Patents by Inventor Jay E. Wrobel
Jay E. Wrobel 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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Patent number: 7253203Abstract: This invention relates to substituted indoline derivative compounds which are antagonists of the progesterone receptor, their preparation and pharmaceutical utility, particularly including contraception and treatment of benign or malignant neoplastic diseases, having the general structure: wherein R1 and R2 may be single substituents or fused to form spirocyclic rings.Type: GrantFiled: March 17, 2006Date of Patent: August 7, 2007Assignee: WyethInventors: Andrew Fensome, Lori L. Miller, John W. Ullrich, Reinhold H. W. Bender, Puwen Zhang, Jay E. Wrobel, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
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Patent number: 7091234Abstract: This invention relates to compounds which are agonists of the progesterone receptor which have the general structure: wherein: R1, R2, R3, R4, R5 and Q1 are as defined herein, or a pharmaceutically acceptable salt thereof, as well as methods of using these compounds to induce contraception or treat progesterone-related carcinomas and adenocarcinomas.Type: GrantFiled: October 20, 2004Date of Patent: August 15, 2006Assignee: WyethInventors: Andrew Fensome, Puwen Zhang, Marci C. Koko, Lin Zhi, Todd K. Jones, Jay E. Wrobel, Christopher M. Tegley, James P. Edwards, Edward G. Melenski
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Patent number: 7084168Abstract: This invention relates to substituted indoline derivative compounds which are antagonists of the progesterone receptor, their preparation and pharmaceutical utility, particularly including contraception and treatment of benign or malignant neoplastic diseases, having the general structure: wherein R1 and R2 may be single substituents or fused to form spirocyclic rings.Type: GrantFiled: June 6, 2003Date of Patent: August 1, 2006Assignee: WyethInventors: Andrew Fensome, Lori L. Miller, John W. Ullrich, Reinhold H.W. Bender, Puwen Zhang, Jay E. Wrobel, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
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Patent number: 7081457Abstract: Methods of using compounds which are progesterone receptor agonists for contraception and the treatment of progesterone-related maladies alone or in combination with an estrogen receptor agonist or progesterone receptor antagonist are provided. These compounds have the structure: wherein R1 and R2 are selected from the group of H, optionally substituted C1 to C6 alkyl, alkenyl, alkynyl, or alkynyl groups C3 to C8 cycloalkyl, aryl, substituted aryl, or heterocyclic groups, or CORA or NRBCORA; or R1 and R2 are fused to form an optionally substituted ring structure as defined herein; RA and RB are as defined herein; R3 is H, OH, NH2, CORC, or optionally substituted C1 to C6 alkyl, C3 to C6 alkenyl, or alkynyl groups; RC is as defined herein; Q1 is S, NR7, or CR8R9; R5 is an optionally trisubstituted benzene ring or an optionally substituted five or six membered heterocyclic ring.Type: GrantFiled: May 6, 2002Date of Patent: July 25, 2006Assignees: Wyeth, Ligand Pharmaceuticals, Inc.Inventors: Puwen Zhang, Andrew Fensome, Eugene A. Terefenko, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley, Jay E. Wrobel, Mark A. Collins
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Patent number: 6982261Abstract: This invention provides a progesterone receptor antagonist of formula 1 having the structure wherein T is O, S, or absent; R1, and R2 are each, independently, hydrogen, alkyl, substituted alkyl; or R1 and R2 are taken together form a ring and together contain —CH2(CH2)nCH2—, —CH2CH2CMe2CH2CH2—, —O(CH2)pCH2—, —O(CH2)qO—, —CH2CH2OCH2CH2—, or —CH2CH2NR7CH2CH2—; n=1–5; p=1–4; q=1–4; R3 is hydrogen, OH, NH2, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, or CORA; RA is hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R4 is hydrogen, halogen, CN, NH2, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R5 is hydrogen, alkyl, or substituted alkyl; R6 is hydrogen, alkyl, substituted alkyl, or CORB; RB is hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R7 is hydrogen or alkyl, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: January 15, 2003Date of Patent: January 3, 2006Assignees: Wyeth, Ligand Pharmaceuticals, Inc.Inventors: Mark A. Collins, Valerie A. Mackner, Jay E. Wrobel, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
