The Other Cyclo In The Bicyclo Ring System Is A Pyridine Ring (including Hydrogenated) (e.g., Pyrido[2,3-d]pyrimidine, Etc.) Patents (Class 514/264.1)
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Publication number: 20120015952Abstract: The invention relates to compounds of formulae (1) and (2): and pharmaceutically acceptable salts thereof for the treatment of cancer, inflammation, auto-immune diseases, diabetes and diabetic complications, infection, cardiovascular disease and ischemia-reperfusion injuries.Type: ApplicationFiled: March 25, 2010Publication date: January 19, 2012Applicant: Profectus Biosciences, Inc.Inventors: Jie Zhang, Drago Robert Sliskovic, Charles E. Ducker
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Publication number: 20120015905Abstract: The present disclosure relates to compounds, which are useful for regulating the expression of apolipoprotein A-I (ApoA-I), and their use for treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for example, atherosclerosis.Type: ApplicationFiled: September 23, 2011Publication date: January 19, 2012Inventor: Henrik C. Hansen
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Patent number: 8097620Abstract: Compounds of Formula I are useful inhibitors of HIF prolyl hydroxylases. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.Type: GrantFiled: May 2, 2008Date of Patent: January 17, 2012Assignee: Amgen Inc.Inventors: Jennifer R. Allen, Kaustav Biswas, Roland Burli, Jennifer E. Golden, Stephanie Mercede, Christopher M. Tegley
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Publication number: 20120009144Abstract: Compounds having the formula I wherein R1, R2, R3 and X are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.Type: ApplicationFiled: July 6, 2011Publication date: January 12, 2012Applicant: Roche Palo Alto LLCInventors: Ryan Craig Schoenfeld, Francisco Xavier Talamas, Leanna Renee Staben
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Publication number: 20120010127Abstract: In part, the present invention is directed to compositions comprising a FabI inhibitor and at least one other bioactive agent. In another part, the present invention is directed to antibacterial compositions comprising a compound of formulas I-III and at least one other antibacterial agent.Type: ApplicationFiled: December 8, 2010Publication date: January 12, 2012Inventors: JUDD M. BERMAN, MOLLY B. SCHMID, JOHN D. MENDLEIN, NACHUM KAPLAN
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Patent number: 8071592Abstract: Bicyclic nitrogen containing compounds and their use as antibacterials.Type: GrantFiled: July 18, 2007Date of Patent: December 6, 2011Assignee: Glaxo Group LimitedInventors: Lluis Ballell, David Barros, Gerald Brooks, Julia Castro Pichel, Steven Dabbs, Robert A Daines, David Thomas Davies, Jose Maria Fiandor Roman, Israil Pendrak, Modesto J Remuiñan Blanco, Jason Anthony Rossi, Ilaria Giordano, Alan Joseph Hennessy, James B Hoffman, Graham Elgin Jones, Timothy James Miles, Neil David Pearson, Lihua(lily) Zhang
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Publication number: 20110294807Abstract: Disclosed are novel compounds that are useful for regulating the expression of apolipoprotein A-I (ApoA-I), and their use for the treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for example, atherosclerosis. Also disclosed are pharmaceutical compositions comprising the novel compounds.Type: ApplicationFiled: January 8, 2010Publication date: December 1, 2011Inventor: Henrik C. Hansen
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Publication number: 20110288090Abstract: The instant invention provides for compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.Type: ApplicationFiled: January 25, 2010Publication date: November 24, 2011Inventors: Donna J. Armstrong, Yasuhiro Goto, Takashi Hashihayata, Tetsuya Kato, Michael J. Kelly, III, Mark E. Layton, Craig W. Lindsley, Yoshio Ogino, Yu Onozaki, Kenvin J. Rodzinak, Michael A. Rossi, Philip E. Sanderson, Jiabing Wang, Melissa M. Yaroschak
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Publication number: 20110281874Abstract: Provided are compounds that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.Type: ApplicationFiled: July 27, 2011Publication date: November 17, 2011Applicant: ARRAY BIOPHARMA INC.Inventors: Thomas D. AICHER, Steven Armen BOYD, Mark Joseph CHICARELLI, Kevin Ronald CONDROSKI, Ronald Jay HINKLIN, Ajay SINGH
