The Nitrogen Is Bonded Directly At The 17-position Patents (Class 552/522)
  • Patent number: 10087211
    Abstract: This invention describes compounds of Structures 1, 2, and 3 and their use as allosteric modulators of the GABA receptor chloride ionophore complex to alleviate stress, anxiety, mood disorders, seizures, depression, treatment of drug and alcohol abuse, memory, premenstrual disorders, and neural system damage.
    Type: Grant
    Filed: November 2, 2016
    Date of Patent: October 2, 2018
    Assignees: RESEARCH TRIANGLE INSTITUTE, THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES
    Inventors: Scott P. Runyon, Michael Rogawski, Edgar Cook, John Kepler, Hernan Navarro, Rafal Kaminski, Matthew Orr
  • Patent number: 9518080
    Abstract: This invention describes compounds of Structures 1, 2, and 3 and their use as allosteric modulators of the GABA receptor chloride ionophore complex to alleviate stress, anxiety, mood disorders, seizures, depression, treatment of drug and alcohol abuse, memory, premenstrual disorders, and neural system damage.
    Type: Grant
    Filed: August 23, 2013
    Date of Patent: December 13, 2016
    Assignees: RESEARCH TRIANGLE INSTITUTE, The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventors: Scott P Runyon, Michael Rogawski, Edgar Cook, John Kepler, Hernan Navarro, Rafal Kaminski, Matthew Orr
  • Patent number: 9266815
    Abstract: Disclosed herein are novel motuporamine compounds that act as anti-metastatic agents with low toxicity and high anti-migration activity. The non-toxic, anti-metastatic agents may be given to patients with potential or actual metastatic cancers, such as pancreatic cancers, alone in combination with known and/or new therapies to help block the growth and spread of tumor(s).
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: February 23, 2016
    Assignee: University of Central Florida Research Foundation, Inc.
    Inventors: Otto Phanstiel, IV, Aaron Muth
  • Publication number: 20140235600
    Abstract: The present disclosure is generally directed to neuroactive 19-alkoxy-17-substituted steroids as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.
    Type: Application
    Filed: December 18, 2013
    Publication date: August 21, 2014
    Applicant: Washington University
    Inventors: Douglas Covey, Albert Jean Robichaud
  • Publication number: 20140094619
    Abstract: This invention describes compounds of Structures 1, 2, and 3 and their use as allosteric modulators of the GABA receptor chloride ionophore complex to alleviate stress, anxiety, mood disorders, seizures, depression, treatment of drug and alcohol abuse, memory, premenstrual disorders, and neural system damage.
    Type: Application
    Filed: August 23, 2013
    Publication date: April 3, 2014
    Applicants: US GOV BY THE SEC. OF DEPT. OF HEALTH & HUMAN SERV, RESEARCH TRIANGLE INSTITUTE
    Inventors: Scott P. RUNYON, Michael ROGAWSKI, Edgar COOK, John KEPLER, Hernan NAVARRO, Rafal KAMINSKI, Matthew ORR
  • Patent number: 8586770
    Abstract: The invention relates to methods to manipulate stem cells in vivo and in vitro to treat, e.g., a condition where cell or tissue repair is needed.
    Type: Grant
    Filed: February 18, 2011
    Date of Patent: November 19, 2013
    Assignee: Harbor Therapeutics, Inc.
    Inventor: James M. Frincke
  • Patent number: 8575375
    Abstract: This invention describes compounds of Structures 1, 2, and 3 and their use as allosteric modulators of the GABA receptor chloride ionophore complex to alleviate stress, anxiety, mood disorders, seizures, depression, treatment of drug and alcohol abuse, memory, premenstrual disorders, and neural system damage.
