Abstract: Novel sulfatase inhibitor compounds useful in the treatment of estrogen dependent illnesses are disclosed. These compounds generally comprise a steroid nucleus substituted at the C17 position. Methods for synthesizing these compounds and using them in the therapeutic and/or prophylactic treatment of a patient are also disclosed.
Type:
Grant
Filed:
August 3, 2001
Date of Patent:
June 4, 2002
Assignees:
Duquesne University of the Holy Ghost, Kyowa Hakko Kogyo Co., Ltd.
Abstract: A computerized data processing system for categorizing documents that applies candidate functions, such as entropy, cross-entropy, and KL-distance, to data classification is disclosed. A computerized method for categorizing documents employing the candidate functions is also disclosed. The computerized data processing system and method of this invention allows for the automatic categorization, retrieval, and filtration of documents based upon the degree and/or rate of divergence from a reference standard.
Abstract: Novel sulfatase inhibitor compounds useful in the treatment of estrogen dependent illnesses are disclosed. These compounds generally comprise a steroid nucleus substituted at the C17 position. Methods for synthesizing these compounds and using them in the therapeutic and/or prophylactic treatment of a patient are also disclosed.
Type:
Grant
Filed:
January 24, 2000
Date of Patent:
April 23, 2002
Assignees:
Duquesne University of the Holy Ghost, Kyowa Hakko Kogyo Co., Ltd.
Abstract: Sulfatase inhibitor compounds useful in the treatment of estrogen dependent illnesses are disclosed. These compounds generally comprise a steroid nucleus substituted at the C17 position. Methods for synthesizing these compounds and using them in the therapeutic and/or prophylactic treatment of a patient are also disclosed.
Type:
Grant
Filed:
January 25, 1999
Date of Patent:
September 11, 2001
Assignees:
Duquesne University of the Holy Ghost, Kyowa Hakko Kogyo Co., Ltd.
Abstract: Novel sulfatase inhibitor/estrogen receptor blocker compounds useful in the treatment of estrogen dependent illnesses are disclosed. The compounds generally comprise a sulfamate moiety and an aromatic, estrogen receptor blocker moiety. Methods for synthesizing these compounds and using them in the therapeutic and/or prophylactic treatment of an estrogen-dependent disease are also disclosed.
Abstract: Estra-1,3,5(10),16-tetraene derivatives represented by the following formula (I):
(wherein R1 represents hydroxy, alkoxy, or NR2R3 (wherein R2 and R3 are the same or different, and each represents hydrogen, straight-chain lower alkyl having 1 to 3 carbon atoms, or branched-chain lower alkyl having 3 to 8 carbon atoms)), or pharmaceutically acceptable salts thereof.
Type:
Grant
Filed:
April 13, 2000
Date of Patent:
July 17, 2001
Assignees:
Kyowa Hakko Kogyo Co., Ltd., Duquesne University of the Holy Ghost
Abstract: Novel sulfatase inhibitor/estrogen receptor blocker compounds useful in the treatment of estrogen dependent illnesses are disclosed. The compounds generally comprise a sulfamate moiety and an aromatic, estrogen receptor blocker moiety. Methods for synthesizing these compounds and using them in the therapeutic and/or prophylactic treatment of an estrogen-dependent disease are also disclosed.
Abstract: This invention discloses compounds, and pharmaceutically acceptable salts thereof, useful in therapeutically and/or prophylactically treating patients with an illness. Such illnesses include cancer, and secondary infections caused by Pneumocystis carinii and Toxoplasmosis gondii in immunocompromised patients. The compounds themselves, methods of making these compounds, and methods of using these compounds are all disclosed.
Abstract: A time release orally administrable drug containing product comprising a core, a drug layer attached to the core, and first and second coating layers is disclosed. The first coating layer is directly adjacent to the drug layer, and has a limited permeability to water. The second coating layer is directly adjacent to the first coating, and is more permeable to water than the first layer. A method for using this drug in the treatment of a patient is also disclosed.
Abstract: The invention also discloses compounds and pharmaceutically acceptable salts having the generic formula (2) ##STR1## wherein X and Y may be the same or different and are selected from the group consisting of OH and NH.sub.2 ; wherein Z is one of either nitrogen or carbon and Q is one of either nitrogen or carbon but when Z equal nitrogen, Q does not equal nitrogen and when Q equals nitrogen, Z does not equal nitrogen; wherein A is selected from the group consisting of nitrogen, carbon and sulfur and B equals carbon when A is selected from the group consisting of sulfur, carbon, and nitrogen, B equals nitrogen when A equals carbon and B equals sulfur when A equals carbon; wherein R.sub.3 is one of either hydrogen or methyl except where Z is nitrogen wherein R.sub.3 is zero; wherein R.sub.4 is one of either a hydrogen or a first lower alkyl group except when A equals sulfur wherein R.sub.4 is zero; wherein R.sub.
