Patents Represented by Attorney Nicole M. Beeler
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Patent number: 8318748Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.Type: GrantFiled: May 25, 2011Date of Patent: November 27, 2012Assignees: Merck, Sharp & Dohme Corp., Axys Pharmaceuticals, Inc.Inventors: Christopher I. Bayly, Cameron Black, Serge Leger, Chun Sing Li, Dan McKay, Christophe Mellon, Jacques Yves Gauthier, Vouy-Linh Truong, Cheuk Lau, Michel Therien, Michael J. Green, Bernard L. Hirschbein, James William Janc, James T. Palmer, Chitra Baskaran
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Patent number: 8273913Abstract: This invention describes an amidation process whereby amino acids of the Formulae IIA or IIB can be activated and treated with an amine in the presence of a base to yield amides of the Formula (I), without loss of optical purity.Type: GrantFiled: March 31, 2008Date of Patent: September 25, 2012Assignee: Merck Canada Inc.Inventors: Paul O'Shea, Francis Gosselin
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Patent number: 8173655Abstract: Compounds of formula I: (wherein variables A1, A2, B, m, n, J, R4, G1, G2, G3 and Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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 CGRP is involved.Type: GrantFiled: April 11, 2008Date of Patent: May 8, 2012Assignee: Merck, Sharp & Dohme Corp.Inventors: Ian M. Bell, Harold G. Selnick, Craig A. Stump
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Patent number: 8163752Abstract: Compounds of formula I: wherein variables A1, A2, B, m, n, J, R4, G1, G2, G3 and Y are as described herein, which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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 CGRP is involved.Type: GrantFiled: June 3, 2008Date of Patent: April 24, 2012Assignee: Merck, Sharp & Dohme Corp.Inventors: Ian Bell, Craig A. Stump
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Patent number: 8148390Abstract: The present invention is directed to compounds of Formula I: (where variables A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. 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 CGRP is involved.Type: GrantFiled: March 7, 2008Date of Patent: April 3, 2012Assignee: Merck, Sharp & Dohme, Corp.Inventors: Craig A. Stump, Ian M. Bell, Harold G. Selnick
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Patent number: 8143266Abstract: Compounds of formula I: (wherein variables A1, A2, B, m, n, J, X, R4, G1, G2, G3 and Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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 CGRP is involved.Type: GrantFiled: April 11, 2008Date of Patent: March 27, 2012Assignee: Merck, Sharp & Dohme CorpInventors: Ian M. Bell, Harold G. Selnick, Craig A. Stump
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Patent number: 8133891Abstract: The present invention is directed to compounds of Formula I: I (where A1, A2, B1, B2, B3, B4, D1, D2, J, K, T, U, V, W, X, Y, Z, R4, R5a, R5b, R5c, m and n are defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. 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 CGRP is involved.Type: GrantFiled: March 5, 2010Date of Patent: March 13, 2012Assignee: Merck, Sharp & Dohme Corp.Inventors: Ian M. Bell, Steven N. Gallicchio, Craig A. Stump, Cory R. Theberge, Joseph P. Vacca, C. Blair Zartman, Xufang Zhang
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Patent number: 8030327Abstract: The present invention relates to a compound represented by the Formula [I]: Wherein: the A ring is a 5-membered aromatic heterocyclic group containing at least one hetero atom selected from a nitrogen atom, and the like; A1 and A2, are each a nitrogen atom, and the like; X2, X3, X4, and X5 are all carbon atoms, or alternatively any one of X2, X3, X4, and X5 is a nitrogen atom and the rest are all carbon atoms; R1 is a hydrogen atom, or the like; R2, R3, R4, and R5, are each a hydrogen atom, or the like; R6 and R6?, are each a hydrogen atom, and the like; R7 is an aryl group and the like; and R8 is an amino group or a hydroxy group, or a pharmaceutically acceptable salt or ester thereof.Type: GrantFiled: November 7, 2005Date of Patent: October 4, 2011Assignee: MDS K.K.Inventors: Yoshiyuki Sato, Hideki Kurihara, Kaori Kamijo, Yu Onozaki, Toshiaki Tsujino, Tetsuya Sugimoto, Akiko Watanabe, Morihiro Mitsuya, Hideya Komatani
