Patents Examined by Sun Jae Loewe
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Patent number: 8288530Abstract: Disclosed are methods of preparing a macromolecular conjugated ligand and a metal complex thereof. The metal complex is targeted for use as a contrast agent, for example, in MRI. The method of preparing a macromolecular conjugated ligand comprises: (a) providing a compound of formula (I) wherein R, A, and Pg are as defined herein, (b) reacting the compound of formula (I) with a macromolecular compound (e.g., dendrimer) in an organic solvent medium which is substantially free of water to obtain a macromolecular conjugated compound, and (c) removing the carboxyl-protecting groups to obtain a carboxyl-deprotected macromolecular conjugated compound. The metal complex can be prepared by reacting the carboxyl-deprotected macromolecular conjugated compound with an ion (e.g., Gd(III)). Also disclosed are two carboxyl-protected 1B4M-DTPA intermediate compounds.Type: GrantFiled: November 6, 2007Date of Patent: October 16, 2012Assignee: The United States of America, as represented by the Department of Health and Human ServicesInventors: Martin W. Brechbiel, Heng Xu
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Patent number: 8288368Abstract: (R)-2-Arylpropionamide compounds of formula (I) are described. The process for their preparation and pharmaceutical preparations thereof are also described. The 2-Arylpropionamides of the invention are useful in the prevention and treatment of tissue damage due to the exacerbate recruitment of polymorphonuclear leukocytes (leukocytes PMN) and of monocytes at the inflammatory sites. In particular, the invention relates to the R enantiomers of omega-aminoalkylamides of 2-aryl propionic acids, of formula (I), for use in the inhibition of the chemotaxis of neutrophils and monocytes induced by the C5a fraction of the complement and by other chemotactic proteins whose biological activity is associated with activation of a 7-TD receptor. Selected compounds of formula (I) are dual inhibitors of both the C5a-induced chemotaxis of neutrophils and monocytes and the IL-8-induced chemotaxis of PMN leukocytes.Type: GrantFiled: February 25, 2002Date of Patent: October 16, 2012Assignee: Dompé Pha.R.Ma S.p.A.Inventors: Marcello Allegretti, Riccardo Bertini, Valerio Berdini, Cinzia Bizzarri, Maria Candida Cesta, Vito Di Cioccio, Gianfranco Caselli, Fracesco Colotta, Carmelo Gandolfi, Janete Peloia Barroso Gandolfi, legal representative, Giulio Agostino Gandolfi, legal representative, Maria Carla Gandolfi, legal representative, Arrigo Aldo Gandolfi, legal representative
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Patent number: 8283363Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.Type: GrantFiled: November 5, 2010Date of Patent: October 9, 2012Assignees: Abbott Laboratories, Abbott GmbH & Co. KGInventors: Helmut Mack, Andreas Kling, Katja Jantos, Achim Moeller, Wilfried Hornberger, Charles W. Hutchins
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Patent number: 8273341Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: GrantFiled: November 8, 2011Date of Patent: September 25, 2012Assignee: Gilead Sciences, Inc.Inventors: Hongyan Guo, Darryl Kato, Thorsten A. Kirschberg, Hongtao Liu, John O. Link, Michael L. Mitchell, Jay P. Parrish, Michael Graupe, Jianyu Sun, James Taylor, Elizabeth M. Bacon, Eda Canales, Aesop Cho, Choung U. Kim, Jeromy J. Cottell, Manoj C. Desai, Randall L. Halcomb, Evan S. Krygowski, Scott E. Lazerwith, Qi Liu, Richard Mackman, Hyung-Jun Pyun, Joseph H. Saugier, James D. Trenkle, Winston C. Tse, Randall W. Vivian, Scott D. Schroeder, William J. Watkins, Lianhong Xu
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Patent number: 8268819Abstract: The present invention relates to intermediates of the formula wherein G1 is N; G2 is selected from the group consisting of C?O and CH2; X is a halogen; and the other groups are defined herein.Type: GrantFiled: March 26, 2012Date of Patent: September 18, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Bohan Jin, Nicholas Scorah, Qing Dong
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Patent number: 8263597Abstract: Disclosed indazoles compounds that are useful as antagonists of CCR1 activity and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: GrantFiled: July 18, 2011Date of Patent: September 11, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Daniel Kuzmich, Can Mao, Alan David Swinamer, David Smith Thomson