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Patent number: 6946454Abstract: This invention relates to methods of co-administering compounds of formula 1 which are agonists of the progesterone receptor which have the general structure: wherein: R1, R2, R3, R4, R5 and Q1 are as defined herein, or a pharmaceutically acceptable salt thereof, with estrogen, an estrogen, or an estrogen receptor agonist for contraception, hormone replacement therapy, or treating progesterone-related carcinomas and adenocarcinomas.Type: GrantFiled: April 5, 2002Date of Patent: September 20, 2005Assignees: Wyeth, Ligand Pharmaceuticals, Inc.Inventors: Andrew Fensome, Puwen Zhang, Marci C. Koko, Lin Zhi, Todd K. Jones, Jay E. Wrobel, Christopher M. Tegley, James P. Edwards, Edward G. Melenski
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Patent number: 6844358Abstract: This invention provides compounds of Formula I having the structure wherein: A is O, S, or N; B is —(CH2)m—, —CH(OH)—, or carbonyl; R1 is hydrogen, halogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, or trifluoromethyl; R2 is alkyl of 1-18 carbon atoms, aryl of 6-10 carbon atoms, arylalkyl of 7-15 carbon atoms, Het-alkyl wherein the alkyl moiety is 1-6 carbon atoms; Het is R2a is alkylene of 1-3 carbon atoms; G is oxygen, sulfur, or nitrogen; R3, R4 are each, independently, hydrogen, halogen, alkyl of 1-3 carbon atoms, aryl of 6-10 carbon atoms or a heterocyclic ring of 5 to 7 ring atom containing 1 to 3 heteroatoms selected from oxygen, nitrogen, sulfur; R5 is hydrogen, alkyl of 1-6 carbon atoms, —CH(R7)R8, —C(CH2)nCO2R9, —C(CH3)2CO2R9, —CH(R7)(CH2)nCO2R9, or CH(R7)C6H4CO2R9; R6 is hydrogen, halogen, alkyl of 1-6 carbon atoms, or —OR5; m=1-6; n=1-6; R7 is hydrogen, alkyl of 1-6 carbon atoms, aryl of 6-10 carbon atoms, or arylalkyl of 7-15 carbon atoms; R8 is —CO2R10, —CONHR10, tetrazolType: GrantFiled: November 21, 2002Date of Patent: January 18, 2005Assignee: WyethInventors: Michael S. Malamas, Jay E. Wrobel, Arlene J. Dietrich, Zenan Li, Iwan Gunawan
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Patent number: 6841568Abstract: This invention relates to compounds which are agonists of the progesterone receptor which have the general structure: wherein: R1, R2, R3, R4, R5 and Q1 are as defined herein, or a pharmaceutically acceptable salt thereof, as well as methods of using these compounds to induce contraception or treat progesterone-related carcinomas and adenocarcinomas.Type: GrantFiled: April 22, 2003Date of Patent: January 11, 2005Assignees: Wyeth, Ligand Pharmaceuticals, Inc.Inventors: Andrew Fensome, Puwen Zhang, Marci C. Koko, Jay E. Wrobel, Edward G. Melenski, Lin Zhi, Todd K. Jones, Christopher M. Tegley, James P. Edwards
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Patent number: 6835744Abstract: This invention provides compounds of the formula I: wherein: R1 and R2 are independently H, OH, OAc, alkylaryl, alkylheteroaryl, 1-propynyl, 3-propynyl, and substituted alkyl, O(alkyl), aryl, or heteroaryl; or R1 and R2 are joined to form a ring comprising —CH2(CH2)nCH2— where n=0-5; —CH2CH2C(CH3)2CH2CH2—; —O(CH2)mCH2— where m=1-4; O(CH2)pO— where p=1-4; —CH2CH2OCH2CH2—; —CH2CH2N(H or alkyl)CH2CH2—; or R1 and R2 together comprise a double bond to C(CH3)2, C(cycloalkyl), O, or C(cycloether); R3 is H, OH, NH2, CORA, or optionally substituted alkenyl or alkynyl groups; RA=H or optionally substituted alkyl, alkoxy, or aminoalkyl groups; R4=H, halo, CN, NH2, or optionally substituted alkyl, alkoxy, or aminoalkyl; R5 is optionally substituted benzene ring; five or six membered heterocyclic ring; 4 or 7-substituted indole or a substituted benzothiophene; or pharmaceutically acceptable salt tType: GrantFiled: April 24, 2002Date of Patent: December 28, 2004Assignees: Wyeth, Ligand Pharmaceuticals, Inc.Inventors: John W. Ullrich, Andrew Fensome, Jay E. Wrobel, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
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Publication number: 20040186101Abstract: This invention provides compounds of Formula (I): 1Type: ApplicationFiled: January 29, 2004Publication date: September 23, 2004Applicants: Wyeth, Ligand Pharmaceuticals, Inc.Inventors: Puwen Zhang, Eugene A. Terefenko, Andrew Fensome, Jay E. Wrobel, Horace Fletcher, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
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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: 20040102480Abstract: This invention provides compounds of Formula I having the structure 1Type: ApplicationFiled: November 21, 2002Publication date: May 27, 2004Applicant: WyethInventors: Michael S. Malamas, Jay E. Wrobel, Arlene J. Dietrich, Zenan Li, Iwan Gunawan
