Patents by Inventor Gary S. Grubb
Gary S. Grubb 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).
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Publication number: 20120220558Abstract: The present invention provides methods of inducing contraception which includes delivering to a female a composition containing a compound of formula I, or tautomers thereof, in a regimen which involves delivering one or more of a selective estrogen receptor modulator, wherein formula I is: and wherein R1-R5 and Q1 are defined as described herein. Methods of providing hormone replacement therapy and for treating carcinomas, dysfunctional bleeding, uterine leiomyomata, endometriosis, and polycystic ovary syndrome is provided which includes delivering a compound of formula I and a selective estrogen receptor modulator are also described.Type: ApplicationFiled: May 8, 2012Publication date: August 30, 2012Applicant: Wyeth LLCInventors: Andrew Fensome, Gary S. Grubb, Diane Deborah Harrison, Richard Craig Winneker
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Patent number: 8242098Abstract: The present invention provides methods of inducing contraception which includes delivering to a female a composition containing a compound of formula I, or tautomers thereof, in a regimen which involves delivering one or more of a selective estrogen receptor modulator, wherein formula I is: and wherein R1-R5 and Q1 are defined as described herein. Methods of providing hormone replacement therapy and for treating carcinomas, dysfunctional bleeding, uterine leiomyomata, endometriosis, and polycystic ovary syndrome is provided which includes delivering a compound of formula I and a selective estrogen receptor modulator are also described.Type: GrantFiled: December 17, 2008Date of Patent: August 14, 2012Assignee: Wyeth LLCInventors: Andrew Fensome, Gary S. Grubb, Diane Deborah Harrison, Richard Craig Winneker
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Publication number: 20090099223Abstract: The present invention provides methods of inducing contraception which includes delivering to a female a composition containing a compound of formula I, or tautomers thereof, in a regimen which involves delivering one or more of a selective estrogen receptor modulator, wherein formula I is: and wherein R1-R5 and Q1 are defined as described herein. Methods of providing hormone replacement therapy and for treating carcinomas, dysfunctional bleeding, uterine leiomyomata, endometriosis, and polycystic ovary syndrome is provided which includes delivering a compound of formula I and a selective estrogen receptor modulator are also described.Type: ApplicationFiled: December 17, 2008Publication date: April 16, 2009Applicant: WyethInventors: Andrew Fensome, Gary S. Grubb, Diane Deborah Harrison, Richard Craig Winneker
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Patent number: 7488734Abstract: The present invention provides methods of inducing contraception which includes delivering to a female a composition containing a compound of formula I, or tautomers thereof, in a regimen which involves delivering one or more of a selective estrogen receptor modulator, wherein formula I is: and wherein R1-R5 and Q1 are defined as described herein. Methods of providing hormone replacement therapy and for treating carcinomas, dysfunctional bleeding, uterine leiomyomata, endometriosis, and polycystic ovary syndrome is provided which includes delivering a compound of formula I and a selective estrogen receptor modulator are also described.Type: GrantFiled: June 23, 2003Date of Patent: February 10, 2009Assignee: WyethInventors: Andrew Fensome, Gary S. Grubb, Diane Deborah Harrison, Richard Craig Winneker
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Patent number: 7297688Abstract: The present invention provides a contraceptive kit which helps to overcome or ameliorate the problem of breakthrough bleeding and spotting associated with lowest dose (15-20 ug EE) estrogen contraceptives.Type: GrantFiled: June 1, 2001Date of Patent: November 20, 2007Assignee: WyethInventor: Gary S. Grubb