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Patent number: 8263044Abstract: The present invention relates to novel stilbene like compounds of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts and compositions, metabolites and prodrugs thereof. The present invention more particularly provides novel stilbene like compounds of the general formula (I). Also included is a method for treatment of cancer, psoriasis, proliferative conditions and conditions mediated by HDAC, in a mammal comprising administering an effective amount of a novel compound of formula (I) as described above.Type: GrantFiled: November 6, 2006Date of Patent: September 11, 2012Assignee: Orchid Research Laboratories LimitedInventors: Akella Satya Surya Visweswara Srinivas, Urkalan Kaveri Balan, Narayana Swamy Punthalir, Rama Swamy Velmurugan, Sriram Rajagopal, Gaddam Om Reddy, Virendra Kachhadia
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Patent number: 8263634Abstract: This invention relates to compounds of formula (I) which are activators of glucokinase and thus may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial.Type: GrantFiled: November 9, 2010Date of Patent: September 11, 2012Assignee: Novo Nordisk A/SInventors: Anthony Murray, Jesper Lau, Lone Jeppesen, Per Vedsø, Michael Ankersen, Jane Marie Lundbeck, Marit Kristiansen, Maria Carmen Valcarce-Lopez, Dharma Rao Polisetti, Govindan Subramanian, Robert Carl Andrews, Daniel P. Christen, Jeremy T. Cooper, Kalpathy Chidambareswarak Santhosh
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Patent number: 8257931Abstract: A composition and method for inhibiting proliferation of a tumor cell compared to a non-tumor cell. Also described are methods of screening for a composition that inhibits cap-dependent translation compared to cap-independent translation of proteins.Type: GrantFiled: January 20, 2006Date of Patent: September 4, 2012Assignee: President and Fellows of Harvard CollegeInventors: Gerhard Wagner, Michael Chorev, Nathan John Moerke, Bertal Huseyin Aktas, José Halperin
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Patent number: 8252825Abstract: A compound having the structure wherein R is an angiotensin receptor antagonist active group, and Y is 1) —(CH2)3R5, 2) —C(O)(CH2)2R5, 3) —C(R1R2)OC(O)O(CH2)nR5, wherein n is 1 or 2, 4) —C(R1R2)OC(O)CH2CH2R5, 5) —C(R1R2)OC(O)OCH2CH2C(R3R4)R5, provided that when Y is —C(O)(CH2)2R5, then R is R1, R2, R3 and R4 are independently selected from the group consisting of hydrogen and C1-4 alkyl; R5 is —CH(ONO2)CH(ONO2)R6; R6 is selected from CH3, CH2CH3 and CH(CH3)2; or a pharmaceutically acceptable salt or hydrate thereof, which is useful for treating hypertension.Type: GrantFiled: November 21, 2008Date of Patent: August 28, 2012Assignees: NicOx, Merck Sharp & Dohme Corp.Inventors: Amjad Ali, Michael Man-Chu Lo, Christopher Franklin, Nicoletta Almirante, Silvia Stefanini, Laura Storoni, Stefano Biondi, Ennio Ongini
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Patent number: 8252923Abstract: The present invention relates to peptidomimetic compounds useful as protease inhibitors, particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel steroselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient.Type: GrantFiled: September 8, 2008Date of Patent: August 28, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Robert Edward Babine, Shu-Hui Chen, Jason Eric Lamar, Nancy June Snyder, Xicheng Sun, Mark Joseph Tebbe, Frantz Victor, Q. May Wang, Yvonne Yee Mai Yip, Ivan Collado, Cristina Garcia-Paredes, Raymond Samuel Parker, III, Ling Jin, Deqi Guo, John Irvin Glass
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Patent number: 8247549Abstract: The present invention discloses a novel method for preparing and purifying 4-(6-Amino-purin-9-yl)-2(S)-hydroxy-butyric acid methyl ester. The preparation started from cheap and easily available L-malic acid, which was transformed to intermediate I after simultaneous protection of the groups of 1-carboxyl and 2-hydroxyl. The intermediate I was selectively reduced to intermediate alcohol II, whose hydroxyl group was further transformed to an easily leaving group to afford intermediate III. The intermediate III was nucleophilically substituted with adenine to afford intermediate IV. The intermediate IV was deprotected and methyl-esterified simultaneously in methanol in the presence of an acid or a base to afford crude 4-(6-Amino-purin-9-yl)-2(S)-hydroxy-butyric acid methyl ester, which was purified by recrystallization to afford the purified product.Type: GrantFiled: November 6, 2008Date of Patent: August 21, 2012Assignee: Shanghai Institute of Materia Medica, Chinese Academy of SciencesInventors: Fajun Nan, Jianping Zuo, Yangming Zhang, Min Gu, Wei Tang