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Patent number: 8058282Abstract: Novel substituted 2,4,8-trisubstituted-8H-pyrido[2,3-d]pyrimidin-7-one compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors.Type: GrantFiled: August 19, 2010Date of Patent: November 15, 2011Assignee: GlaxoSmithKline LLCInventors: Jerry L. Adams, Jeffrey C. Boehm, Ralph Hall, Qi Jin, Jiri Kasparec, Domingos J. Silva, John J. Taggart
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Publication number: 20110275647Abstract: The present invention relates to a compound represented by a formula (I): or a pharmaceutically acceptable salt thereof, wherein R1 represents lower alkyl or the like; R2 represents phenyl or the like; R represents a halogen atom or the like; X represents an oxygen atom or the like; Y1, Y2, Y3 and Y4 represent CH or the like; l represents an integer of from 0 to 3; m and n each represent an integer of 1 or 2; p represents an integer of from 0 to 2; and q represents an integer of from 1 to 3.Type: ApplicationFiled: February 22, 2010Publication date: November 10, 2011Applicant: MSD K.K.Inventors: Keisuke Arakawa, Yoshiki Ito, Hiroshi Kawamoto, Junichi Sakaki, Tadashi Shimamura
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Publication number: 20110269779Abstract: The present invention provides chemical entities or compounds and pharmaceutical compositions thereof that are capable of modulating signal transduction by certain protein kinases such as mTor, tyrosine kinases, and/or lipid kinases such as PB kinase in an ocular tissue. Also provided in the present invention are methods of using these compositions to modulate activities of one or more of these kinases, especially for therapeutic applications.Type: ApplicationFiled: November 17, 2009Publication date: November 3, 2011Applicant: INTELLIKINE, INC.Inventors: Troy Edward Wilson, Christian Rommel, Yi Liu, Pingda Ren
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Publication number: 20110263619Abstract: The present invention relates to use of an inhibitor of the renin-angiotensin system (RAS) or a pharmaceutically acceptable derivative thereof, such as ramipril or ramiprilat, in the prevention of stroke, diabetes and/or congestive heart failure (CHF).Type: ApplicationFiled: December 1, 2010Publication date: October 27, 2011Inventors: Bernward Schölkens, Norbert Bender, Badrudin Rangoonwala, Gilles Dagenais, Hertzel Gerstein, Anders Ljunggren, Salim Yusuf
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Publication number: 20110257151Abstract: A compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R1 to R5 have the significance given in claim 1, can be used as a medicament.Type: ApplicationFiled: April 7, 2011Publication date: October 20, 2011Inventors: Li Chen, Lichun Feng, Mengwei Huang, Yongfu Liu, Guolong Wu, Jim Zhen Wu, Mingwei Zhou
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Patent number: 8039505Abstract: Disclosed are compounds and compositions that modulate T-cells. Such compounds can be used to treat T-cell mediated disease like T-ALL, rheumatoid arthritis, multiple sclerosis, and graft-vs-host disease (GvHD), to name but a few. The compounds have a general structure as shown in Formula I. Ar1-L-Ar2??I wherein Ar1 and Ar2, are independent of one another, a substituted aryl, unsubstituted aryl, substituted heteroaryl, or unsubstituted heteroaryl; and L is a bond or a linker spanning two, three, four, or five atoms.Type: GrantFiled: April 11, 2008Date of Patent: October 18, 2011Assignee: University of Utah Research FoundationInventor: Nikolaus S. Trede
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Publication number: 20110245209Abstract: The present invention relates to Pyridopyrimidine Derivatives of formula (I), compositions comprising a Pyridopyrimidine Derivative and methods for using the Pyridopyrimidine Derivatives for treating or preventing a metabolic disorder, dyslipidemia, a cardiovascular disease, a neurological disorder, a hematological disease, cancer, inflammation, a respiratory disease, a gastroenterological disease, diabetes, a diabetic complication, obesity, an obesity-related disorder or non-alcoholic fatty liver disease.Type: ApplicationFiled: December 15, 2009Publication date: October 6, 2011Inventors: Dong Xiao, Anandan Palani, Michael J. Sofolarides, Robert G. Aslanian