    Type: Grant
    Filed: June 16, 2008
    Date of Patent: November 5, 2013
    Assignees: Research Triangle Institute, The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventors: Scott P. Runyon, Michael A. Rogawski, John Kepler, Hernan Navarro, Rafal Kaminski, Matthew Orr, Kevin M. Cook
  • Patent number: 8569275
    Abstract: The invention relates to the use of compounds to ameliorate or treat an condition such as a cystic fibrosis, neutropenia or other exemplified conditions. Exemplary compounds that can be used include 3?-hydroxy-17?-aminoandrost-5-ene, 3?-hydroxy-16?-fluoro-17?-aminoandrost-5-ene, 3?-hydroxy-16?-fluoro-17?-aminoandrost-5-ene, 3?-hydroxy-16?-fluoro-17?-aminoandrost-5-ene, 1?,3?-dihydroxy-4?-fluoroandrost-5-ene-17-one, 1?,3?,17?-trihydroxy-4?-fluoroandrost-5-ene, 1?,3?-dihydroxy-6?-bromoandrost-5-ene, 1?-fluoro-3?,12?-dihydroxyandrost-5-ene-17-one, 1?-fluoro-3?,4?-dihydroxyandrost-5-ene and 4?-fluoro-3?,6?,17?-trihydroxyandrostane.
    Type: Grant
    Filed: April 27, 2011
    Date of Patent: October 29, 2013
    Assignee: Harbor Therapeutics, Inc.
    Inventor: James M. Frincke
  • Publication number: 20130266645
    Abstract: The present invention relates to compounds derived from steroids of the general formula (I) wherein L represents a linker and R# represents a steroid residue, the use of compounds of the general formula (I) in medicine and for the prophylaxis and/or the treatment of infectious diseases. Furthermore described are pharmaceutical compositions containing at least one compound of the general formula (I). A further aspect of the invention relates to the synthesis of said compounds of the general formula (I).
    Type: Application
    Filed: October 6, 2011
    Publication date: October 10, 2013
    Applicant: Justus-Liebig-Universitat Giessen
    Inventors: Katja Becker, Reimar Krieg, Bruno Schönecker
  • Publication number: 20110212935
    Abstract: The invention relates to the use of compounds to ameliorate or treat an condition such as a cystic fibrosis, neutropenia or other exemplified conditions. Exemplary compounds that can be used include 3?-hydroxy-17?-aminoandrost-5-ene, 3?-hydroxy-16?-fluoro-17?-aminoandrost-5-ene, 3?-hydroxy-16?-fluoro-17?-aminoandrost-5-ene, 3?-hydroxy-16?-fluoro-17?-aminoandrost-5-ene, 1?,3?-dihydroxy-4?-fluoroandrost-5-ene-17-one, 1?,3?,17?-trihydroxy-4?-fluoroandrost-5-ene, 1?,3?-dihydroxy-6?-bromoandrost-5-ene, 1?-fluoro-3?,12?-dihydroxyandrost-5-ene-17-one, 1?-fluoro-3?,4?-dihydroxyandrost-5-ene and 4?-fluoro-3?,6?,17?-trihydroxyandrostane.
    Type: Application
    Filed: April 27, 2011
    Publication date: September 1, 2011
    Applicant: Harbor BioSciences, Inc.
    Inventor: James M. Frincke
  • Publication number: 20110092473
    Abstract: This invention describes compounds of Structures 1, 2, and 3 and their use as allosteric modulators of the GABA receptor chloride ionophore complex to alleviate stress, anxiety, mood disorders, seizures, depression, treatment of drug and alcohol abuse, memory, premenstrual disorders, and neural system damage.
    Type: Application
    Filed: June 16, 2008
    Publication date: April 21, 2011
    Applicants: Research Triangle Institute, US GOV BY THE SEC. OF DEPT. OF HEALTH & HUMAN SERV.
