The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 548/204)
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Publication number: 20090012133Abstract: The present invention relates to a novel polymorphic form of the compound {2-methyl-4-[4-methyl-2-(4-trifluoromethylphenyl)thiazol-5-ylmethylthio]phenoxy}-acetic acid, methods of preparing it, pharmaceutical compositions and medicaments containing the same, and use of such polymorphs, compositions and medicaments in the treatment of PPAR mediated diseases or conditions.Type: ApplicationFiled: January 10, 2007Publication date: January 8, 2009Applicant: SMITHKLINE BEECHAM CORPORATIONInventor: Gonzalo Alva
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Patent number: 7468360Abstract: Disclosed herein is a compound having a structure: Therapeutic methods, compositions, and medicaments relating thereto are also disclosed.Type: GrantFiled: August 8, 2007Date of Patent: December 23, 2008Assignee: Allergan, Inc.Inventors: David W. Old, Danny T. Dinh
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Publication number: 20080312300Abstract: The invention relates to processes for the preparation of a polymorphic form of ritonavir. More particularly, it relates to the preparation of a stable polymorphic Form I of ritonavir. The invention also relates to pharmaceutical compositions that include the stable Form I of ritonavir and use of the compositions for treatment of HIV infections in combination with other antiretro viral agents.Type: ApplicationFiled: May 30, 2006Publication date: December 18, 2008Inventors: Yoginder Pal Sachdeva, Prosenjit Bose
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Patent number: 7465804Abstract: The present invention provides compounds useful, for example, for modulating insulin levels in a subject, having the general formula I: wherein Q is an optionally substituted phenyl; L is a bond or O; P is a benzene or an optionally substituted thiazole ring; and R1 has the values provided herein. The present invention also provides compositions, uses, and methods for use of the compounds, for instance, for treatment of type II diabetes.Type: GrantFiled: May 17, 2006Date of Patent: December 16, 2008Assignee: Amgen Inc.Inventors: Jonathan Houze, Jiwen Liu, Zhihua Ma, Julio C. Medina, Michael J. Schmitt, Rajiv Sharma, Ying Sun, Yingcai Wang, Liusheng Zhu
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Publication number: 20080306121Abstract: The present invention provides small molecule compounds of bisheterocycle in tandem having the structural formula of P1-P2, and the use thereof as well as a composition containing the compounds, each of P1 and P2 is an unsaturated 5-member heterocyclic ring having one or two heteroatoms. This compound may effectively inhibit the replication of influenza virus, the DNA replication of hepatitis B virus (HBV), and the formation of HBsAg and HBeAg. These compounds can be used for the preparation of a medicament for viral diseases, and may overcome the limitations of the known nucleosides drugs, including cytotoxicity, the requirement of other drugs having different structures for against the drug-resistant virus variants induced by long-term therapy. The structure of the compounds according to the invention is relatively simple and easy to be prepared.Type: ApplicationFiled: January 24, 2006Publication date: December 11, 2008Applicant: Shanghai Institute of Materia Medica, Chinese Academy of SciencesInventors: Fajun Nan, Jianping Zuo, Wenlong Wang, Haijun Chen, Peilan He
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Publication number: 20080287409Abstract: The present invention comprises phenyl and pyridinyl 1,2,4-oxadiazolone compounds their physiologically acceptable salts and physiologically functional derivatives that exhibit peroxisome proliferator activator receptor (PPAR) delta agonist activity. Also described and claimed are processes for their preparation and their use as pharmaceuticals. These are compounds of formula I, in which the R-group substituents are defined herein. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and de-myelinating and other neurodegenerative disorders of the central and peripheral nervous system.Type: ApplicationFiled: March 26, 2008Publication date: November 20, 2008Applicant: SANOFI-AVENTISInventors: Patrick Bernardelli, Stefanie Keil, Matthias Urmann, Hans Matter, Wolfgang Wendler, Maike Glien, Karen Chandross, Lan Lee, Corinne Terrier, Herve Minoux