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Publication number: 20110245172Abstract: The present invention relates to biocompatible oligomer-polymer compositions for the in situ formation of implants, wherein the implants release a bioactive agent, a metabolite, or a prodrug thereof, at a controlled rate. The sustained release delivery system includes a flowable composition containing a bioactive agent, a metabolite, or a prodrug thereof, and an implant containing a bioactive agent, a metabolite, or a prodrug thereof. The flowable composition may be injected into tissue whereupon it coagulates to become the solid or gel, monolithic implant. The flowable composition includes a biodegradable, thermoplastic polymer, a biocompatible end-capped oligomeric liquid, and a bioactive agent, a metabolite, or a prodrug thereof.Type: ApplicationFiled: June 3, 2009Publication date: October 6, 2011Applicant: Tolmar Therapeutics, Inc.Inventor: Richard L. Norton
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Patent number: 8030317Abstract: Compounds of the following formula are provided for use with MEK: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: GrantFiled: December 18, 2007Date of Patent: October 4, 2011Assignee: Takeda Pharmaceutical Company LimitedInventors: Qing Dong, Stephen W. Kaldor
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Patent number: 8022077Abstract: The present invention relates to the use of pyrido[2,3-d]pyrimidines of formula (I) wherein L, R1, R2 and R3 have specific meaning. The present invention also relates to the use of the compounds of formula (I) as inhibitors of HCV replication as well as their use in pharmaceutical compositions aimed to treat or combat HCV infections. In addition, the present invention relates to compounds of formula (I) per se and their use as medicines. The present invention also concerns processes for the preparation of such compounds, pharmaceutical compositions comprising them, and combinations of said compounds with other anti-HCV agents.Type: GrantFiled: May 12, 2006Date of Patent: September 20, 2011Assignee: Tibotec Pharmaceuticals Ltd.Inventors: Kenneth Alan Simmen, Dominique Louis Nestor Ghislain Surleraux, Tse-I Lin, Oliver Lenz, Pierre Jean-Marie Bernard Raboisson
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Publication number: 20110224221Abstract: Methods for reducing or preventing the effects of ionizing radiation in healthy cells arc provided. The methods relate to the use of selective cyclin-dependent kinase (CDK) 4/6 inhibitors to induce transient quiescence in CDK4/6 dependent cells, such as hematopoietic stem cells and/or hematopoietic progenitor cells. Radioprotection can be effected in mammals by treatment with selective CDK4/6 inhibitor compounds either before, at the same time as, or after exposure to the ionizing radiation.Type: ApplicationFiled: October 1, 2009Publication date: September 15, 2011Inventors: Norman E. Sharpless, Chad D. Torrice, Matthew R. Ramsey, Soren Johnson, Jessica F. Bell
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Publication number: 20110217300Abstract: The present invention relates to quinazolinone compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising the quinazolinone compounds.Type: ApplicationFiled: April 6, 2011Publication date: September 8, 2011Applicant: ARQULE, INC.Inventors: Jifeng Liu, Syed M. Ali, Mark A. Ashwell, Ping Ye, Yousheng Guan, Shi-Chung Ng, Rocio Palma, Dan Yohannes
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Publication number: 20110207741Abstract: Provided herein are methods of treating a medical condition in which RAS activation is increased. The method comprises the step of administering to a subject a c-Src inhibitor in an amount effective to treat the medical condition. The invention also provides a method of treating or preventing a cardiac arrhythmia. The method comprises the step of administering to the subject a c-Src inhibitor in an amount effective to treat or prevent the cardiac arrhythmia. The invention additionally provides a method of delaying the onset of sudden cardiac death. The method comprises the step of administering to the subject a c-Src inhibitor in an amount effective to delay the onset of SCD. Methods of augmenting gap junction function and methods of increasing Connexin 43 levels in a subject in need thereof are further provided.Type: ApplicationFiled: February 22, 2011Publication date: August 25, 2011Applicant: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOISInventor: Samuel Dudley