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Patent number: 7192956Abstract: The present invention provides methods of inducing contraception which includes delivering to a female a composition containing a compound of formula I or formula II, or tautomers thereof, in a regimen which involves delivering one or more of a selective estrogen receptor modulator, wherein formula I is: and wherein R1–R5 and Q1 are defined as described herein. Methods of providing hormone replacement therapy and for treating carcinomas, dysfunctional bleeding, uterine leiomyomata, endometriosis, and polycystic ovary syndrome is provided which includes delivering a compound of formula I and a selective estrogen receptor modulator are also described.Type: GrantFiled: June 23, 2003Date of Patent: March 20, 2007Assignee: WyethInventors: Andrew Fensome, Gary S. Grubb, Diane Deborah Harrison, Richard Craig Winneker, Puwen Zhang, Jeffrey Curtis Kern, Eugene Anthony Terefenko
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Patent number: 6794373Abstract: This invention relates to cyclic combination therapies and regimens utilizing indoline compounds which are antagonists of the progesterone receptor and having the general structure: A is O, S, or NR4; B is a bond or CR5R6; R4, to R6 are H, C1 to C6 alkyl, C2 to C6 alkenyl, C2 to C6 alkynyl, C3 to C8 cycloalkyl, aryl, or heterocyclic, or R4 and R5 are fused to form a ring; R1 is H, OH, NH2, C1 to C6 alkyl, C3 to C6 alkenyl, alkynyl, or CORA; RA is as defined; R2 is H, halogen, CN, NO2, C1 to C6 alkyl, C1 to C6 alkoxy, or C1 to C6 aminoalkyl; R3 is a substituted benzene ring, or heteroaromatic ring, in combination with a progestational agent and/or an estrogen to treat or prevent secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis, polycystic ovary syndrome, carcinomas and adenocarcinomas, and contraception, among others.Type: GrantFiled: March 1, 2002Date of Patent: September 21, 2004Assignees: Wyeth, Ligand Pharmaceuticals, Inc.Inventors: Gary S. Grubb, Puwen Zhang, Reinhold R. W. Bender, Jay E. Wrobel, James P. Edwards, Todd K. Jones, Christopher M. Tegley, Lin Zhi
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Patent number: 6759408Abstract: This invention relates to cyclic combination therapies and regimens utilizing substituted indoline derivative compounds which are antagonists of the progesterone receptor having the general structure: wherein R1 and R2 may be single substituents or fused; R3 is H, OH, NH2, C1 to C6 alkyl, CORC, or optionally substituted C1 to C6 alkyl, C3 to C6 alkenyl, or alkynyl; RC is H, or optionally substituted C1 to C3 alkyl, aryl, C1 to C3 alkoxy, or C1 to C3 aminoalkyl; R4 is H, halogen, CN, NO2, or optionally substituted C1 to C6 alkyl, alkynyl, C1 to C6 alkoxy, amino, or C1 to C6 aminoalkyl; and R5 is a benzene ring, a five or six membered heterocyclic ring; or pharmaceutically acceptable salt thereof. Methods of treatment include contraception, secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis, polycystic ovary syndrome, carcinomas, adenocarcinomas minimization of side effects, or food intake stimulation.Type: GrantFiled: May 9, 2002Date of Patent: July 6, 2004Assignees: Wyeth, Ligand Pharmaceuticals, Inc.Inventors: Gary S. Grubb, Puwen Zhang, Eugene A. Terefenko, Andrew Fensome, Jay E. Wrobel, Horace Fletcher, III, James P. Edwards, Todd K. Jones, Christopher M. Tegley, Lin Zhi
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Publication number: 20040006060Abstract: The present invention provides methods of inducing contraception which includes delivering to a female a composition containing a compound of formula I or formula II, or tautomers thereof, in a regimen which involves delivering one or more of a selective estrogen receptor modulator, wherein formula I is: 1Type: ApplicationFiled: June 23, 2003Publication date: January 8, 2004Applicant: WyethInventors: Andrew Fensome, Gary S. Grubb, Diane Deborah Harrison, Richard Craig Winneker, Puwen Zhang, Jeffrey Curtis Kern, Eugene Anthony Terefenko
