are specifically useful in the arresting and treatment of neoplasia: ##STR1## Wherein R.sub.1 and R.sub.2 are independently selected from the group consisting of hydrogen, lower alkyl, and benzyl,R.sub.3 and R.sub.4 are selected from the group consisting of substituted or unsubstituted phenyl, and the like,R.sub.5 is selected from the group consisting of hydrogen, lower alkyl, and the like,Y is selected from the group consisting of CH.sub.2, C.dbd.O, CH--OH; m is an integer from 0-3; X is selected from the group consisting of CH.sub.2, C.dbd.O, CH--OH, and SO.sub.2 ; and n is an integer from 0-2.
Abstract: This invention provides a method to identify compounds potentially useful for the treatment of neoplasia in mammals. The phosphodiesterase inhibitory activity of a compound is determined along with COX inhibitory activity. Growth inhibitory and apoptosis inducing effects on cultured tumor cells are also determined. Compounds that exhibit phosphodiesterase inhibiton, growth inhibition and apoptosis induction, but not substantial prostaglandin inhibitory activity, are desirable for the treatment of neoplasia.
Abstract: Benzothienopyrimidine derivatives for inducing or promoting apoptosis and for arresting uncontrolled neoplastic cell proliferation, and specifically for arresting and treating neoplasia, including precancerous and cancerous lesions of formula I: ##STR1## wherein R.sub.1 and R.sub.2 are independently selected from the group consisting of hydrogen, A, OA, alkenyl, alkynyl, --NO.sub.2, --CF.sub.3 or halogen, with the proviso that one of R.sub.1 or R.sub.2 is not hydrogen; R.sub.3 and R.sub.4 are independently selected from the group consisting of hydrogen, A, --OA, halogen, --NO.sub.2, --NH.sub.2, --NHA or --NAA', or R.sub.3 and R.sub.4 are together form a moiety selected from the group consisting of --O--CH.sub.2 --CH.sub.2 --, --O--CH.sub.2 --O-- or --O--CH.sub.2 --CH.sub.
Abstract: A method for selecting compounds for the treatment of neoplasia includes assessing whether the compounds cause an increase in PKG activity in the neoplasia of interest.
Abstract: A method for inhibiting neoplasia, particularly cancerous and precancerous lesions by exposing the affected cells to pyrazolopyridylpyridazinone derivatives.
Abstract: Substituted condensation products of N-benzyl-3-indenylacetamides with heterocyclic aldehydes are useful for inducing or promoting apotosis and for arresting uncontrolled neoplastic cell proliferation, and are specifically useful in the arresting and treatment of neoplasias, including precancerous and cancerous lesions.
Type:
Grant
Filed:
December 7, 1998
Date of Patent:
May 23, 2000
Assignees:
Cell Pathways, Inc., University of Arizona
Inventors:
Gerhard J. Sperl, Paul Gross, Klaus Brendel, Gary A. Piazza, Rifat Pamukcu
Abstract: Derivatives of Phenyl Cycloamino Pyrimidinone are useful for the treatment of patients having precancerous lesions. These compounds are also useful to inhibit growth of neoplastic cells.
Abstract: Derivatives of quinazoline are useful for the treatment of patients having precancerous lesions. These compounds are also useful to inhibit the growth of neoplastic cells.
Abstract: Derivatives of phenyl pyridinone are useful for the treatment of patients having precancerous lesions. These compounds are also useful to inhibit the growth of neoplastic cells.
Abstract: This invention relates to a method for the selective inhibition of neoplastic cells, for example, for the treatment of precancerous lesions or other neoplasias in mammals.
Abstract: Substituted condensation products of 1H-indenylhydroxyalkanes with aldehydes are useful for inducing or promoting apoptosis and for arresting uncontrolled neoplastic cell proliferation, and are specifically useful in the arresting and treatment of neoplasia, including precancerous and cancerous lesions.
Type:
Grant
Filed:
April 3, 1998
Date of Patent:
February 22, 2000
Assignee:
Cell Pathways, Inc.
Inventors:
Gerhard Sperl, Paul Gross, Klaus Brendel, Gary Piazza, Rifat Pamukcu
Abstract: In position 7 substituted indenyl-3-acetic acid derivatives and pharmaceutically acceptable salts and amides thereof have anti-neoplastic activity.