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Patent number: 8003657Abstract: The present invention relates to heterocyclic substituted bisarylurea derivatives of formula I, the use of the compounds of formula I as inhibitors of one or more kinases, the use of the compounds of formula I for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient.Type: GrantFiled: October 6, 2005Date of Patent: August 23, 2011Assignee: Merck Patent GmbHInventors: Frank Stieber, Alfred Jonczyk, Guenter Hoelzemann, Hans-Peter Buchstaller, Lars Thore Burgdorf, Wilfried Rautenberg, Hartmut Greiner
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Patent number: 8003656Abstract: 2-Phenoxy pyrimidinone analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.Type: GrantFiled: August 22, 2007Date of Patent: August 23, 2011Assignee: Neurogen CorporationInventors: Rajagopal Bakthavatchalam, Scott M. Capitosti, Jianjun Xu, Bertrand L. Chenard, Manuka Ghosh, Charles A. Blum
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Publication number: 20110201628Abstract: The present invention relates to compounds of Formula (I) and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds provide a treatment for myeloproliferative disorders and cancer.Type: ApplicationFiled: September 29, 2009Publication date: August 18, 2011Inventors: Claudio Edmundo Chuaqui, Shan Huang, Stephanos Ioannidis, Jie Shi, Mei Su, Qibin Su
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Publication number: 20110195954Abstract: The present invention relates to new CGRP-antagonists of general formula I wherein U, V, X, Y, R1, R2, R3 and R4 are defined as mentioned in the description, the tautomers thereof, the isomers thereof, the diastereomers thereof, the enantiomers thereof, the hydrates thereof, the mixtures thereof and the salts thereof as well as the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, medicaments containing these compounds, the use thereof and processes for the preparation thereof.Type: ApplicationFiled: November 21, 2008Publication date: August 11, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Dirk Gottschling, Georg Dahmann, Henri Doods, Annekatrin Heimann, Stephan Georg Mueller, Klaus Rudolf, Gerhard Georg Schaenzle, Dirk Stenkamp
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Publication number: 20110190283Abstract: Compounds of the Formula (I) are disclosed which are Fab I inhibitors and are useful in the treatment of bacterial infections.Type: ApplicationFiled: July 6, 2010Publication date: August 4, 2011Inventors: William H. Miller, Kenneth A. Newlander, Mark A. Seefeld, Irene N. Uzinskas, Walter E. DeWolf, JR., Dalia R. Jakas
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Publication number: 20110190292Abstract: A compound of Formula (I) and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I, and methods of treating conditions associated with the activity of p38 kinase.Type: ApplicationFiled: April 12, 2011Publication date: August 4, 2011Inventors: T. G. Murali Dhar, Stephen T. Wrobleski
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Publication number: 20110165118Abstract: The present invention relates to 3-Heterocyclic Substituted Indole Derivatives, compositions comprising at least one 3-Heterocyclic Substituted Indole Derivative, and methods of using the 3-Heterocyclic Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: ApplicationFiled: November 13, 2008Publication date: July 7, 2011Inventors: Tin-Yau Chan, Jose S. Duca, Liwu Hong, Charles A. Lesburg, Brian A. McKittrick, Haiyan Pu, Li Wang, Henry M. Vaccaro
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Patent number: 7968557Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the FAK, Abl, BCR-Abl, PDGF-R, c-Kit, NPM-ALK, Flt-3, JAK2 and c-Met kinases.Type: GrantFiled: February 14, 2005Date of Patent: June 28, 2011Assignee: Novartis AGInventors: Ha-Soon Choi, Zhicheng Wang, Nathanael Schiander Gray, Xiang-ju Gu, Xiaohui He, Yun He, Tao Jiang, Yi Liu, Wendy Richmond, Taebo Sim, Kunyong Yang
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Publication number: 20110152243Abstract: The invention provides a compound of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.Type: ApplicationFiled: December 21, 2010Publication date: June 23, 2011Applicant: ABBOTT LABORATORIESInventors: Neil Wishart, Theresa Dunstan, Jeremy J. Edmunds, Anna M. Ericsson, Catherine R. Ferenz, Adrian D. Hobson, David C. Ihle, Kent D. Stewart, Lei Wang, Lu Wang