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Patent number: 7449468Abstract: The present invention provides a compound of formula (I): wherein R1-R5, R25, R26, Y, y, and X2are as defined herein. The compounds activate human peroxisome proliferater activated receptors (hPPARs) and are useful for the treatment of associated disorders such as dyslipidemia, syndrome X, hypercholesteremia, type II diabetes mellitus, type I diabetes, insulin resistance, hyperlipidemia, and obesity.Type: GrantFiled: May 25, 2007Date of Patent: November 11, 2008Assignee: SmithKline Beecham CorporationInventors: Pierette Banker, Rodolfo Cadilla, Millard Hurst Lambert, III, Stephen William Rafferty, Daniel David Sternbach, Marcos Luis Sznaidman
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Publication number: 20080262036Abstract: The present invention comprises phenyl-[1,2,4]-oxadiazol-5-one derivatives of the general formula I: wherein the R1-R10 and B, U, V, W, X, Y and Z substituents are defined herein. The claimed invention also comprises the compounds isomers and their physiologically acceptable salts as well as processes for their preparation. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.Type: ApplicationFiled: March 26, 2008Publication date: October 23, 2008Applicant: SANOFI-AVENTISInventors: Stefanie Keil, Patrick Bernardelli, Matthias Urmann, Hans Matter, Wolfgang Wendler, Maike Glien, Karen Chandross, Lan Lee
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Publication number: 20080255202Abstract: The present application relates to novel phenylthioacetic acid derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular disorders, in particular dyslipidaemias and arteriosclerosis.Type: ApplicationFiled: March 26, 2005Publication date: October 16, 2008Applicant: Bayer HealthCare AGInventors: Hilmar Bischoff, Elke Dittrich-Wengenroth, Nils Griebenow, Axel Kretschmer, Joachim Kruger, Elisabeth Woltering, Lars Barfacker, Claudia Hirth-Dietrich, Peter Ellinghaus, Martin Raabe, Stephen Bartel, Christian Pilger, Ulrich Rosentreter, Klemens Lustig, Armin Kern, Dieter Lang
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Publication number: 20080249093Abstract: The present invention encompasses compounds of Formula I: as well as the pharmaceutically acceptable salts thereof. The compounds are S1P1/Edg1 receptor agonists and thus have immunosuppressive, anti-inflammatory and hemostatic activities by modulating leukocyte trafficking, sequestering lymphocytes in secondary lymphoid tissues, and enhancing vascular integrity. The invention is also directed to pharmaceutical compositions containing such compounds and methods of treatment or prevention.Type: ApplicationFiled: December 13, 2004Publication date: October 9, 2008Applicant: MERCK & CO., INC.Inventors: Vincent J. Colandrea, George A. Doherty, Jeffrey J. Hale, Pei Huo, Irene E. Legiec, Leslie Toth, Petr Vachal, Lin Yan
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Publication number: 20080242869Abstract: Compounds of Formula (I) or pharmaceutically acceptable salts thereof, are useful in the prophylactic and therapeutic treatment of hyperglycemia and diabetes.Type: ApplicationFiled: April 19, 2005Publication date: October 2, 2008Inventor: Matthew Fyfe
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Publication number: 20080233163Abstract: Disclosed are novel NO-donating compounds, designed such that when NO is released from the compound a residue which is a naturally occurring metabolite is formed, and thus a development of tolerance to the compounds upon repetitive administration is prevented or decreased. Also disclosed are methods of preparing such NO-donating compounds, pharmaceutical compositions and medical devices containing such compounds and methods utilizing such compounds in the treatment of various medical conditions.Type: ApplicationFiled: March 24, 2008Publication date: September 25, 2008Applicant: Renopharm Ltd.Inventor: Peter Assaf