    Inventors: Scott P. Runyon, Michael Rogawski, Edgar Cook, Kevin M. Cook, John Kepler, Hernan Navarro, Rafal Kaminski, Matthew Orr
  • Patent number: 7910571
    Abstract: The invention relates to the use of compounds to ameliorate or treat an condition such as a cystic fibrosis, neutropenia or other exemplified conditions. Exemplary compounds that can be used include 3?-hydroxy-17?-aminoandrost-5-ene, 3?-hydroxy-16?-fluoro-17?-aminoandrost-5-ene, 3?-hydroxy-16?-fluoro-17?-aminoandrost-5-ene, 3?-hydroxy-16?-fluoro-17?-aminoandrost-5-ene, 1?,3?-dihydroxy-4?-fluoroandrost-5-ene-17-one, 1?,3?,17?-trihydroxy-4?-fluoroandrost-5-ene, 1?,3?-dihydroxy-6?-bromoandrost-5-ene, 1?-fluoro-3?,12?-dihydroxyandrost-5-ene-17-one, 1?-fluoro-3?,4?-dihydroxyandrost-5-ene and 4?-fluoro-3?,6?,17?-trihydroxyandrostane.
    Type: Grant
    Filed: October 13, 2006
    Date of Patent: March 22, 2011
    Assignee: Harbor BioSciences, Inc.
    Inventor: James M. Frincke
  • Publication number: 20100069627
    Abstract: The invention relates to a diastereoselective method for obtaining a primary amine on a steroid, comprising the reduction of an oxime by lithium in ammonia at a low temperature in an ether/alcohol mixture.
    Type: Application
    Filed: June 12, 2009
    Publication date: March 18, 2010
    Applicant: SANOFI-AVENTIS
    Inventors: Gilles ODDON, Daniel BERNARD, Gerard CAZENAVE, Andre SIMONNET, Joelle BOUSQUET-FRANCES
  • Patent number: 7135581
    Abstract: Compositions and methods for treating mammalian disease characterized by undesirable angiogenesis by administering derivatives of 2-methoxyestradiol of the general formula: wherein the variables are defined in the specification.
    Type: Grant
    Filed: August 24, 2001
    Date of Patent: November 14, 2006
    Assignee: Entremed, Inc.
    Inventors: Gregory E. Agoston, Jamshed H. Shah, Kimberly A. Hunsucker, Victor S. Pribluda, Theresa M. LaVallee, Shawn J. Green, Christopher J. Herbstritt, Xiaoguo H. Zhan, Anthony M. Treston
  • Patent number: 6995278
    Abstract: Compositions and methods for treating mammalian disease characterized by undesirable angiogenesis by administering derivatives of 2-methoxyestradiol of the general formula: wherein the variables are defined in the specification.
    Type: Grant
    Filed: February 8, 2001
    Date of Patent: February 7, 2006
    Assignee: Entre Med, Inc.
    Inventors: Gregory E. Agoston, Victor Pribluda, Anthony M. Treston, Shawn J. Green
  • Patent number: 6562805
    Abstract: The present invention relates to methods, compounds and compositions for inhibiting effective binding of a chemokine to its cellular receptor. In one form of the invention, a method includes contacting a cellular population with an effective amount of cosalane or an analog thereof. The invention further relates to methods, compounds and compositions for treating inflammatory diseases. In one form, a method includes administering to a patient a therapeutically effective amount of cosalane or an analog thereof.
    Type: Grant
    Filed: January 29, 2001
    Date of Patent: May 13, 2003
    Assignees: Purdue Research Foundation, The United States of America as represented by the Department of Health and Human Services
    Inventors: Mark S. Cushman, O. M. Zack Howard
  • Patent number: 6436918
    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: November 8, 2001
    Date of Patent: August 20, 2002
    Assignees: Duquesne University of the Holy Ghost, Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Pui-Kai Li, Chikara Murakata, Shiro Akinaga
  • Patent number: 6399595
    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.
    Inventors: Pui-Kai Li, Chikara Murakata, Shiro Akinaga
  • Patent number: 6262042
    Abstract: The invention is directed to a novel class of steroids which exhibit potent antiprogestational activity.
    Type: Grant
    Filed: May 29, 1998
    Date of Patent: July 17, 2001
    Assignee: Research Triangle Institute
    Inventors: C. Edgar Cook, John A. Kepler, Gary S. Bartley
  • Patent number: 6136992
    Abstract: 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.