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Publication number: 20110136783Abstract: Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. These novel compounds have the structure: or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein n1, n2, n3, n4, A, B, D, E, G, Y, Z, R1 and R2 are defined herein.Type: ApplicationFiled: February 8, 2011Publication date: June 9, 2011Inventors: John M. Fevig, Dean A. Wacker
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Patent number: 7947690Abstract: The present invention provides a condensed pyrimidine compound represented by formula (I) or pharmaceutically acceptable salt thereof: where A represents a ring where at least one carbon atom within said ring is optionally substituted with one or more groups selected from the group consisting of lower alkyl, —O-(lower alkyl), halogen atom, carboxyl, —CO2-(lower alkyl), and carbamoyl, R1 represents: (1) phenyl substituted with at least three halogen atoms, which may have at least one additional substituent, or (2) cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl, each of which is optionally substituted; and R2 represents a group represented by formula (II) or an optionally substituted cyclic amino: wherein R21 and R22 may be identical or different and each represents —H, lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, phenyl, heteroaryl, non-aromatic heterocyclyl, or —O-(lower alkyl), each of which is optionally substituted.Type: GrantFiled: October 17, 2005Date of Patent: May 24, 2011Assignee: Astellas Pharma Inc.Inventors: Yasuhiro Yonetoku, Kenji Negoro, Kenichi Onda, Masahiko Hayakawa, Daisuke Sasuga, Takahiro Nigawara, Kazuhiko Iikubo, Hiroyuki Moritomo, Shigeru Yoshida, Takahide Ohishi
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Publication number: 20110118287Abstract: Bicycloheteroaryl compounds are disclosed that have formula (I). The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.Type: ApplicationFiled: March 16, 2007Publication date: May 19, 2011Applicant: RENOVIS, INC.Inventors: Michael G. Kelly, John Kincaid, Yunfeng Fang, Jianhua He, Yeyu Cao, Carl Kaub, Sumithra Gowlugari
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Publication number: 20110118271Abstract: The present invention relates to novel kinase inhibitors and modulator compounds useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferrably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.Type: ApplicationFiled: January 26, 2011Publication date: May 19, 2011Inventors: Daniel L. FLYNN, Peter A. PETILLO, Michael D. KAUFMAN, William C. PATT
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Publication number: 20110118288Abstract: The present invention provides a pharmaceutical composition comprising the following active ingredients: 1) an angiotensin II receptor antagonist or a pharmaceutically acceptable salt thereof, 2) pioglitazone or a pharmaceutically acceptable salt thereof; and 3) rosuvastatin or a pharmaceutically acceptable salt thereof. The present invention also provides use of the pharmaceutical composition in preparing a medicament for treating hypertension or metabolic syndrome. The pharmaceutical composition of the present invention can treat hypertension or metabolic syndrome, while effectively controlling the incidence of associated cardiovascular diseases and more potently improving survival prognosis in hypertensive patients. When blood pressure is lowered to desired level, the risk factors such as cardiovascular diseases are rectified, metabolic disorders and prognosis of patients are improved, and survival rate of hypertensive patients is raised.Type: ApplicationFiled: July 23, 2009Publication date: May 19, 2011Inventor: Zhiquan Zhao
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Patent number: 7939538Abstract: Compounds are provided having the formula: wherein variables Ra, R1, R2, R3, R4, A1, A4, L, Q, X and subscript n as described herein. The subject compounds are useful for treatment of inflammatory and immune conditions and diseases. Compositions and methods of treatment using the subject compounds are also provided. For example, the subject methods are useful for treatment of inflammatory and immune disorders and disease such as multiple sclerosis, rheumatoid arthritis, psoriasis, and inflammatory bowel disease.Type: GrantFiled: June 27, 2005Date of Patent: May 10, 2011Assignee: Amgen Inc.Inventors: Zice Fu, Michael G. Johnson, An-Rong Li, Andrew P. Marcus, Julio C. Medina, Philippe Bergeron, Xiaoqi Chen, Xiaohui Du, Jeffrey Deignan, Jason A. Duquette, Darin Gustin, Jeffrey T. Mihalic, Jiwen Liu
