Patents by Inventor Philip M. Weintraub
Philip M. Weintraub 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: 20120202795Abstract: The present invention relates to a series of 2,3,5-substituted pyridone derivatives of formula I: wherein R, R1, R2, R3 and R4 are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are inhibitors of poly(adenosine 5?-diphosphate ribose) polymerase (PARP) and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases, including diseases associated with the central nervous system and cardiovascular disorders.Type: ApplicationFiled: April 18, 2012Publication date: August 9, 2012Applicant: AVENTIS PHARMACEUTICALS INC.Inventors: Philip M. WEINTRAUB, Paul R. EASTWOOD, Shujaath MEHDI, David W. STEFANY, Kwon Yon MUSICK, Neil MOORCROFT, Sungtaek LIM, John Z. JIANG, Hartmut RUTTEN, Stefan PEUKERT, Uwe SCHWAHN
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Patent number: 8173682Abstract: The present invention relates to a series of 2,3,5-substituted pyridone derivatives of formula I: wherein R, R1, R2, R3 and R4 are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are inhibitors of poly(adenosine 5?-diphosphate ribose) polymerase (PARP) and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases, including diseases associated with the central nervous system and cardiovascular disorders.Type: GrantFiled: September 26, 2006Date of Patent: May 8, 2012Assignee: Aventis Pharmaceuticals Inc.Inventors: Philip M. Weintraub, Paul R. Eastwood, Shujaath Mehdi, David W. Stefany, Kwon Yon Musick, Neil Moorcroft, Sungtaek Lim, John Z. Jiang, Hartmut Rutten, Stefan Peukert, Uwe Schwahn
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Patent number: 7169925Abstract: This invention discloses and claims a new class of indole derivatives for use in treating allergy, asthma, rhinitis, dermatitis, B-cell lymphomas, tumors and diseases associated with bacterial, rhinovirus or respiratory syncytial virus (RSV) infections. It has now been found that the compounds of this invention are capable of modulating T helper (Th) cells, Th1/Th2, and thereby capable of inhibiting the transcription of interleukin-4 (IL-4) message, IL-4 release or IL-4 production.Type: GrantFiled: April 23, 2003Date of Patent: January 30, 2007Assignee: Aventis Pharmaceuticals Inc.Inventors: Gregory H. Merriman, Philip M. Weintraub, Jeffrey S. Sabol, Ramalinga M. Dharanipragada, Nicholas J. Hrib, John G. Jurcak, Alexandre Gross, Brian Whiteley, Kwon Yon Musick, Joseph T. Klein
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Publication number: 20040010029Abstract: This invention discloses and claims a new class of indole derivatives for use in treating allergy, asthma, rhinitis, dermatitis, B-cell lymphomas, tumors and diseases associated with bacterial, rhinovirus or respiratory syncytial virus (RSV) infections. It has now been found that the compounds of this invention are capable of modulating T helper (Th) cells, Th1/Th2, and thereby capable of inhibiting the transcription of interleukin-4 (IL-4) message, IL-4 release or IL-4 production.Type: ApplicationFiled: April 23, 2003Publication date: January 15, 2004Inventors: Gregory H. Merriman, Philip M. Weintraub, Jeffrey S. Sabol, Ramalinga M. Dharanipragada, Nicholas J. Hrib, John G. Jurcak, Alexandre Gross, Brian Whiteley, Kwon Yon Musick, Joseph T. Klein
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Patent number: 6413951Abstract: 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: GrantFiled: June 21, 2001Date of Patent: July 2, 2002Assignee: Aventis Pharmaceuticals, Inc.Inventors: Norton P. Peet, Philip M. Weintraub, Joseph P. Burkhart, Cynthia A. Gates
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Patent number: 6365597Abstract: 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: GrantFiled: February 11, 1997Date of Patent: April 2, 2002Assignee: Aventis Pharmaceuticals Inc.Inventors: James R. Pribish, Cynthia A. Gates, Philip M. Weintraub
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Publication number: 20020019548Abstract: 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: ApplicationFiled: June 21, 2001Publication date: February 14, 2002Inventors: Norton P. Peet, Philip M. Weintraub, Joseph P. Burkhart, Cynthia A. Gates
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Patent number: 5990328Abstract: 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: GrantFiled: February 24, 1999Date of Patent: November 23, 1999Assignee: Merrell Pharmaceuticals Inc.Inventors: Philip M. Weintraub, Michael R. Angelastro, Cynthia A. Gates, Gary Alan Flynn, Timothy Thomas Curran, Chi-Hsin Richard King
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Patent number: 5965550Abstract: 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: GrantFiled: January 22, 1998Date of Patent: October 12, 1999Assignee: Merrell Pharmaceuticals Inc.Inventors: Philip M. Weintraub, Michael R. Angelastro, Cynthia A. Gates, Timothy Thomas Curran, Gary Alan Flynn, Chi-Hsin Richard King