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Patent number: 7977336Abstract: The present invention relates to a compound represented by Formula [I]: or a pharmaceutically acceptable salt or ester thereof, wherein R1 and R2, which may be the same or different, are each a hydrogen atom, a lower alkyl group, a cycloalkyl group, or the like; R3 and R4, which may be the same or different, are each a hydrogen atom, a lower alkyl group, NRaRb, a phenyl group, a lower alkyl group substituted with a phenyl group, a 4-to 7-membered aliphatic heterocyclic group, a lower alkyl group substituted with a 4- to 7-membered aliphatic heterocyclic group, a 5-or 6-membered aromatic heterocyclic group, a lower alkyl group substituted with a 5-or 6-membered aromatic heterocyclic group, or the like; and R5 is a hydrogen atom, a cyano group, a halogen atom, or a lower alkyl group.Type: GrantFiled: December 18, 2007Date of Patent: July 12, 2011Assignee: Banyu Pharmaceutical Co. LtdInventors: Takashi Hashihayata, Mikako Kawamura, Morihiro Mitsuya, Yoshiyuki Sato
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Patent number: 7973037Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.Type: GrantFiled: April 8, 2008Date of Patent: July 5, 2011Assignees: Axys Pharmaceuticals, Inc., Merck Canada Inc.Inventors: Christopher I. Bayly, Cameron Black, Serge Leger, Chun Sing Li, Dan McKay, Christophe Mellon, Jacques Yves Gauthier, Vouy-Linh Truong, Cheuk Lau, Michel Therien, Michael J. Green, Bernard L. Hirschbein, James William Janc, James T. Palmer, Chitra Baskaran
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Patent number: 7935708Abstract: The invention relates to compounds of a general formula (I): wherein Ar1 is an optionally-substituted aryl or heteroaromatic group; R1 is an optionally-substituted lower alkyl, lower alkenyl, lower alkynyl or cyclo-lower alkyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R2 is a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R3 is a hydrogen atom or a lower alkyl group; R4 is a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a group of —N(R1k)R1m; T and U are a nitrogen atom or a methine group, etc. The compounds of the invention have excellent Weel kinase-inhibitory effect and are therefore useful in the field of medicines, especially treatment of various cancers.Type: GrantFiled: April 25, 2007Date of Patent: May 3, 2011Assignee: MSD K.K.Inventors: Takeshi Sagara, Sachie Otsuki, Satoshi Sunami, Toshihiro Sakamoto, Kenji Niiyama, Fuyuki Yamamoto, Takashi Yoshizumi, Hidetomo Furuyama, Yasuhiro Goto, Makoto Bamba, Keiji Takahashi, Hiroshi Hirai, Toshihide Nishibata
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Patent number: 7928091Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.Type: GrantFiled: July 5, 2006Date of Patent: April 19, 2011Assignee: Merck Frosst Canada Ltd.Inventors: Cameron Black, Sheldon Crane, Renata Oballa, Joel Robichaud
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Patent number: 7915407Abstract: The present invention is concerned with a process for the preparation of the compound {3-[2(R)-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3(S)-(4-fluorophenyl) -morpholin-4-yl]methyl]-5-oxo-4,5-dihydro-[1,2,4]-triazol-1-yl}phosphonic acid, and pharmaceutically acceptable salts thereof. This compound is useful as a substance P (neurokinin-1) receptor antagonist. In particular, the compound is useful e.g., in the treatment of emesis and inflammatory diseases.Type: GrantFiled: August 25, 2010Date of Patent: March 29, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: James Michael McNamara, Louis Matty, Jonathan D. Rosen