Abstract: This invention discloses compounds, and pharmaceutically acceptable salts thereof, useful in therapeutically and/or prophylactically treating patients with an illness. Such illnesses include cancer, and secondary infections caused by Pneumocystis carinii and Toxoplasmosis gondii in immunocompromised patients. The compounds themselves, methods of making these compounds, and methods of using these compounds are all disclosed.
Abstract: This invention discloses compounds, and pharmaceutically acceptable salts thereof, useful in therapeutically and/or prophylactically treating patients with an illness. Such illnesses include cancer, and secondary infections caused by Pneumocystis carinii and Toxoplasmosis gondii in immunocompromised patients. The compounds themselves, methods of making these compounds, and methods of using these compounds are all disclosed. More specifically, furo[2,3-d[pyrimidines are disclosed.
Abstract: This invention discloses compounds, and pharmaceutically acceptable salts thereof, useful in therapeutically and/or prophylactically treating patients with an illness. Such illnesses include cancer, and secondary infections caused by Pneumocystis carinii and Toxoplasmosis gondii in immunocompromised patients. The compounds themselves, methods of making these compounds, and methods of using these compounds are all disclosed.
Abstract: This invention discloses compounds, and pharmaceutically acceptable salts thereof, useful in therapeutically and/or prophylactically treating patients with an illness. Such illnesses include cancer, and secondary infections caused by Pneumocystis carinii and Toxoplasmosis gondii in immunocompromised patients. The compounds themselves, methods of making these compounds, and methods of using these compounds are all disclosed. More specifically, the compounds include pyrrolo?2,3-d!pyrimidines and furo?2,3-d!pyrimides and derivatives thereof.
Abstract: Pyrrolo?2,3-d!pyrimidine derivatives, and pharmaceutical acceptable salts thereof, useful in therapeutically and/or prophylactically treating patients with an illness are disclosed.
Abstract: A method of creating a unique deacetylated, depolymerized chitosan which may be employed to provide a time release chitosan-drug complex. The chitosan is deacetylated at least 60 percent and preferably at least 70 percent. It is preferred to employ a chitosan having a molecular weight of about 3.5 kDa to 250 kDa and preferably about 3.5 kDa to 75 kDa. The complex may be employed in various delivery systems including tablets, films, matrix supported drug delivery units or as coatings or films on implants. A method of making a drug delivering implant includes providing an implant, creating a complex of a depolymerized chitosan and a drug and establishing a layer of a chitosan drug complex on at least a portion of said implant. The chitosan-drug complex is preferably created through ionic bonding and may be a coating or a film self-adhered to a portion of an exterior surface of the implant. It is also preferred to deacetylate the chitosan prior to depolymerization.
Abstract: A method of microwave assisted chemical reaction includes providing a microwavable reaction vessel which contains at least one material in a sample. The sample is heated by microwave energy to elevate the temperature of the reagent and at least partially volatilize the sample to establish a gas phase within the vessel followed by positive cooling of the gas phase to reduce the temperature and responsively reduce the pressure of the gas phase without effecting substantial cooling of the liquid phase. The method may involve employing cooling exteriorly of and adjacent to the gas phase containing portion of the vessel or cooling by means of a coolant flowing within coils disposed in the interior of the vessel or both. The process is preferably a continuous process. The apparatus may be a vessel transparent to microwave energy for receiving the sample. The vessel has space overlying the liquid phase containing portion for a gas phase.
Abstract: Sulfatase inhibitor compounds having the formula: ##STR1## wherein X, Y, R.sub.1, R.sub.2 and R.sub.3 are as defined in the specification. The compounds are useful in the treatment of estrogen dependent illnesses. Methods for synthesizing these compounds are also disclosed.
Abstract: This invention discloses compounds, and pharmaceutically acceptable salts thereof, useful in therapeutically and/or prophylactically treating patients with an illness. Such illnesses include cancer, and secondary infections caused by Pneumocystis carinii and Toxoplasmosis gondii in immunocompromised patients. The compounds themselves, methods of making these compounds, and methods of using these compounds are all disclosed.
Abstract: This invention discloses compounds useful as steroid sulfatase inhibitors. The compounds comprise the formula (1) ##STR1## wherein (a) R is selected from the group consisting of hydrogen, a lower alkyl group, an alkoxy group, halogen, NH.sub.2, NO.sub.2, C.tbd.N and N.dbd.C.dbd.S; and (b) the ring system ABCD is a steroid nucleus selected from the group consisting of estrone, dehydroepiandrosterone, estradiols, estradiolesters, pregnenolone, substituted estrones, substituted dehydroepiandrosterones, substituted estradiols, substituted estradiolesters and substituted pregnenolone. The compounds also comprise the formula (5) ##STR2## wherein (a) R.sub.1 is hydrogen and R.sub.2 is selected from the group consisting of SO.sub.2 CF.sub.3, SO.sub.2 NH.sub.2, SO.sub.2 (C.sub.1 -C.sub.6 -alkyl), COCF.sub.3, CONH.sub.2, CO(C.sub.1 -C.sub.