    Type: Grant
    Filed: March 12, 1998
    Date of Patent: October 24, 2000
    Assignees: The United States of America as represented by the Department of Health and Human Services, Pharm-Eco Laboratories, Incorporated
    Inventors: Siya Ram, Ravi Varma, Yesh Sachdeva
  • Patent number: 6093707
    Abstract: The invention is directed to a novel class of steroids which exhibit potent antiprogestational activity.
    Type: Grant
    Filed: November 5, 1999
    Date of Patent: July 25, 2000
    Assignee: Research Triangle Institute
    Inventors: C. Edgar Cook, John A. Kepler, Rupa S. Shetty, Gary S. Bartley, David Yue-wei Lee
  • Patent number: 5990328
    Abstract: The present invention provides 4-nitro-.DELTA..sup.4 -3-ketosteroids, their use as steroid C.sub.17-20 lyase and 5.alpha.-reductase inhibitors and to a novel process for preparing a compound of the formula: ##STR1## comprising sequentially: a) reacting a starting compound of the formula ##STR2## with an effective amount of a strong base at an elevated or suitable temperature for a time sufficient to create the corresponding thermodynamic dienolate, followed by addition of a neutral nitrating agent to produce the 4-nitrosteroid; and then;b) reacting the 4-nitrosteroid with a suitable reducing agent.
    Type: Grant
    Filed: February 24, 1999
    Date of Patent: November 23, 1999
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Philip M. Weintraub, Michael R. Angelastro, Cynthia A. Gates, Gary Alan Flynn, Timothy Thomas Curran, Chi-Hsin Richard King
  • Patent number: 5965550
    Abstract: The invention discloses 3-ketosteroids of the following formula used to inhibit steroid C.sub.17-20 lyase: ##STR1## wherein R is OH, C.sub.1 -C.sub.6 alkanoyl, C.sub.1 -C.sub.6 alkanoyloxy, C.sub.1 -C.sub.4 alkanol, COCH.sub.2 OH, CO.sub.2 H, CONR.sub.7 R.sub.8, cyclopropyloxy, cyclopropylamino, acetylthioalkane, 2,2-dimethyldioxolan4-yl, 1,2-dihydroxyethyl and C.sub.1-4 alkylthiol;R.sub.1 is hydrogen, hydroxy or C.sub.1-6 alkyl;R and R.sub.1 together may indicate .dbd.O, that is an oxygen double bonded to the 17 carbon;R.sub.2, R.sub.3, and R.sub.4 are each independently hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.5 and R.sub.6 are each independently hydrogen or OH;R.sub.5 and R.sub.6 together may indicate .dbd.O, that is an oxygen double bonded to the 11 carbon;R.sub.7 is hydrogen or C.sub.1 -C.sub.8 alkyl;R.sub.8 is C.sub.1 -C.sub.8 alkyl; andwith the proviso that, when R is OH, then R.sub.1 is hydrogen; andwith the proviso that, when R.sub.5 is OH, then R.sub.6 is hydrogen.
    Type: Grant
    Filed: January 22, 1998
    Date of Patent: October 12, 1999
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Philip M. Weintraub, Michael R. Angelastro, Cynthia A. Gates, Timothy Thomas Curran, Gary Alan Flynn, Chi-Hsin Richard King
  • Patent number: 5910478
    Abstract: The present invention provides peptides, cyclized peptides and peptidomimetics which inhibit the oncogenic and/or transforming activity of the p21 ras protein, pharmaceutical compositions containing at least one of the ras-inhibiting peptides, cyclized peptides and peptidomimetics, and methods for inhibiting the ras-mediated oncogenic and/or transformation process in mammalian cells or tissues.
    Type: Grant
    Filed: September 20, 1996
    Date of Patent: June 8, 1999
    Assignee: Innapharma, Inc.
    Inventors: Joseph J. Hlavka, John Fowler Noble, Henry Baxter Abajian, Andrew S. Kende, Matthew R. Pincus
  • Patent number: 5892069
    Abstract: The application discloses methods of treating mammalian diseases characterized by abnormal cell mitosis by administering estradiol derivatives including those comprising colchicine or combretastatin A-4 structural motifs of the general formulae found below in a dosage sufficient to inhibit cell mitosis. The application discloses novel compounds used in the methods.