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Publication number: 20080234344Abstract: The invention provides novel compounds of general formula I wherein R1, R2 and R3 are independently hydrogen, OR4, C1-C6 alkyl or C2-C6 alkenyl, R4 is hydrogen, C1-C6 alkyl or C2-C6 alkenyl, —N-(AA) represents the residue of an amino acid or of a peptide which is bonded over the N-terminus of the amino acid or the peptide and the peptide is composed of 2 to 6, that means 2, 3, 4, 5 or 6, amino acids, wherein the C-terminus of the amino acid or the peptide is optionally esterified with a C1-C16 hydrocarbon moiety and n is an integer of 1 to 5. The compounds are in particular useful for cosmetic applications.Type: ApplicationFiled: March 23, 2005Publication date: September 25, 2008Inventors: Jochen Klock, Philippe Emmanuel Maillan, Juergen H. Vollhardt, Raphael Beumer
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Publication number: 20080227794Abstract: Compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and n are as defined in the description, processes for the preparing the compounds, new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and uses of the compounds in therapy.Type: ApplicationFiled: February 15, 2006Publication date: September 18, 2008Inventors: Bradford Van Wagenen, Radhakrishnan Ukkiramapandian, Joshua Clayton, Ian Egle, James R. Empfield, Methvin Isaac, Fupeng Ma, Abdelmalik Slassi, Gary Steelman, Rebecca Urbanek, Sally Walsh
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Publication number: 20080227744Abstract: Resistance-repellent and multidrug resistant retroviral protease inhibitors are provided. Pharmaceutical composition comprising such compounds, and methods of using such compounds to treat HIV infections in mammals, are also provided.Type: ApplicationFiled: March 17, 2008Publication date: September 18, 2008Applicant: SEQUOIA PHARMACEUTICALS, INC.Inventor: Michael Eissenstat
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Publication number: 20080214448Abstract: The present invention relates to novel compounds, methods, and formulations useful for the oral delivery of a GLP-1 compound or an MC4 agonist peptide.Type: ApplicationFiled: August 18, 2004Publication date: September 4, 2008Applicant: EMISPHERE TECHNOLOGIES INC.Inventors: Robert Jason Herr, Louis Nickolaus Jungheim, John McNeill McGill, Kenneth Jeff Thrasher, Muralikrishna Valluri
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Publication number: 20080207620Abstract: The present application provides for a compound of Formula IV, or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods and include the administration of such compounds with at least one additional therapeutic agent.Type: ApplicationFiled: February 22, 2008Publication date: August 28, 2008Inventors: Manoj C. Desai, Allen Y. Hong, Hon C. Hui, Hongtao Liu, Randall W. Vivian, Lianhong Xu
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Patent number: 7407975Abstract: This invention relates to the new epothilone derivatives of general formula I, in which substituents Y, Z, R2a, R2b, R3, R4a, R4b, D-E, R5, R6, R7, R8 and X have the meanings that are indicated in more detail in the description. The new compounds interact with tubulin by stabilizing microtubuli that are formed. They are able to influence the cell-splitting in a phase-specific manner and are suitable for treating malignant tumors, for example, ovarian, stomach, colon, adeno-, breast, lung, head and neck carcinomas, malignant melanomas, acute lymphocytic and myelocytic leukemia. In addition, they are suitable for anti-angiogenesis therapy as well as for treatment of chronic inflammatory diseases (psoriasis, arthritis). To avoid uncontrolled proliferation of cells and for better compatibility of medical implants, they can be applied or introduced into polymer materials.Type: GrantFiled: August 10, 1998Date of Patent: August 5, 2008Assignee: Bayer Schering Pharma AGInventors: Ulrich Klar, Wolfgang Schwede, Werner Skuballa, Bernd Buchmann