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Patent number: 8247583Abstract: Disclosed is a 3-ethyloxethane compound having a hydroxyl group which is represented by the following general formula (1). (1) (In the formula, A represents an alkylene group having 3-5 carbon atoms which may have an ether bond or an alkylene group having 3-5 carbon atoms which may be substituted by a hydroxyl group.) The 3-ethyloxethane compound having a hydroxyl group can be produced by reacting a 3-ethyloxethane compound represented by the general formula (2) below, a diol compound represented by the general formula (3) below and a base. (2) (In the formula, X represents a leaving group.) (3) (In the formula, A is as defined above.Type: GrantFiled: June 5, 2007Date of Patent: August 21, 2012Assignee: UBE Industries, Ltd.Inventors: Kenji Hirotsu, Tadashi Murakami
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Patent number: 8242117Abstract: Provided are 5-membered heterocycle-based p38 kinase inhibitors. Further provided are pyrazole and imidazole-based p38 kinase, including p38? and p38? kinase, inhibitors. Pharmaceutical compositions containing the compounds are also provided. Methods of use of the compounds and compositions are also provided, including methods of treatment, prevention, or amelioration of one or more symptoms of p38 kinase mediated diseases and disorders, including, but not limited to, inflammatory diseases and disorders.Type: GrantFiled: November 19, 2010Date of Patent: August 14, 2012Assignee: Novartis AGInventors: Olga M. Fryszman, Hengyuan Lang, Jiong Lan, Edcon Chang, Yunfeng Fang
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Patent number: 8236798Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.Type: GrantFiled: April 27, 2010Date of Patent: August 7, 2012Assignees: Abbott GmbH & Co. KG, Abbott LaboratoriesInventors: Helmut Mack, Andreas Kling, Katja Jantos, Achim Moeller, Wilfried Hornberger, Charles W. Hutchins
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Patent number: 8227630Abstract: The present invention concerns a process for the preparation of a compound of formula (I) wherein the dotted line is a single bond and n is 1 or the dotted line is a double bond and n is 0, and wherein the relative configuration is as shown, in the form of any one of its diastereoisomers or enantiomers or mixtures thereof.Type: GrantFiled: October 20, 2008Date of Patent: July 24, 2012Assignee: Firmenich SAInventor: Charles Fehr
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Patent number: 8221737Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: GrantFiled: June 15, 2010Date of Patent: July 17, 2012Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yat Sun Or, Xiaowen Peng, Lu Ying, Ce Wang, Yao-Ling Qiu
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Patent number: 8211402Abstract: A compound that recognizes and binds to the CA-IX protein has Formula I, II, III, or IV. The compounds may include a radioactive element for radioimaging or therapeutic applications. Thus, pharmaceutical compositions may be prepared with one or more of the compounds of Formula I, II, III, or IV.Type: GrantFiled: December 4, 2009Date of Patent: July 3, 2012Assignee: Molecular Insight Pharmaceuticals, Inc.Inventors: John W. Babich, Craig Zimmerman, John Joyal, Kevin P. Maresca, Genliang Lu, Shawn Hillier
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Patent number: 8212050Abstract: Novel amidine compounds which may be active ingredients in herbicides that are reliably effective at a lesser dose and highly safe, and herbicides containing these compounds as active ingredients are provided. Amidine compounds represented by a formula (1?) and herbicides containing at least one kind of these compounds as active ingredients, [wherein G is an optionally substituted nitrogen-containing heterocyclic group represented by a formula (2?) with a proviso that the number of carbons constituting the nitrogen-containing heterocycle of the nitrogen-containing heterocyclic group is 10 or less and that 2H-Indazole ring is excluded; Q? represents cyano or the like; and A? represents substituted phenyl or the like].Type: GrantFiled: August 2, 2006Date of Patent: July 3, 2012Assignee: Nippon Soda Co., Ltd.Inventors: Yasuhiro Miyashita, Koichi Kutose, Kazuyuki Tomida, Shigeo Yamada
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Patent number: 8211939Abstract: The present invention relates to new 3-substituted 6-nitrooxy-hexahydrofuro[3,2-b]furane derivatives possessing a superior pharmacological activity in thrombosis and in coronary ischemia models.Type: GrantFiled: December 15, 2008Date of Patent: July 3, 2012Assignee: Lacer, S.A.Inventors: Juan Carlos Del Castillo Nieto, Marisabel Mourelle Mancini, Francisco Pubill Coy, Lydia Cabeza Llorente, Jose Repolles Moliner