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Patent number: 6713478Abstract: This invention provides compounds of Formula (I): wherein R1 and R2 are independent substituents or are fused to form spirocyclic rings; R3, RC, and R4 are as defined herein; and R5 is a substituted benzene ring or a substituted five or six membered heterocyclic ring having in its backbone 1, 2, or 3 heteroatoms including O, S, SO, SO2 or NR6; or pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions and methods using the compounds as antagonists of the progesterone receptor.Type: GrantFiled: March 12, 2003Date of Patent: March 30, 2004Assignees: Wyeth, Ligand Pharmaceuticals, Inc.Inventors: Puwen Zhang, Eugene A. Terefenko, Andrew Fensome, Jay E. Wrobel, Horace Fletcher, III, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
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Patent number: 6693103Abstract: This invention provides compounds which are agonists and antagonists of the progesterone receptor having the general structure: wherein: R1 and R2 are independently selected from H, CORA, or NRBCORA, or optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, or heterocyclic moieties; or R1 and R2 are fused 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, C1 to C3 alkyl, or substituted C1 to C3 alkyl; R3 is H, OH, NH2, CORC or optionally substituted alkyl, alkenyl, or alkynyl; RC is H or optionally substituted alkyl, aryl, alkoxy, or aminoalkyl; R4 is H, halogen, CN, NO2, or optionally substituted alkyl alkynyl, alkoxy, amino or aminoalkyl; R5 is an optionally substituted benzene or five or six membered ring with 1, 2, or 3 heteroatoms selected from O, S, SO, SO2 or NR6; R6 is H or C1 to C3 alkyl; G1 is O, NR7, or CR7R8; G2 is CO, CS, or CR7R8; provided that when G1 is OType: GrantFiled: December 17, 2001Date of Patent: February 17, 2004Assignees: Wyeth, Ligand Pharmaceuticals Inc.Inventors: Puwen Zhang, Andrew Fensome, Eugene A. Terefenko, Jay E. Wrobel, James P. Edwards, Todd K. Jones, Christopher M. Tegley, Lin Zhi
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Publication number: 20030225109Abstract: This invention relates to compounds which are agonists of the progesterone receptor which have the general structure: 1Type: ApplicationFiled: April 22, 2003Publication date: December 4, 2003Applicants: Wyeth, Ligand Pharmaceuticals, Inc.Inventors: Andrew Fensome, Puwen Zhang, Marci C. Koko, Jay E. Wrobel, Edward G. Melenski, Lin Zhi, Todd K. Jones, Christopher M. Tegley, James P. Edwards
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Publication number: 20030220388Abstract: This invention relates to substituted indoline derivative compounds which are antagonists of the progesterone receptor, their preparation and pharmaceutical utility, particularly including contraception and treatment of benign or malignant neoplastic diseases, having the general structure: 1Type: ApplicationFiled: June 6, 2003Publication date: November 27, 2003Applicants: Wyeth, Ligand Pharmaceuticals, Inc.Inventors: Andrew Fensome, Lori L. Miller, John W. Ullrich, Reinhold H.W. Bender, Puwen Zhang, Jay E. Wrobel, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
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Publication number: 20030216388Abstract: This invention provides compounds of Formula (I): 1Type: ApplicationFiled: March 12, 2003Publication date: November 20, 2003Applicants: Wyeth, Ligand Pharmaceuticals, Inc.Inventors: Puwen Zhang, Eugene A. Terefenko, Andrew Fensome, Jay E. Wrobel, Horace Fletcher, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
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Publication number: 20030158182Abstract: This invention provides a progesterone receptor antagonist of formula 1 having the structure 1Type: ApplicationFiled: January 15, 2003Publication date: August 21, 2003Applicant: WyethInventors: Mark A. Collins, Valerie A. Mackner, Jay E. Wrobel, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
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Patent number: 6608068Abstract: This invention relates to substituted indoline derivative compounds which are antagonists of the progesterone receptor, their preparation and pharmaceutical utility, particularly including contraception and treatment of benign or malignant neoplastic diseases, having the general structure: wherein R1 and R2 may be single substituents or fused to form spirocyclic rings.Type: GrantFiled: December 11, 2001Date of Patent: August 19, 2003Assignees: Wyeth, Ligand PharmaceuticalsInventors: Andrew Fensome, Lori L. Miller, John W. Ullrich, Reinhold H. W. Bender, Puwen Zhang, Jay E. Wrobel, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley