Patents Represented by Attorney, Agent or Law Firm Mark R. Daniel
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Patent number: 7947664Abstract: A compound having the structure wherein R is an angiotensin receptor antagonist active group, Y is selected from the group consisting of and 2) —C(R1H)OC(O)X((CR12R13)—(CHR10)m—(CH2)n—Zp—(CH2)q—(CHR11)r—(CR16R17))—R5; Z is —O— or —(CR14R15)—; m, n, p, q, and r are independently selected from the group consisting of 0 and 1; X is —O— or —(CR18R19)—; R1 is selected from the group consisting of hydrogen, C1-4 alkyl, aryl and C1-4 alkylaryl; R5 is —O—N?N(O)—NR3R4; or a pharmaceutically acceptable salt or hydrate thereof, which is useful for treating hypertension.Type: GrantFiled: January 8, 2009Date of Patent: May 24, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Amjad Ali, Michael Man-Chu Lo, Christopher Franklin, Brent R. Whitehead
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Patent number: 7935727Abstract: Compounds having a biphenyl group substituted with a phenyl or heteroaromatic group, as shown in Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis:Type: GrantFiled: October 13, 2006Date of Patent: May 3, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Yi-Heng Chen, Zhijian Lu, Peter J. Sinclair
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Patent number: 7915252Abstract: Sulfonyl derivatives of structural formula I are selective inhibitors of the 11?-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome or Syndrome X, and other symptoms associated with NIDDM.Type: GrantFiled: August 3, 2005Date of Patent: March 29, 2011Assignee: Merck Sharp & DohmeInventors: Sherman T. Waddell, James M. Balkovec, Gina M. Santorelli, Aaron H. Leeman, Milana Maletic, Xin Gu
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Patent number: 7915271Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. The compounds have 3 cyclic groups connected by single bonds, as for example triphenyl, which are attached directly to the ring of formula I or attached at the position B.Type: GrantFiled: December 29, 2006Date of Patent: March 29, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Amjad Ali, Zhijian Lu, Peter J. Sinclair, Yi-Heng Chen, Cameron J. Smith, Hong Li
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Patent number: 7910592Abstract: Compounds having the structure of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula (I), B is a cyclic group other than phenyl, and B has a cyclic substituent at a position that is ortho to the position at which B is connected to the remainder of the structure of Formula (I). The 5-membered ring of Formula (I) has a second cyclic substituent in addition to B.Type: GrantFiled: December 29, 2006Date of Patent: March 22, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Amjad Ali, Zhijian Lu, Peter J. Sinclair, Yi-Heng Chen, Cameron J. Smith, Hong Li, Christopher F. Thompson
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Patent number: 7906521Abstract: The present invention relates to compounds useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.Type: GrantFiled: September 17, 2004Date of Patent: March 15, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: B. Wesley Trotter, Richard Isaacs
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Patent number: 7879839Abstract: The present invention relates to compounds having the structure useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.Type: GrantFiled: July 27, 2005Date of Patent: February 1, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Christopher J. Dinsmore, Jeffrey M. Bergman, Douglas C. Beshore, B. Wesley Trotter, Kausik K. Nanda, Richard Isaacs, Linda S. Payne, Lou Anne Neilson, Zhicai Wu, Mark T. Bilodeau, Peter J. Manley, Adrienne E. Balitza
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Patent number: 7863307Abstract: An efficient process is disclosed for producing a compound that is an inhibitor of CETP. The last step of the process is the coupling of an oxazolidinone derivative with a biphenyl moiety to provide a compound of formula (I). In a specific embodiment of this synthesis, a crystalline product is produced which is characterized as a non-solvated crystalline polymorph.Type: GrantFiled: June 29, 2006Date of Patent: January 4, 2011Inventors: Ross A. Miller, Aaron S. Cote
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Patent number: 7786305Abstract: The present invention is directed to compounds of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, n and the dashed line are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2. The present invention is also directed to intermediates useful in the preparation of formula I compounds.Type: GrantFiled: May 28, 2004Date of Patent: August 31, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Richard Jiao, Gregori Morriello, Lihu Yang, Changyou Zhou, Shankaran Kothandaraman, Christopher Moyes
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Patent number: 7781426Abstract: Compounds having the structure of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula (I), B or R2 is a phenyl group which has an ortho amine or aminomethyl substituent which is further substituted, and the other of B or R2 is also a cyclic group.Type: GrantFiled: December 29, 2006Date of Patent: August 24, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Amjad Ali, Zhijian Lu, Peter J. Sinclair, Gayle E. Taylor, Christopher F. Thompson, Cameron J. Smith, Adrian A. Dowst, Yi-Heng Chen