    Type: Grant
    Filed: April 25, 1997
    Date of Patent: April 6, 1999
    Assignee: The Children's Medical Center Corporation
    Inventors: Robert John D'Amato, Moses Judah Folkman
  • Patent number: 5880115
    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.
    Type: Grant
    Filed: July 18, 1997
    Date of Patent: March 9, 1999
    Assignee: Duquesne University of the Holy Ghost
    Inventors: Pui-Kai Li, Kyle W. Selcer
  • Patent number: 5621123
    Abstract: Provided are cyclic hydrocarbons of Formula I ##STR1## with an aminoalkyl sidechain that are useful for treating phospholipase A2 mediated conditions, diabetes, and obesity.
    Type: Grant
    Filed: May 20, 1994
    Date of Patent: April 15, 1997
    Assignee: The Upjohn Company
    Inventors: Roy A. Johnson, Gordon L. Bundy, Gilbert A. Youngdale, Douglas R. Morton, Donald P. Wallach, deceased, Vera M. Wallach, legal representative
  • Patent number: 5599806
    Abstract: The invention describes hydrazino and hydroxyamino-14.beta.-hydroxyandrostane derivatives having general formula (I): ##STR1## wherein the symbol means .alpha. or .beta. configuration and A, B, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 have the meanings given in the description and their use in the treatment of cardiovascular disorders such as heart failure and hypertension.
    Type: Grant
    Filed: May 18, 1995
    Date of Patent: February 4, 1997
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Alberto Cerri, Giuseppe Bianchi, Patrizia Ferrari, Elena Folpini, Piero Melloni
  • Patent number: 5439899
    Abstract: Novel compounds having anti-HIV activity are disclosed along with formulations and methods for treating human immunodeficiency viral infections employing these compounds.
    Type: Grant
    Filed: March 10, 1993
    Date of Patent: August 8, 1995
    Assignees: Purdue Research Foundation, The United States of America as represented by the Department of Health and Human Services
    Inventors: Mark Cushman, Rudiger D. Haugwitz, Wieslaw M. Golebiewski
  • Patent number: 5372996
    Abstract: A method of treatment of androgen-related diseases such as prostate cancer in susceptible male animals, including humans, comprises administering novel antiandrogens and/or novel sex steroid biosynthesis inhibitors as part of a combination therapy. Sex steroid biosynthesis inhibitors, especially those capable of inhibiting conversion of dehydroepiandrosterone (DHEA) or 4-androstenedione (.DELTA..sup.4 -dione) to natural sex steroida (and testosterone into dihydrotestosterone) in peripheral tissues, are used in combination with antiandrogens usually after blockade of testicular hormonal secretions. Antiestrogens can also be part of the combination therapy. Pharmaceutical compositions and two, three, four and five component kits are useful for such combination treatment.
    Type: Grant
    Filed: October 19, 1992
    Date of Patent: December 13, 1994
    Assignee: Endorecherche, Inc.
    Inventor: Fernand Labrie
  • Patent number: 5334712
    Abstract: Provided are cyclic hydrocarbons of Formula I ##STR1## with an aminoalkyl sidechain that are useful for treating phospholipase A2 mediated conditions, diabetes, and obesity.
    Type: Grant
    Filed: November 16, 1992
    Date of Patent: August 2, 1994
    Assignee: The Upjohn Company
    Inventors: Roy A. Johnson, Gordon L. Bundy, Gilbert A. Youngdale, Douglas R. Morton, Donald P. Wallach, deceased
  • Patent number: 5274089
    Abstract: Provided are cyclic hydrocarbons of Formula I ##STR1## with an aminoalkyl sidechain that are useful for treating phospholipase A2 mediated conditions, diabetes, and obesity.
    Type: Grant
    Filed: November 6, 1992
    Date of Patent: December 28, 1993
    Assignee: The Upjohn Company
    Inventors: Gordon L. Bundy, Donald P. Wallach, deceased
  • Patent number: 5187299
    Abstract: Provided are cyclic hydrocarbons of Formula I ##STR1## with an aminoalkyl sidechain.