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Publication number: 20040002535Abstract: The present invention provides methods of inducing contraception which includes delivering to a female a composition containing a compound of formula I, or tautomers thereof, in a regimen which involves delivering one or more of a selective estrogen receptor modulator, wherein formula I is: 1Type: ApplicationFiled: June 23, 2003Publication date: January 1, 2004Applicant: WyethInventors: Andrew Fensome, Gary S. Grubb, Diane Deborah Harrison, Richard Craig Winneker
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Publication number: 20030216368Abstract: This invention relates to methods for providing hormone replacement therapy in perimenopausal, menopausal, and postmenopausal women through the sequential administration of combinations of conjugated estrogens and trimegestone.Type: ApplicationFiled: May 15, 2003Publication date: November 20, 2003Applicant: WyethInventors: Gary S. Grubb, James H. Pickar
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Publication number: 20030191097Abstract: This invention relates to methods and pharmaceutical compositions for providing hormone replacement therapy in perimenopausal, menopausal, and postmenopausal women through the continuous administration of combinations of conjugated estrogens and trimegestone.Type: ApplicationFiled: April 1, 2003Publication date: October 9, 2003Applicant: WyethInventors: Gary S. Grubb, James H. Pickar, Ginger D. Constantine, Michael S. Dey
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Publication number: 20030191103Abstract: This invention relates to methods and pharmaceutical compositions for providing hormone replacement therapy in perimenopausal, menopausal, and postmenopausal women through the continuous administration of combinations of conjugated estrogens and trimegestone.Type: ApplicationFiled: April 1, 2003Publication date: October 9, 2003Applicant: WyethInventors: Gary S. Grubb, James H. Pickar, Ginger D. Constantine, Michael S. Dey
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Patent number: 6544970Abstract: This invention relates to cyclic combination therapies and regimens utilizing substituted indoline derivative compounds which are antagonists of the progesterone receptor having the general structure: wherein R1 and R2 may be single substituents or fused to form spirocyclic rings, in combination with progestins, estrogens, or both. These methods of treatment may be used for contraception, for the treatment and/or prevention of secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis, polycystic ovary syndrome, carcinomas and adenocarcinomas of the endometrium, ovary, breast, colon, or prostate, minimization of side effects, cyclic menstrual bleeding, or stimulation of food intake.Type: GrantFiled: May 22, 2002Date of Patent: April 8, 2003Assignees: WYETH, Ligand Pharmaceuticals, Inc.Inventors: Gary S. Grubb, Andrew Fensome, Lori L. Miller, John W. Ullrich, Reinhold H. W. Bender, Puwen Zhang, Jay E. Wrobel, James P. Edwards, Todd K. Jones, Christopher M. Tegley, Lin Zhi
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Publication number: 20030050288Abstract: This invention relates to cyclic combination therapies and regimens utilizing substituted indoline derivative compounds which are antagonists of the progesterone receptor having the general structure: 1Type: ApplicationFiled: May 22, 2002Publication date: March 13, 2003Applicant: WYETHInventors: Gary S. Grubb, Andrew Fensome, Lori L. Miller, John W. Ullrich, Reinhold H.W. Bender, Puwen Zhang, Jay E. Wrobel, James P. Edwards, Todd K. Jones, Christopher M. Tegley, Lin Zhi
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Publication number: 20030045511Abstract: This invention relates to cyclic combination therapies and regimens utilizing substituted indoline derivative compounds which are antagonists of the progesterone receptor having the general structure: 1Type: ApplicationFiled: May 9, 2002Publication date: March 6, 2003Applicant: WYETHInventors: Gary S. Grubb, Puwen Zhang, Eugene A. Terefenko, Andrew Fensome, Jay E. Wrobel, Horace Fletcher, James P. Edwards, Todd K. Jones, Christopher M. Tegley, Lin Zhi