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Patent number: 7407959Abstract: 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: November 18, 2005Date of Patent: August 5, 2008Assignee: Merck Frosst Canada & Co.Inventors: Jacques Yves Gauthier, Chun Sing Li, Christophe Mellon
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Publication number: 20080161351Abstract: Compounds, compositions and methods that are useful for the treatment of metabolic disorders, inflammatory diseases and cancer are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of proteins involved in lipid metabolism, inflammation and cell proliferation. The subject compounds are linked biaryl compounds.Type: ApplicationFiled: August 20, 2004Publication date: July 3, 2008Inventors: Hiroyuki Abe, Jonathan Houze, Hisashi Kawasaki, Frank Kayser, Rajiv Sharma, Samuel Sperry
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Publication number: 20080161580Abstract: The invention relates to new protected 3,5-dihydroxy-2,2-dimethyl-valeroamides for the synthesis of epothilones and derivatives and process for the production and the use of the new compounds for the production of epothilones or epothilone derivatives.Type: ApplicationFiled: March 6, 2008Publication date: July 3, 2008Inventors: Jurgen Westermann, Johannes Platzek, Orlin Petrov
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Publication number: 20080132494Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is a group of formula A or formula B, and X, R2, R3, R4, R5, R6, Ra and Rb are as defined herein. Also provided are methods of using the compounds for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist and methods of making the subject compounds.Type: ApplicationFiled: November 8, 2007Publication date: June 5, 2008Inventors: Michael Patrick Dillon, Ronald Charles Hawley, Li Chen, Lichun Feng, Minmin Yang
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Publication number: 20080125467Abstract: The present invention provides novel beta-secretase inhibitors and methods for their use, including methods of treating of Alzheimer's disease.Type: ApplicationFiled: September 19, 2005Publication date: May 29, 2008Inventors: Arun K. Ghosh, Hui Lei, Thippeswamy Devasamudram, Jordan J. N. Tang, Geoffrey Bilcer, Chungfeng Liu
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Patent number: 7375134Abstract: 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: February 28, 2003Date of Patent: May 20, 2008Assignees: Axys Pharmaceuticals, Inc., Merck Frosst Canada & Co.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
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Publication number: 20080114175Abstract: The present invention is directed to a process for preparing certain cysteine protease inhibitors.Type: ApplicationFiled: September 16, 2005Publication date: May 15, 2008Inventor: Jiayao Li
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Patent number: 7361769Abstract: The present invention discloses compounds of formula I wherein m, n, p, R1, R2 and X, are herein defined, the compounds being novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.Type: GrantFiled: July 14, 2005Date of Patent: April 22, 2008Assignee: Schering CorporationInventors: Jing Su, Brian A. McKittrick, Haiqun Tang, Thavalakulamgara K. Sasikumar, Li Qiang
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Patent number: 7358266Abstract: The invention relates to cis- and trans-12, 13-cyclopropyl and 12,13-cyclobutyl epothilones of formula I to IV wherein Ar is a radical represented by the following structure: and the other radicals and symbols have the meanings as defined herein; to their chemical synthesis and biological evaluation; their use in the treatment of neoplastic diseases and to pharmaceutical preparations containing such compounds. The compounds described herein are potent tubulin polymerization promoters and cytotoxic agents.Type: GrantFiled: August 23, 2002Date of Patent: April 15, 2008Assignee: The Scripps Research InstituteInventors: Kyriacos C. Nicolaou, Kenji Namoto, Andreas Ritzen, Mitsuru Shoji, Trond Ulven, Karl-Heinz Altmann
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Patent number: 7351825Abstract: The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): wherein R1 is —(CH2)m—X—(CH2)n-A1 etc., wherein m and n are the same or different and each is 0 to 6, X is a single bond, etc. and A1 is a substituted C3-14 hydrocarbon ring group, etc.; R2 and R3 are the same or different and each is a hydrogen atom, —(CH2)p—X1—(CH2)q-A2, etc., wherein p and q are the same or different and each is 0 to 6, X1 is a single bond, etc. and A2 is an optionally substituted C3-14 hydrocarbon ring group, etc.; R4 is —CO2R9, etc., wherein R9 is a hydrogen atom, etc.; and R20 and R21 are the same or different and each is a hydrogen atom, —(CH2)m12—X12—(CH2)m12—R30, etc., wherein m12 and m12 are the same or different and each is 0 to 6, X12 is a single bond, etc. and R30 is a hydrogen atom, etc.Type: GrantFiled: December 15, 2004Date of Patent: April 1, 2008Assignee: Japan Tobacco Inc.Inventors: Takashi Inaba, Julia Haas, Makoto Shiozaki, Nicole M. Littmann, Katsutaka Yasue, Steven W. Andrews, Atushi Sakai, Andrew M. Fryer, Takafumi Matsuo, Ellen R. Laird, Akira Suma, Yuichi Shinozaki, Yoshikazu Hori, Hiroto Imai, Tamotsu Negoro
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Patent number: 7345067Abstract: This invention relates to compounds of the formula wherein X is N and Y is S or O; or X is S or O and Y is N; R1 is hydrogen or C1-7-alkyl; R2 and R3 independently from each other are selected from the group consisting of hydrogen, C1-7-alkyl and C1-7-alkoxy; R4, R5, R6, and R7 independently from each other are selected from the group consisting of hydrogen, C1-7-alkyl, C3-7-cycloalkyl, halogen, C1-7-alkoxy, C1-7-alkyl-C1-7-alkoxy-C1-7-alkyl, C2-7-alkenyl, C2-7-alkinyl, fluoro-C1-7-alkyl and cyano; R8 is selected from the group consisting of hydrogen, C1-7-alkyl, C3-7-cycloalkyl and fluoro-C1-7-alkyl; R9 is selected from the group consisting of hydrogen, C1-7-alkyl, C2-7-alkinyl, C3-7-cycloalkyl and fluoro-C1-7-alkyl; R10 is selected from the group consisting of hydrogen, C1-7-alkyl, C2-7-alkinyl, C3-7-cycloalkyl and fluoro-C1-7-alkyl; R11 is aryl or heteroaryl; N is 0, 1 or 2; and all enantiomers and pharmaceutically acceptable salts and/or esters thereof and their use as PPAR activators.Type: GrantFiled: June 1, 2004Date of Patent: March 18, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Jean Ackermann, Johannes Aebi, Alfred Binggeli, Uwe Grether, Georges Hirth, Bernd Kuhn, Hans-Peter Maerki, Markus Meyer, Peter Mohr, Matthew Blake Wright
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Patent number: 7332608Abstract: The present invention is related to a process for preparing anthranilamides of formula I, in which R(1) to R(7) have the meanings indicated herein, a process for their preparation, their use as medicaments, and pharmaceutical preparations containing them. The compounds act on the Kv1.5 potassium channel and inhibit a potassium current which is referred to as the ultra-rapidly activating delayed rectifier in the atrium of the human heart. The compounds are therefore suitable for use as novel antiarrhythmic agents for the treatment and prophylaxis of atrial arrhythmias (e.g., atrial fibrillation (AF) or atrial flutter).Type: GrantFiled: November 9, 2006Date of Patent: February 19, 2008Assignee: SANOFI-AVENTIS Deutschland GmbHInventors: Joachim Brendel, Stefan Peukert, Heinz-Werner Kleemann, Horst Hemmerle
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Publication number: 20080038225Abstract: The present invention relates to compounds of Formula I or II, or pharmaceutically acceptable salts, esters or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. 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 to the subject a pharmaceutical composition comprising a compound of the present invention.Type: ApplicationFiled: August 7, 2007Publication date: February 14, 2008Inventors: Ying Sun, Yat Sun Or, Zhe Wang
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Patent number: 7323573Abstract: Recombinant Myxococcus host cells can be used to produce polyketides, including epothilone and epothilone analogs that can be purified from the fermentation broth and crystallized.Type: GrantFiled: August 8, 2005Date of Patent: January 29, 2008Assignee: Kosan Biosciences, Inc.Inventor: Robert L. Arslanian
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Patent number: 7312211Abstract: Disclosed are cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R2, R3, R4, R6, R8 and Y are defined herein. The compounds are useful for treating autoimmune and other diseases.Type: GrantFiled: August 26, 2004Date of Patent: December 25, 2007Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Younes Bekkali, Denice Mary Spero, Sanxing Sun, Yancey David Ward
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Patent number: 7309709Abstract: The present invention relates to compounds of the Formula: wherein R1 to R6, X, Z and A are as defined. These compounds have activity inhibiting production of A?-peptide. The invention also relates to pharmaceutical compositions and methods for treating diseases, for example, neurodegenerative diseases, e.g., Alzheimer's disease, in a mammal comprising compounds of the present Formula.Type: GrantFiled: March 11, 2005Date of Patent: December 18, 2007Assignee: Pfizer Inc.Inventor: Lei Zhang
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Patent number: 7294640Abstract: The present invention relates to substituted thiazole derivatives that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin and MCAK activity, and for inhibiting KSP kinesin and MCAK. The invention also relates to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: GrantFiled: January 21, 2005Date of Patent: November 13, 2007Assignee: Merck & Co., Inc.Inventors: Paul J. Coleman, Robert M. Garbaccio, Lou Anne Neilson
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Patent number: 7265137Abstract: A compound represented by the following general formula (I): (wherein R1 represents phenyl, etc. which can have substituents selected from the group consisting of C1-8 alkyl, C1-8 alkyl having halogen, halogen, hydroxyl, etc.; R2 represents C1-8 alkyl, etc.; A represents oxygen, sulfur, etc.; X represents C1-8 alkylene chain, etc.; Y represents C(?O), CH?CH, etc.; R3, R4, and R5 each represents hydrogen, C1-8 alkyl, etc.; B represents CH or nitrogen; Z represents oxygen or sulfur; R6 and R7 each represents hydrogen, C1-8 alkyl, etc.; and R8 represents hydrogen or C1-8 alkyl; provided that at least one of R3, R4, and R5 is not hydrogen) or a salt of the compound; and a PPAR-? activator which contains the compound or salt as the active ingredient.Type: GrantFiled: August 2, 2002Date of Patent: September 4, 2007Assignee: Nippon Chemiphar Co., Ltd.Inventors: Shogo Sakuma, Tomio Yamakawa, Takashi Kanda, Seiichiro Masui
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Patent number: 7259157Abstract: Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain.Type: GrantFiled: April 2, 2002Date of Patent: August 21, 2007Assignee: Merck & Co., Inc.Inventors: Nigel J. Liverton, John W. Butcher, Charles McIntyre, Christopher F. Claiborne, David A. Claremon, John A. McCauley, Joseph J. Romano, Wayne Thompson, Peter M. Munson
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Patent number: 7250412Abstract: The present invention is directed to water-soluble derivatives of 2,6-diisopropylphenol (Propofol). The compounds act as prodrugs of 2,6-diisopropylphenol and metabolize rapidly to Propofol thereby providing an alternative to the water-insoluble 2,6-diisopropylphenol. Pharmaceutical compositions comprising these compounds, methods of induction and maintenance of anesthesia or sedation as well as methods of treating neurodegenerative diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.Type: GrantFiled: March 15, 2004Date of Patent: July 31, 2007Assignee: Auspex Pharmaceuticals, Inc.Inventors: Subramanian Marappan, Cris Davenport, Sepehr Sarshar
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Patent number: 7244594Abstract: A microbial method for the preparation of an epothilone containing a terminal hydroxyalkyl group, comprising contacting at least one epothilone having a terminal alkyl group with an enzyme or microorganism capable of catalyzing the selective hydroxylation of said alkyl group to a hydroxyalkyl group, and effecting said hydroxylation.Type: GrantFiled: March 23, 2004Date of Patent: July 17, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Wenying Li, James A. Matson, Xiaohua Huang, Kin Sing Lam, Grace A. McClure
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Patent number: 7241899Abstract: The present invention relates to improved methods for the production, isolation and purification of epothilone B. These methods include, for example, a fermentation process for the production of epothilone B, isolation via adsorption onto a resin, and subsequent purification.Type: GrantFiled: March 22, 2004Date of Patent: July 10, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Daniel A. Benigni, Jack Z. Gougoutas, John D. DiMarco
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Patent number: 7241801Abstract: A compound, represented by formula (I): wherein A, B, R1, R2, R3, R5, R6, R7, R9, and R10 are as defined herein, or an enantiomer, diastereoisomer or tautomer thereof, including a salt, ester or derivative thereof, as an inhibitor of HCV NS5B polymerase.Type: GrantFiled: July 15, 2005Date of Patent: July 10, 2007Assignee: Boehringer Ingelheim International GmbHInventors: Pierre Beaulieu, Christian Brochu, Stephen Kawai, Jean Rancourt, Timothy A. Stammers, Bounkham Thavonekham, Youla S. Tsantrizos
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Patent number: 7241901Abstract: The present invention provides a process for preparing thiazole derivatives of formula (XI), that activate the delta subtype of the human Peroxisome Proliferator Activated Receptor (hPPAR?), and also provides processes for compounds of formula (VI), (VII), (VIII) and (IX), intermediate compounds for preparation of the above compounds of formula (XI).Type: GrantFiled: May 1, 2003Date of Patent: July 10, 2007Inventors: Heonjoong Kang, Jungyeob Ham
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Patent number: 7235690Abstract: The present invention is related to anthranilamides of formula I, in which R(1) to R(7) have the meanings indicated herein, a process for their preparation, their use as medicaments, and pharmaceutical preparations containing them. The compounds act on the Kv1.5 potassium channel and inhibit a potassium current which is referred to as the ultra-rapidly activating delayed rectifier in the atrium of the human heart. The compounds are therefore suitable for use as novel antiarrhythmic agents for the treatment and prophylaxis of atrial arrhythmias (e.g., atrial fibrillation (AF) or atrial flutter).Type: GrantFiled: April 26, 2002Date of Patent: June 26, 2007Assignee: Sanofi-Aventis Deutschland GmbHInventors: Joachim Brendel, Bernard Pirard, Stefan Peukert, Heinz-Werner Kleemann, Horst Hemmerle
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Patent number: 7229998Abstract: The present invention provides a compound of formula (I): wherein R1–R5, R25, R26, Y and X2 are as defined herein. The compounds activate human peroxisome proliferator activated receptors (hPPARs) and are useful for the treatment of associated disorders such as cardiovascular disease and hypercholesteremia.Type: GrantFiled: October 17, 2006Date of Patent: June 12, 2007Assignee: SmithKline Beecham CorporationInventors: Rodolfo Cadilla, Millard Hurst Lambert, III, Stephen William Rafferty, Daniel David Sternbach
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Patent number: 7220752Abstract: This invention relates to novel compounds that are liver selective glucocorticoid receptor antagonists, to methods of preparing such compounds, and to methods for using such compounds in therapy and in the regulation of metabolism, especially lowering blood glucose levels. The compounds referred to are compounds according to the formula 1: wherein the variables are as defined herein.Type: GrantFiled: November 28, 2001Date of Patent: May 22, 2007Assignees: Karo Bio AB, Abbott LaboratoriesInventors: Benjamin Pelcman, Annika Gustafsson, Philip R. Kym