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Patent number: 7847095Abstract: The present invention is concerned with a novel process for the preparation of the compound 5-[[2(R)-[1(R)-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3(S)-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2-dihydro-3H-1,2,4 -tria-zol-3-one. This compound is useful as a substance P (neurokinin-1) receptor antagonist. In particular, the compound is useful e.g., in the treatment of psychiatric disorders, inflammatory diseases and emesis.Type: GrantFiled: April 17, 2003Date of Patent: December 7, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: David Hands, Mark Huffman, Mahmoud S. Kaba, Joseph F. Payack
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Patent number: 7834019Abstract: The invention relates to compounds of a general formula (I): wherein Ar1 is an optionally-substituted aryl or heteroaromatic group; R1 is an optionally-substituted lower alkyl, lower alkenyl, lower alkynyl or cyclo-lower alkyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R2 is a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R3 is a hydrogen atom or a lower alkyl group; R4 is a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a group of —N(R1k)R1m; T and U are a nitrogen atom or a methine group, etc. The compounds of the invention have excellent Weel kinase-inhibitory effect and are therefore useful in the field of medicines, especially treatment of various cancers.Type: GrantFiled: April 25, 2007Date of Patent: November 16, 2010Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Takeshi Sagara, Sachie Otsuki, Satoshi Sunami, Toshihiro Sakamoto, Kenji Niiyama, Fuyuki Yamamoto, Takashi Yoshizumi, Hidetomo Furuyama, Yasuhiro Goto, Makoto Bamba, Keiji Takahashi, Hiroshi Hirai, Toshihide Nishibata
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Patent number: 7807829Abstract: The present invention is concerned with a process for the preparation of the compound {3-[2(R)-[(1R)-1-[3,5-bis(tri-fluoromethyl)phenyl]ethoxy]-3(S)-(4-fluorophenyl)-morpholin-4-yl]methyl]-5-oxo-4,5-dihydro-[1,2,4]-triazol-1-yl}phosphonic acid, and pharmaceutically acceptable salts thereof. This compound is useful as a substance P (neurokinin-1) receptor antagonist. In particular, the compound is useful e.g., in the treatment of emesis and inflammatory diseases.Type: GrantFiled: November 3, 2005Date of Patent: October 5, 2010Assignees: Merck & Co., Inc., Merck Sharp & Dohme Corp.Inventors: James Michael McNamara, Louis Matty, Jonathan D. Rosen
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Patent number: 7763634Abstract: The instant invention provides for tetracyclic compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.Type: GrantFiled: June 5, 2007Date of Patent: July 27, 2010Assignees: Merck & Co., Inc., Merck Sharp & Dohme Corp.Inventors: Jonathan R. Young, Andrew Haidle, Paul Tempest, Michelle Machacek
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Patent number: 7745639Abstract: The present invention relates to dihydropyrazole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: GrantFiled: March 4, 2003Date of Patent: June 29, 2010Assignees: Merck & Co., Inc., Merck Sharp & Dohme Corp.Inventors: Michael J. Breslin, Paul J. Coleman, Christopher D. Cox, J. Christopher Culberson, George D. Hartman, Brenda J. Mariano, Maricel Torrent
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Patent number: 7732472Abstract: The present invention relates to dihydroisoxazoles that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also relates to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: GrantFiled: August 15, 2005Date of Patent: June 8, 2010Assignees: Merck & Co., Inc., Merck Sharp & Dohme Corp.Inventors: Mark E. Fraley, Robert M. Garbaccio, George D. Hartman
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Patent number: 7723365Abstract: The present invention relates to oxadiazoles that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also relates to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: GrantFiled: August 15, 2005Date of Patent: May 25, 2010Assignees: Merck & Co., Inc., Merck Sharp & Dohme Corp.Inventors: Christopher D. Cox, Mark E. Fraley, Robert M. Garbaccio