Patents Represented by Attorney Richard S. Parr
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Patent number: 8338449Abstract: The present invention relates to compounds having the structure useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.Type: GrantFiled: April 2, 2010Date of Patent: December 25, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: B. Wesley Trotter, Christopher Claiborne, Gerald S. Ponticello, Charles J. McIntyre, Nigel Liverton, David A. Claremon
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Patent number: 8299091Abstract: The invention relates to the compound N-(2-oxo-2-propoxyethyl)-?-phenyl-D-phenyl-alanyl-N-[(1-amino-6-iso-quinolinyl)methyl]-L-prolinamide or a pharmaceutically acceptable salt thereof, to a pharmaceutical composition comprising said compound, as well as to the use of the compound for the manufacture of a medicament for treating or for preventing thrombin mediated diseases.Type: GrantFiled: August 6, 2007Date of Patent: October 30, 2012Assignee: MSD Oss B.V.Inventors: Robert Gilfillan, David Jonathan Bennett
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Patent number: 8293777Abstract: A compound having the structure wherein R is an angiotensin receptor antagonist active group, and Y is Y is selected from the group consisting of R1 is selected from the group consisting of —O—C1-6 alkyl, —O-aryl, —O-heteroaryl, —O—C3-8 cycloalkyl, —C1-6 alkyl, -aryl, -heteroaryl, and —C3-8 cycloalkyl; R2 and R3 are independently selected from the group consisting of hydrogen and C1-4 alkyl, or a pharmaceutically acceptable salt or hydrate thereof, which is useful for treating hypertension.Type: GrantFiled: December 2, 2009Date of Patent: October 23, 2012Assignee: Merck Sharp & Dohme, Corp.Inventors: Michael Man-Chu Lo, Amjad Ali, Ravi P. Nargund
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Patent number: 8278317Abstract: The present invention relates to compounds having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.Type: GrantFiled: July 18, 2006Date of Patent: October 2, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: B. Wesley Trotter, Kausik K. Nanda, Scott E. Wolkenberg, M. Brad Nolt, David Wisnoski
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Patent number: 8207208Abstract: A compound having the structure R—Y wherein R is, for example, Y is selected from the group consisting of 1) R5, 2) —C(R1R2)(C(R3R4))0-1Y1R5, and 3) —C(R1R2)—O—Y1R5; R1, R2, R3 and R4 are independently selected from the group consisting of hydrogen and C1-4 alkyl; R5 is Y1 is selected from the group consisting of —C(O)—O— and —P(O)(OR6)—O—; and R6 is hydrogen or CH3, or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.Type: GrantFiled: May 6, 2009Date of Patent: June 26, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Amjad Ali, Michael Man-chu Lo, Iyassu K. Sebhat, Chris Franklin, Nicoletta Almirante, Silvia Stefanini, Stefano Biondi, Ennio Ongini
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Patent number: 8183228Abstract: The present invention relates compounds of the formula: oligosaccharide-spacer-(GpIIb/IIIa antagonist), wherein the oligosaccharide is a negatively charged oligosaccharide residue comprising four to twenty five monosaccharide units, the charge being compensated by positively charged counterions, and wherein the oligosaccharide residue is derived from an oligosaccharide which has (AT-III mediated) anti-Xa activity per se; the spacer is a bond or an essentially pharmacologically inactive linking residue; the GpIIb/IIIa antagonist is a residue mimicking the RGD and/or K(QA)GD fragment of fibrinogen, comprising a carboxylate moiety and a basic moiety located within the residue at a distance of 10-20 ? from each other; or a pharmaceutically acceptable salt thereof or a prodrug or a solvate thereof; wherein the compound of formula I further comprises at least one covalent bond with a biotin label or an analogue thereof.Type: GrantFiled: October 6, 2006Date of Patent: May 22, 2012Assignee: MSD OSS B.V. NetherlandsInventors: Martin De Kort, Constant Adriaan Anton Van Boeckel, Charles David Nicholson
