Patents by Inventor Cynthia A. Gates

Cynthia A. Gates has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Patent number: 8187874
    Abstract: The present invention relates to drug discovery methods, particularly antiviral drug discovery methods.
    Type: Grant
    Filed: October 27, 2004
    Date of Patent: May 29, 2012
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Robert B. Perni, Cynthia Gates, John Thomson
  • Publication number: 20060003317
    Abstract: The present invention relates to drug discovery methods, particularly antiviral drug discovery methods.
    Type: Application
    Filed: October 27, 2004
    Publication date: January 5, 2006
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Robert Perni, Cynthia Gates, John Thomson
  • Patent number: 6413951
    Abstract: The invention relates to 20&xgr;-fluoropregna-4,17(20)-dien-3-on-21-oic acid ethyl ester, 20&xgr;-fluoro-3&bgr;-hydroxypregna-5,17(20)-dien-21-oic acid ethyl ester, 20&xgr;-fluoro-21-hydroxypregna-4,17 (20)-dien-3-one, 20&xgr;-fluoropregna-5,17(20)-dien-3&bgr;,21-diol and related compounds and to compositions incorporating these compounds, as well as the inhibition of C17,20 lyase, 5&agr;-reductase and C17-hydroxylase, and to the use of these compounds in the treatment of androgen and estrogen mediated or dependent disorders, including benign prostatic hyperplasia, prostate cancer, breast cancer and DHT-mediated disorders such as acne and hirsutism. Treatment of disorders related to the over synthesis of cortisol, for example, Cushing's Syndrome are also included. The treatment of androgen-dependent disorders also includes a combination therapy with known androgen-receptor antagonists, such as flutamide.
    Type: Grant
    Filed: June 21, 2001
    Date of Patent: July 2, 2002
    Assignee: Aventis Pharmaceuticals, Inc.
    Inventors: Norton P. Peet, Philip M. Weintraub, Joseph P. Burkhart, Cynthia A. Gates
  • Patent number: 6365597
    Abstract: The invention related to 4-aza-17&bgr;-(cyclopropoxy)-androst-5&agr;-androstan-3-one, 4-aza-17&bgr;-(cyclopropylamino)-androst-4-en-3-one and related compounds and to compositions incorporating these compounds, as well as the inhibition of C17-20 lyase, 5&agr;-reductase and C17&agr;-hydroxylase and to the use of these compounds in the treatment of androgen and estrogen mediated disorders, including benign prostatic hyperplasia, androgen mediated prostate cancer, estrogen mediated breast cancer and to DHT-mediated disorders such as acne. Disorders relating to the oversynthesis of cortisol, for example, Cushing's Syndrome, are also included. The treatment of androgen-dependent disorders also includes a combination therapy with known androgen-receptor antagonists, such as flutamide.
    Type: Grant
    Filed: February 11, 1997
    Date of Patent: April 2, 2002
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: James R. Pribish, Cynthia A. Gates, Philip M. Weintraub
  • Publication number: 20020019548
    Abstract: The invention related to 20&xgr;-fluoropregna-4,17(20)-dien-3-on-21-oic acid ethyl ester, 20&xgr;-fluoro-3&bgr;-hydroxypregna-4,17(20)-dien-21-oic acid ethyl ester, 20&xgr;-fluoro-21-hydroxypregna-4,17(20)-dien-3-one, 20&xgr;-fluoropregna-4,17(20)-dien-3&bgr;,21-diol and related compounds and to compositions incorporating these compounds, as well as the inhibition of C17,20 lyase, 5&agr;-reductase and C17-hydroxylase, and to the use of these compounds in the treatment of androgen and estrogen mediated or dependent disorders, including benign prostatic hyperplasia, prostate cancer, breast cancer and DHT-mediated disorders such as acne and hirsutism. Treatment of disorders related to the over synthesis of cortisol, for example, Cushing's Syndrome are also included. The treatment of androgen-dependent disorders also includes a combination therapy with known androgen-receptor antagonists, such as flutamide.
    Type: Application
    Filed: June 21, 2001
    Publication date: February 14, 2002
    Inventors: Norton P. Peet, Philip M. Weintraub, Joseph P. Burkhart, Cynthia A. Gates
  • 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: 5977094
    Abstract: The present invention relates to methods and compositions using .DELTA..sup.16 unsaturated steroids which are useful as steroid C.sub.17-20 lyase inhibitors.