    Type: Grant
    Filed: November 13, 1991
    Date of Patent: February 16, 1993
    Assignee: The Upjohn Company
    Inventors: Roy A. Johnson, Gordon L. Bundy, Gilbert A. Youngdale, Douglas R. Morton, Donald P. Wallach, deceased, Wallach, Legal Representative, by Vera M.
  • Patent number: 5157031
    Type: Grant
    Filed: March 21, 1989
    Date of Patent: October 20, 1992
    Assignee: Research Corporation Technologies, Inc.
    Inventors: Arthur G. Schwartz, Marvin L. Lewbart
  • Patent number: 5093502
    Abstract: A process for the preparation of novel 14.alpha., 17.alpha.-dihydroxy-17.beta.-substituted steroids by reacting 14.alpha.-hydroxy-17-oxo-steroids with metal organic compounds and the use of the said novel steroids in the production of 14.alpha., 17.alpha.-methylenedioxy-pregnane derivatives.
    Type: Grant
    Filed: February 16, 1990
    Date of Patent: March 3, 1992
    Assignee: Akzo N.V.
    Inventors: Peter M. Smid, Willem J. Van Zoest, Pieter G. Weber, Arthur F. Marx
  • Patent number: 5075434
    Abstract: This invention is a compound of formula 1 and pharmaceutically acceptable salts thereof; ##STR1## wherein R.sub.1 is fluorine, chlorine or bromine; wherein R.sub.2 is hydrogen or (C.sub.1 -C.sub.3) alkyl; wherein n is one or 2; wherein R.sub.3 is phenyl, 2-furyl, 3-furyl, 2-thienyl, 3-thienyl, 2-pyridinyl, 3-pyridinyl, 4-pyridinyl; wherein phenyl is optionally substituted with one substituent selected from the group consisting of halogen, trifluoromethyl or sulfonamide. These compounds are useful as hypoglycemic agents.
    Type: Grant
    Filed: September 20, 1990
    Date of Patent: December 24, 1991
    Assignee: The Upjohn Company
    Inventor: Gilbert A. Youngdale
  • Patent number: 5075464
    Abstract: This invention is directed to 17.beta.-(cyclopropylamino)androstenes and also to a method for using such compounds in the treatment of androgen-dependent disorders. The compounds are prepared by the hydride reduction of an appropriate steroidal imine or enamine.
    Type: Grant
    Filed: June 14, 1989
    Date of Patent: December 24, 1991
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Thomas R. Blohm, Michael R. Angelastro
  • Patent number: 4966898
    Abstract: This invention is directed to 4-substituted 17.beta.-(cyclopropylamino)androst-5-en-3.beta.-ol and related compounds and also to a method for using such compounds in the treatment of androgen-dependent disorders. The compounds are prepared by the hydride reduction of an appropriate steroidal imine or enamine.
    Type: Grant
    Filed: August 15, 1989
    Date of Patent: October 30, 1990
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Michael R. Angelastro, Thomas R. Blohm
  • Patent number: 4954446
    Abstract: Invented are substituted acrylate analogues of steroidal synthetic compounds, pharmaceutial compositions containing the compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase including using these compounds to reduce prostate size. Also invented are intermediates used in preparing these compounds.
    Type: Grant
    Filed: July 14, 1989
    Date of Patent: September 4, 1990
    Assignee: SmithKline Beecham Corporation
    Inventors: Dennis A. Holt, Mark A. Levy, Brian W. Metcalf
  • Patent number: 4917826
    Abstract: Provided are cyclic hydrocarbons of Formula I ##STR1## with an aminoalkyl sidechain that are useful for treating phospholipase A2 mediated conditions, diabetes, and obesity.
    Type: Grant
    Filed: June 16, 1987
    Date of Patent: April 17, 1990
    Assignee: The Upjohn Company
    Inventors: Roy A. Johnson, Gordon L. Bundy, Gilbert A. Youngdale, Douglas R. Morton, Donald P. Wallach, deceased