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Patent number: 8178546Abstract: 2,5-Diaryl-1,2,4-triazole derivatives of structural formula I are selective inhibitors of the 11?-hydroxysteroid dehydrogenase Type 1 enzyme (11?-HSD-1). The compounds are useful for the treatment of diabetes, hyperglycemia, obesity, insulin resistance, atherosclerosis, dyslipidemia, hyperlipidemia, hypertension, and Metabolic Syndrome. Also disclosed are novel compounds of structural formula II which are inhibitors of 11?-HSD-1.Type: GrantFiled: April 14, 2010Date of Patent: May 15, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Susan D. Aster, James M. Balkovec, Donald W. Graham, Xin Gu, Nancy J. Kevin, Gool F. Patel, Mitree Ponpipom
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Patent number: 8168595Abstract: The present invention relates to compounds of the formula (I) oligosaccharide-spacer-A (1), wherein the oligosaccharide is a negatively charged oligosaccharide residue comprising two to twenty five monosaccharide units, the charge being compensated by positively charged counterions, and wherein the oligosaccharide residue is derived from an oligosaccharide which has (AT-III mediated) anti-Xa activity per se; the spacer is an essentially pharmacologically inactive flexible linking residue having a chain length of 10 to 70 atoms; A is the residue —CH[NH—SO2—R1[CO—NR2—CH(4-benzamidine)-CO—NR3R4], wherein R1 is phenyl, naphthyl, 1,2,3,4-tetrahydronaphthyl, (iso)quinolinyl, tetrahydro(iso)quinolinyl, 3,4-dihydro-1H-isoquinolinyl, chromanyl or the camphor group, which groups may optionally be substituted with one or more substituents selected from (1-8C)alkyl or (1-8C)alkoxy; and wherein R2 and R3 are independently H or (1-8C)alkyl; R4 is (-8C)alkyl or (3-8C)cycloalkyl; or R3 and R4 together with the nitrogen atomType: GrantFiled: December 21, 2005Date of Patent: May 1, 2012Assignee: Msd Oss B.VInventors: Martin De Kort, Constant Adriaan Anton Van Boeckel
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Patent number: 8148363Abstract: The present invention relates to novel heterocyclic compounds of Formulae I-III; as disclosed herein or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosed are pharmaceutical compositions comprising said compounds, and methods for using said compounds for treating or preventing a thromboembolic disorder.Type: GrantFiled: May 18, 2009Date of Patent: April 3, 2012Assignee: Schering CorporationInventors: Martin C. Clasby, William J. Greenlee, Yan Xia, Tin-Yau Chan, Mariappan V. Chelliah, Samuel Chackalamannil, Haiyan Pu, Keith A. Eagen, Henry Vaccaro, Brian A. McKittrick, Liyuan Wang, Xiaobang Gao
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Patent number: 8148535Abstract: The present invention relates to compounds having the structure useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.Type: GrantFiled: October 17, 2006Date of Patent: April 3, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: B. Wesley Trotter, Kausik K. Nanda, Scott Wolkenberg, M. Brad Nolt, Peter Manley, Nathan R. Kett, Mark T. Bilodeau
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Patent number: 8119806Abstract: A compound having the structure wherein X is selected from the group consisting of: a bond, —NHCH2(CH2)nCH2OC(O)—, —CH2NHC(O)CH2NHC(O)—, —CH2OC(O)—, —OCH(CH3)OC(O)—, —OCH2OC(O)—, —O—, —NR1—, —CR1R3—, —(CH2)p—, —(CH2)qNR1C(O)—, —CHR5NR2C(O)—, —(CH2)qC(O)—, —(CH2)qC(O)NR1—, or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.Type: GrantFiled: July 27, 2009Date of Patent: February 21, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Amjad Ali, Iyassu K. Sebhat, Christopher L. Franklin, Kathleen M. Rupprecht, Robert K. Baker, Ravi P. Nargund, Lin Yan, Pei Huo, Dong-Ming Shen, Nicoletta Almirante, Stefano Biondi, Massimiliano Ferrario, Alessia Nicotra
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Patent number: 8106034Abstract: A compound having the structure wherein R is an angiotensin receptor blocking group Y is —(CR1R20)1-7R5, or —C(O)(CR1R20)1-7R5; R1 and R20 are independently selected from the group consisting of hydrogen or C1-4 alkyl; R5 is —O—N?N(O)—NR3R4; and R3 and R4 are independently selected from the group consisting of —CH2CH2OH, —CH2CH2OCH3, —C1-4 alkyl, unsubstituted or substituted C1-6 alkenyl, unsubstituted or substituted morpholino, amino, unsubstituted or substituted benzyl, unsubstituted or substituted phenyl, unsubstituted or substituted arylC1-4 alkyl, or R3 and R4 together with the nitrogen atom to which they are attached, form a ring selected from the group consisting of or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable salt of the stereoisomer thereof, which is useful for treating hypertension.Type: GrantFiled: January 29, 2009Date of Patent: January 31, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Amjad Ali, Michael Man-Chu Lo