    Type: Grant
    Filed: May 6, 1998
    Date of Patent: November 2, 1999
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Norton P. Peet, Joseph P. Burkhart, Cynthia A. Gates
  • Patent number: 5965548
    Abstract: The present invention relates to .DELTA..sup.16 unsaturated steroids which are useful as steroid C.sub.17-20 lyase inhibitors.
    Type: Grant
    Filed: May 6, 1998
    Date of Patent: October 12, 1999
    Assignee: Merrel Pharmaceuticals, Inc.
    Inventors: Norton P. Peet, Joseph P. Burkhart, Cynthia A. Gates
  • 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: 5869475
    Abstract: The invention discloses 3-ketosteroids of the following formula used to inhibit steroid 5.alpha.-reductase: ##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, cyclopropoxy, acetylthioalkane, cyclopylamino, 2-2-dimethyldioxolan-4-yl, 1,2-dihydroxyethyl and C.sub.1-4 alkanethiol;R.sub.1 is hydrogen, hydroxy or C.sub.1-6 alkyl;R.sub.1 and R.sub.2 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.1-6 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.1-8 alkyl;R.sub.8 is C.sub.1-8 alkyl; andwith the proviso that, when R is OH, then R.sub.1 is hydrogen; and with the proviso that, when R.sub.5 is OH, then R.sub.6 is hydrogen.
    Type: Grant
    Filed: November 14, 1997
    Date of Patent: February 9, 1999
    Assignee: Merrell Pharmaceuticals, Inc.
    Inventors: Timothy Thomas Curran, Chi-Hsin Richard King, Gary Alan Flynn, Philip M. Weintraub, Michael R. Angelastro, Cynthia A. Gates
  • Patent number: 5750744
    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-nitro-steroid; and then;b) reacting the 4-nitrosteroid with a suitable reducing agent.
    Type: Grant
    Filed: February 11, 1997
    Date of Patent: May 12, 1998
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Philip M. Weintraub, Cynthia A. Gates, Michael R. Angelastro, Gary Alan Flynn, Chi-Hsin Richard King, Timothy Thomas Curran
  • Patent number: 5677293
    Abstract: The present invention relates to .DELTA..sup.16 unsaturated C.sub.17 heterocyclic steroids which are useful as steroid C.sub.17-20 lyase inhibitors.
    Type: Grant
    Filed: July 15, 1996
    Date of Patent: October 14, 1997
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Norton P. Peet, Joseph P. Burkhart, Cynthia A. Gates
  • Patent number: 5486511
    Abstract: This invention is directed to 4-amino-17.beta.-(cyclopropyloxy)androst-4-en-3-one, 4-amino-17.beta.-(cyclopropylylamino)androst-4-en-3-one and related compounds, a process for their synthesis, a pharmaceutical composition having C.sub.17-20 lyase and 5.alpha.-reductase inhibitory activity, the use of the present compounds as C.sub.17-20 lyase and 5.alpha.-reductase inhibitors and also to a method for using such compounds in the treatment of androgen and/or estrogen dependent disorders, including bengin prostatic hyperplasia, breast cancer and prostatic cancer. The 4-amino compounds are prepared by the reaction of the appropriate 4,5-epoxide with sodium azide in an inert solvent in the presence of a catalytic amount of strong acid under appropriate reaction conditions. Alternatively, the 4-amino compounds are prepared by first nitration and then reduction of the appropriate steroid under appropriate reaction conditions.
    Type: Grant
    Filed: May 2, 1994
    Date of Patent: January 23, 1996
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Philip M. Weintraub, Cynthia A. Gates, Michael R. Angelastro, Timothy T. Curran, J. O'Neal Johnston
  • Patent number: 5143909
    Abstract: The present invention relates to a method for the inhibition of C.sub.17-20 lyase enzyme which comprises administering to a patient in need of such inhibition, an effective amount of certain 4-amino-17-(hydroxyalkyl or dihydroxyalkyl)steroids or their esters or ethers. Certain of the aminosteroids used in the process are novel compounds.
    Type: Grant
    Filed: March 19, 1991
    Date of Patent: September 1, 1992
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Philip M. Weintraub, Cynthia A. Gates, Thomas R. Blohm