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Patent number: 6503939Abstract: This invention relates to cyclic combination therapies and regimens utilizing substituted indoline derivative compounds that are antagonists of the progesterone receptor having the structure: wherein: R1 and R2 are (i) H, OH, OAc, alkylaryl, alkylheteroaryl, 1-propynyl, 3-propynyl, and optionally substituted alkyl, O(alkyl), aryl, or heteroaryl; (ii) a ring or (iii) a double bond; R3 is H, OH, NH2, CORA; or optionally substituted alkenyl or alkynyl; RA=H or optionally substituted alkyl, alkoxy, or aminoalkyl groups; R4=H, halo, CN, NH2, or optionally substituted alkyl, alkoxy, or aminoalkyl; R5 is a benzene ring; heterocyclic ring; an indole or benzothiophene; or pharmaceutically acceptable salt. R6 and R7 are H, methyl, ethyl, propyl, butyl, iso-propyl, isobutyl, cyclohexyl, aryl, substituted aryl, heteroaryl, or substituted heteroaryl.Type: GrantFiled: October 15, 2001Date of Patent: January 7, 2003Assignees: Wyeth, Ligand Pharmaceuticals, Inc.Inventors: Gary S. Grubb, John W. Ullrich, Andrew Fensome, Jay E. Wrobel, James P. Edwards, Todd K. Jones, Christopher M. Tegley, Lin Zhi
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Patent number: 6498154Abstract: This invention relates to cyclic combination therapies utilizing, in combination with progestins, estrogens, or both, compounds which are progesterone receptor antagonists of the general structure: wherein: R1 and R2 are H, CORA, or NRBCORA, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, or heterocyclic; or R1 and R2 fuse to form 3 to 8 membered spirocyclic alkyl, alkenyl or heterocyclic rings; RA is H or optionally substituted alkyl, aryl, alkoxy, or aminoalkyl groups; RB is H or alkyl; R3 is H, OH, NH2, CORC or alkyl, alkenyl, or alkynyl; RC is H, alkyl, aryl, alkoxy, or aminoalkyl; R4 is H, halogen, CN, NO2, alkyl, alkynyl, alkoxy, amino or aminoalkyl; R5 is benzene or 5- or 6-membered heterocyclic ring; R6 is H or alkyl; G1 is O, NR7, or CR7R8; G2 is CO or CR7R8; provided that when G1 is O, G2 is CR7R8, and G1 and G2 cannot both be CR7R8; R7 and R8 are H or an optionally substituted alkyl, aryl, or heterocyclic moiety; or pharmaceutically acceptable salt thereof.Type: GrantFiled: April 19, 2000Date of Patent: December 24, 2002Assignees: Wyeth, Ligand Pharmaceuticals, Inc.Inventors: Gary S. Grubb, Lin Zhi, Todd K. Jones, Puwen Zhang, James P. Edwards, Andrew Fensome, Eugene A. Terefenko, Jay E. Wrobel, Christopher M. Tegley
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Publication number: 20020151531Abstract: This invention relates to cyclic combination therapies and regimens utilizing indoline compounds which are antagonists of the progesterone receptor and having the general structure: 1Type: ApplicationFiled: March 1, 2002Publication date: October 17, 2002Inventors: Gary S. Grubb, Puwen Zhang, Reinhold R.W. Bender, Jay E. Wrobel, James P. Edwards, Todd K. Jones, Christopher M. Tegley, Lin Zhi
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Patent number: 6462032Abstract: This invention relates to cyclic combination therapies and regimens utilizing substituted indoline derivative compounds which are antagonists of the progesterone receptor having the general structure: wherein R1 and R2 may be single substituents or fused to form spirocyclic rings, in combination with progestins, estrogens, or both. These methods of treatment may be used for contraception or for the treatment and/or prevention of secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis; polycystic ovary syndrome, carcinomas and adenocarcinomas of the endometrium, ovary, breast, colon, prostate, or minimization of side effects or cyclic menstrual bleeding. Additional uses of the invention include stimulation of food intake.Type: GrantFiled: April 19, 2000Date of Patent: October 8, 2002Assignees: Wyeth, Ligand Pharmaceuticals, Inc.Inventors: Gary S. Grubb, Andrew Fensome, Lori L. Miller, John W. Ullrich, Reinhold H. W. Bender, Puwen Zhang, Jay E. Wrobel, James P. Edwards, Todd K. Jones, Christopher M. Tegley, Lin Zhi