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Patent number: 7973059Abstract: The present invention relates to compounds having the structure useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.Type: GrantFiled: October 17, 2006Date of Patent: July 5, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Scott Wolkenberg, Mark T. Bilodeau, M. Brad Nolt
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Patent number: 7579331Abstract: Disclosed is a pharmaceutical composition comprising a therapeutically effective amount of KW-3902, or a salt, ester, amide, metabolite, or prodrug thereof, and a non-adenosine modifying diuretic. Also disclosed are methods of inducing a diuretic effect in an animal comprising the step of administering a therapeutically effective amount of KW-3902, or a salt, ester, amide, metabolite, or prodrug thereof, in combination with second pharmaceutical composition capable of inducing a diuretic effect.Type: GrantFiled: April 23, 2004Date of Patent: August 25, 2009Assignee: Novacardia, Inc.Inventors: Kenneth J. Widder, Lauren Otsuki, Howard C. Dittrich, Scott Thomson, Roland Blantz
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Patent number: 7569589Abstract: The present invention relates to compounds having the structure useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.Type: GrantFiled: July 25, 2005Date of Patent: August 4, 2009Assignee: Merck & Co., Inc.Inventors: Mark T. Bilodeau, Christopher J. Dinsmore, Jeffrey M. Bergman, B. Wesley Trotter, Lou Anne Neilson, Zhicai Wu, Peter Manley, John Hartnett
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Patent number: 7214768Abstract: This invention relates to an improved process for the minimization of acid-catalyzed reactions of certain echinocandins of the kind disclosed in U.S. Pat. No. 5,378,804. The process involves the use of a boronic acid.Type: GrantFiled: April 8, 2002Date of Patent: May 8, 2007Assignee: Merck & Co., Inc.Inventors: Kevin M. Belyk, William R. Leonard
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Patent number: 7176008Abstract: The invention is a process for purifying TAFIa from a serum sample in the presence of a reversible inhibitor of TAFIa. The invention is also a method of measuring the activity of TAFIa in the presence of a reversible inhibitor.Type: GrantFiled: December 16, 2003Date of Patent: February 13, 2007Assignee: Merck & Co., Inc.Inventors: Shi-Shan Mao, Dennis Colussi, Steve Gardell
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Patent number: 7144899Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure Formula (I): wherein u is CH or N; Q is 1)—N(R25)CH(R30)— wherein the nitrogen atom is attached to R1, and R25 and R30 are independently selected from the group consisting of hydrogen, C3-6cycloalkyl, and C1-6alkyl, or 2) wherein the nitrogen atom is attached to R1, and m is 0, 1, or 2Type: GrantFiled: February 5, 2002Date of Patent: December 5, 2006Assignee: Merck & Co., Inc.Inventors: Harold G. Selnick, Mary Beth Young, Philippe G. Nantermet, James C. Barrow, Peter D. Williams, Terry A. Lyle, Donnette D. Staas, Kenneth J. Stauffer, Philip E. Sanderson
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Patent number: 7109004Abstract: A process for preparing (R)-hydroxy ester (II) from alpha-keto ester I comprising adding the alpha-keto ester I to a mixture comprising the ketoreductase enzyme and non-ketoreductase enzyme components, wherein the ketoreductase enzyme has a molecular weight between 36000 and 38000, and wherein the ketoreductase enzyme has an N-terminal amino acid sequence selected from the group of sequences consisting of (SEQ. ID NO. 1) Ala-Ile-Pro-Asp-Asn-Ala-Val-Leu-Glu-Gly-Ser-Leu- Val-Lys-Val-Thr-Gly-Ala-Asn-Gly (SEQ. ID NO. 4) Met-Ala-Ile-Pro-Asp-Asn-Ala-Val-Leu-Glu-Gly-Ser- Leu-Val-Lys-Val-Thr-Gly-Ala-Asn-Gly, and (SEQ. ID NO. 2) Met-Ala-Lys-Ile-Asp-Asn-Ala-Val-Leu-Pro-Glu-Gly- Ser-Leu-Val-Leu-Val-Thr-Gly-Ala-Asn-Gly.Type: GrantFiled: July 8, 2003Date of Patent: September 19, 2006Assignee: Merck & Co., Inc.Inventors: Jeffrey C. Moore, Michael G. Sturr, Kathleen McLaughlin, Jaehon Kim
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Patent number: 7084134Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof.Type: GrantFiled: May 1, 2003Date of Patent: August 1, 2006Assignee: Merk & Co., Inc.Inventors: James C. Barrow, Philippe G. Nantermet, Harold G. Selnick