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Patent number: 7737295Abstract: Compounds of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula 1, A1 and A2 are each an aromatic ring, a 5-6-membered heterocyclic ring, an aromatic ring fused to a heterocyclic ring, a phenyl ring fused to a heterocyclic ring, or a cycloalkyl ring.Type: GrantFiled: April 8, 2005Date of Patent: June 15, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Amjad Ali, Joann Bohn, Qiaolin Deng, Zhijian Lu, Peter J. Sinclair, Gayle E. Taylor, Christopher F. Thompson, Nazia Quraishi
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Patent number: 7700591Abstract: Cyclopentyl compounds linked to a benzoxazinyl group through an amido moiety utilizing the ring nitrogen of the benzoxazine, and further substituted with a heterocyclic moiety, such compounds represented by formula I: which are used to modulate the CCR-2 chemokine receptor to prevent or treat inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis; and pharmaceutical compositions comprising these compounds and the use of these compounds and compositions.Type: GrantFiled: May 13, 2005Date of Patent: April 20, 2010Assignee: Merck & Co., Inc.Inventors: Stephen D. Goble, Sander G. Mills, Lihu Yang, Alexander Pasternak, Celine Bonnefous, Theodore M Kamenecka, Jean-Michel Vernier, John H. Hutchinson, Essa Hu, Steven Govek
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Patent number: 7659408Abstract: Pyrazole carboxamides of structural formula I are selective inhibitors of the 11?-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM.Type: GrantFiled: August 3, 2004Date of Patent: February 9, 2010Assignee: Merck Sharp & Dhome Corp.Inventors: Ying-Duo Gao, Xin Gu, Nancy J. Kevin, Sherman T. Waddell
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Patent number: 7652049Abstract: Compounds having the structures of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis: In the compounds of Formula I, B or R2 is a phenyl group which has an ortho aryl, heterocyclic, benzoheterocyclic or benzocycloalkyl substituent, and one other position on the 5-membered ring has an aromatic, heterocyclic, cycloalkyl, benzoheterocyclic or benzocycloalkyl substituent connected directly to the ring or attached to the ring through a —CH2—.Type: GrantFiled: July 1, 2005Date of Patent: January 26, 2010Assignee: Merck & Co., Inc.Inventors: Amjad Ali, Joann M. Napolitano, Qiaolin Deng, Zhijian Lu, Peter J. Sinclair, Gayle E. Taylor, Christopher F. Thompson, Nazia Quraishi, Cameron J. Smith, Julianne A. Hunt, Adrian A. Dowst, Yi-Heng Chen, Hong Li
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Patent number: 7629372Abstract: A class of compounds having Formula I and pharmaceutically acceptable salts thereof are useful as therapeutic compounds, particularly in the treatment of hyperlipidemia, hypercholesterolemia, dyslipidemia, and other lipid disorders, and in delaying the onset of or reducing the risk of developing conditions and sequelae that are associated with these diseases, such as atherosclerosis.Type: GrantFiled: September 12, 2005Date of Patent: December 8, 2009Assignee: Merck & Co., Inc.Inventors: James F. Dropinski, Guo Q. Shi, Yong Zhang
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Patent number: 7598243Abstract: The present invention is directed to compounds of the formula I: Wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X, n and the broken lines are as defined herein which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.Type: GrantFiled: October 15, 2004Date of Patent: October 6, 2009Assignee: Merck & Co., Inc.Inventors: Gabor Butora, Stephen D. Goble, Alexander Pasternak, Lihu Yang, Changyou Zhou, Christopher R. Moyes
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Patent number: 7589085Abstract: The present invention is further directed to compounds of the formulas: (I) (II) (wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, R17, R18, R19, R24 and R25 are as defined herein) which are modulators of chemokine receptor activity and are useful in the prevention or treatment of certain inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which chemokine receptors are involved.Type: GrantFiled: August 6, 2004Date of Patent: September 15, 2009Assignee: Merck & Co., Inc.Inventors: Gabor Butora, Lihu Yang, Stephen D. Goble
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Patent number: 7034026Abstract: The present invention is directed to compounds comprising a 2,3-diphenylquinoxaline moiety which inhibit the activity of Akt, a serine/threonine protein kinase.Type: GrantFiled: April 8, 2002Date of Patent: April 25, 2006Assignee: Merck & Co., Inc.Inventors: Stanley F. Barnett, Samuel L. Graham, David C. Remy
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Patent number: 6835727Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of Cathepsins K and L. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.Type: GrantFiled: August 23, 2002Date of Patent: December 28, 2004Assignees: Merck Frosst Canada & Co., Banyu Pharmaceutical Co., Ltd., Axys Pharmaceuticals, Inc.Inventors: Osamu Okamoto, Jean-Pierre Falgueyret, Renata Marcella Oballa, Petpiboon Prasit, Robert Rydzewski
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Patent number: 6800785Abstract: The present invention relates to processes for the synthesis of intermediates useful for the synthesis of estrogen receptor modulators. The process includes new methods for annelating 5-, 6- and 7-membered cycloalkenones onto an indanone.Type: GrantFiled: October 15, 2003Date of Patent: October 5, 2004Assignee: Merck & Co., Inc.Inventor: Dongfang Meng