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Patent number: 5869475Abstract: 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: GrantFiled: November 14, 1997Date of Patent: February 9, 1999Assignee: Merrell Pharmaceuticals, Inc.Inventors: Timothy Thomas Curran, Chi-Hsin Richard King, Gary Alan Flynn, Philip M. Weintraub, Michael R. Angelastro, Cynthia A. Gates
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Patent number: 5750744Abstract: 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: GrantFiled: February 11, 1997Date of Patent: May 12, 1998Assignee: Merrell Pharmaceuticals Inc.Inventors: Philip M. Weintraub, Cynthia A. Gates, Michael R. Angelastro, Gary Alan Flynn, Chi-Hsin Richard King, Timothy Thomas Curran
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Patent number: 5486511Abstract: 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: GrantFiled: May 2, 1994Date of Patent: January 23, 1996Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Philip M. Weintraub, Cynthia A. Gates, Michael R. Angelastro, Timothy T. Curran, J. O'Neal Johnston
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Patent number: 5436237Abstract: The present invention relates to 4-amino-.DELTA..sup.4 -steroids which are useful as inhibitors of 5.alpha.-reductase. The compounds are prepared by the reaction of an appropriate 4-azido steroid with triphenylphosphine in an aqueous inert solvent with heating.Type: GrantFiled: February 25, 1994Date of Patent: July 25, 1995Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Philip M. Weintraub, Joseph P. Burkhart, Thomas R. Blohm
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Patent number: 5426101Abstract: The compound (R)-2-[(phenylisopropyl)amino]adenosine whose structure is given below: ##STR1## (R)-2-[(phenylisopropyl)amino]adenosine is about two orders of magnitude greater in its selectivity between the A-1 and A-2 adenosine receptors than its diastereoisomer. This compound is useful for lowering blood pressure.Type: GrantFiled: September 15, 1994Date of Patent: June 20, 1995Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Norton P. Peet, David R. Borcherding, Nelsen L. Lentz, Philip M. Weintraub, Philip R. Kastner
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Patent number: 5318961Abstract: The present invention relates to 4-amino-.DELTA..sup.4 -steroids which are inhibitors of 5.alpha.-reductase. The compounds are useful for treating DHT-mediated diseases.Type: GrantFiled: December 20, 1992Date of Patent: June 7, 1994Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Philip M. Weintraub, Joseph P. Burkhart, Thomas R. Blohm
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Patent number: 5218110Abstract: The present invention relates to 4-azido-.DELTA..sup.4 -steroids which are useful as inhibitors of 5.alpha.-reductase. The compounds are prepared by the reaction of an appropriate 4-azido steroid with triphenylphosphine in an aqueous inert solvent with heating.Type: GrantFiled: March 20, 1992Date of Patent: June 8, 1993Assignee: Merrell Dow PharmaceuticalsInventor: Philip M. Weintraub
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Patent number: 5189032Abstract: The present invention relates to 4-amino-.DELTA..sup.4,6 -steroids which are useful as inhibitors of 5.alpha.-reductase. The compounds are prepared by the reaction of an appropriate 4,5-epoxy steroid with sodium azide in an inert solvent in the presence of a strong acid such as sulfuric acid at about 100.degree. C.Type: GrantFiled: March 20, 1992Date of Patent: February 23, 1993Assignee: Merrell Dow Pharmaceuticals Inc.Inventor: Philip M. Weintraub
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Patent number: 5143909Abstract: 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: GrantFiled: March 19, 1991Date of Patent: September 1, 1992Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Philip M. Weintraub, Cynthia A. Gates, Thomas R. Blohm
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Patent number: 5130424Abstract: The present invention relates to 4-amino-.DELTA..sup.4,6 -steroids which are useful as inhibitors of 5.alpha.-reductase. The compounds are prepared by the reaction of an appropriate 4,5-epoxy steroid with sodium azide in an inert solvent in the presence of a strong acid such as sulfuric acid at about 100.degree. C.Type: GrantFiled: July 2, 1991Date of Patent: July 14, 1992Assignee: Merrell Dow Pharmaceuticals Inc.Inventor: Philip M. Weintraub
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Patent number: 5120840Abstract: The present invention relates to 4-amino-.DELTA..sup.4 -steroids which are useful as inhibitors of 5.alpha.-reductase. The compounds are prepared by the reaction of an appropriate 4-azido steroid with triphenylphosphine in an aqueous inert solvent with heating.The present application is a continuation-in-part of application Ser. No. 561,041, filed Aug. 1, 1990 and application Ser. No. 671,555, filed Mar. 19, 1991.Type: GrantFiled: July 2, 1991Date of Patent: June 9, 1992Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Philip M. Weintraub, Joseph P. Burkhart, Thomas R. Blohm