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Patent number: 7217832Abstract: The present invention relates to a 5-amidino-2-hydroxybenzenesulfonamide derivative represented by the general formula: wherein R1 is a hydrogen atom or an optionally substituted lower alkyl group; R2 is a di(lower alkyl)amino group, a lower alkyl group, a cycloalkyl group, an optionally substituted aryl group, an optionally substituted heterocycloalkyl group, or an optionally substituted aromatic heterocyclic group; T is an oxygen atom, a sulfur atom, a sulfonyl group etc.; Q is a hydrogen atom or an optionally substituted lower alkyl group; and Z is a hydrogen atom, a hydroxy group etc., or a pharmaceutically acceptable salt thereof, which exert a potent and selective activated blood coagulation factor X inhibitory activity and is useful as an agent for the prevention or treatment of a disease occurred associating an activated blood coagulation factor X, a pharmaceutical composition comprising the same, a pharmaceutical use thereof and an intermediate thereof.Type: GrantFiled: February 23, 2006Date of Patent: May 15, 2007Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Kosuke Okazaki, Masahiko Uchida, Harunobu Mukaiyama, Hiroaki Kobayashi, Yuichiro Kai, Hideki Takeuchi, Kenji Yokoyama, Yoshihiro Terao, Yuji Hoyano, Hiroaki Shiohara, Norihiko Kikuchi
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Patent number: 7214678Abstract: According to the invention there is provided a compound the formula I; wherein A, X, B, R1, R2, R3 and R4 are as defined in the specification.Type: GrantFiled: June 1, 2006Date of Patent: May 8, 2007Assignee: Allergan, Inc.Inventors: Robert M. Burk, Sophie Beauchemin
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Patent number: 7214802Abstract: Disclosed compounds of formula (I) which inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease. Also disclosed are processes for preparing these compounds and pharmaceutical compositions comprising these compounds.Type: GrantFiled: March 7, 2005Date of Patent: May 8, 2007Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Derek Cogan, Ming-Hong Hao, Victor Marc Kamhi, Craig Andrew Miller, Matthew Russell Netherton, Alan David Swinamer
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Patent number: 7211668Abstract: This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: wherein E is sulfur or oxygen; J is nitrogen or C—R?; R1, R? is independently H, halogen, alkyl, nitro, nitrile, alkoxy, halogenated alkyl, halogenated alkoxy or a functional group having one of following general formulae: wherein A1, A2, A3, A4, A5, is independently selected from H, halogen such as F, Cl, Br or I, CF3, alkyl, preferably C1–C4 alkyl, nitro, nitrile, alkoxy, preferably C1–C4 alkoxy, halogenated (such as F, Cl, Br and I) alkyl, preferably halogenated C1–C4 alkyl, halogenated (such as F, Cl, Br and I) alkoxy, preferably halogenated C1–C4 alkoxy, phenyl, and halogenated (such as F, Cl, Br and I phenyl; R2 is H or protected or unprotected side chain of natural or unnatural ?-amino acid; and B is a natural or unnatural nucleobase, wherein when said nucType: GrantFiled: April 6, 2004Date of Patent: May 1, 2007Assignee: Panagene, Inc.Inventors: Sung Kee Kim, Hyunil Lee, Jong Chan Lim, Sung Hee Lee
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Patent number: 7211593Abstract: The present invention relates to compounds useful in the treatment of cancer or other proliferative diseases represented by the formula wherein: R1, R2, R3, R4, R5 are hydrogen or lower alkyl; R6 is selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, cycloalkyl, or heterocyclo; X is hydrogen and Y is hydroxy, or X and Y taken together represent a carbon-carbon bond; and pharmaceutically acceptable salts, solvates, or hydrates thereof. Also included are therapeutic compositions containing the compounds represented by formula I as active ingredients, alone or in combination with other therapeutic agents useful in the treatment of cancer or other proliferative diseases.Type: GrantFiled: March 11, 2003Date of Patent: May 1, 2007Assignee: Bristol-Myers Squibb Co.Inventors: Gregory D. Vite, Alicia Regueiro-Ren