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Publication number: 20110105539Abstract: A process for obtaining 2?-halo-4-methylbiphenyls is described, which comprises reacting 4 halotoluene with a 1,2-dihalobenzene in the presence of elemental metal such as magnesium, lithium or zinc, wherein 0 to 0.9 molar, particularly 0 to 0.2 molar excess of 4-halotoluene in regard to 1,2-dihalobenzene is used, and arised organometal intermediates are quenched by elemental mental halogen. In addition, the coupling of arised 2?-halo-4-methylbiphenyls with 2-(1-propyl)-4-methyl-6-(1?-methylbenzimidazole-2-il)benzimidazole to afford 3?-(2?-halo-biphenyl-4-ylmethyl)-1,7?-dimethyl-2?-propyl-1H,3?H-[2,5?]bibenzoimidazolyl, which can be further converted to organometallic compound and said organometallic compound is further reacted with formic acid derivative, such as N,N-dimethylformamide, alkylformiate or carbon dioxide to obtain telmisartan, is also described.Type: ApplicationFiled: March 19, 2009Publication date: May 5, 2011Applicant: LEK Pharmaceuticals D.D.Inventors: Anton Copar, Zdenko Casar, Andrej Premrl
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Publication number: 20110098277Abstract: Compounds are disclosed which are Fab I inhibitors and are useful in the treatment bacterial infections.Type: ApplicationFiled: April 12, 2010Publication date: April 28, 2011Inventors: Walter J. Burgess, Dalia Jakas, William F. Huffman, William H. Miller, Kenneth A. Newlander, Mark A. Seefeld, Irene N. Uzinskas
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Patent number: 7928112Abstract: The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: August 27, 2010Date of Patent: April 19, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Tesfaye Biftu, Ping Chen, Danqing Feng, Ann E. Weber
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Publication number: 20110071148Abstract: The compounds according to formula VIII, their pharmaceutically acceptable acid or base addition salts, and the uses thereof is disclosed. These compounds and their pharmaceutically acceptable acid or base addition salts can be used for the preparing a medicament for modulating estrogen related receptor (ERR), and treating metabolic diseases, such as high blood fat, fatty liver, hyperglycemia, diabetes, obesity, etc. The definition of the groups of the formula is defined as the description.Type: ApplicationFiled: September 10, 2010Publication date: March 24, 2011Applicant: Guangzhou Institute of Biomedicine and Health, Chinese Academy of SciencesInventors: Ke Ding, Chiwai Wong, Zhanfang Kang, Xi Zhou
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Patent number: 7910595Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) or other viruses are disclosed. This invention is also directed to compositions comprising such compounds, co-formulation or co-administration of such compounds with other anti-viral or therapeutic agents, processes and intermediates for the syntheses of such compounds, and methods of using such compounds for the treatment of HCV or other viral infections.Type: GrantFiled: December 20, 2006Date of Patent: March 22, 2011Assignee: Abbott LaboratoriesInventors: David A. Betebenner, David A. DeGoey, Clarence J. Maring, Allan C. Krueger, Nobuhiko Iwasaki, Todd W. Rockway, Curt S. Cooper, David D. Anderson, Pamela L. Donner, Brian E. Green, Dale J. Kempf, Dachun Liu, Keith F. McDaniel, Darold L. Madigan, Christopher E. Motter, John K. Pratt, Jason P. Shanley, Michael D. Tufano, Rolf Wagner, Rong Zhang, Akhteruzzaman Molla, Hongmei Mo, Tami J. Pilot-Matias, Sherie V L. Masse, Robert J. Carrick, Wenping He, Liangjun Lu, David J. Grampovnik
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Publication number: 20110065676Abstract: The present invention is directed to a pharmaceutical composition comprising an effective amount of at least one PAR1 antagonist, at least one NAR agonist, optionally, an effective amount of at least one cardiovascular agent, and, optionally, a pharmaceutically acceptable carrier. The present invention also provides for the use of theses pharmaceutical compositions to treat various diseases associated with thrombosis.Type: ApplicationFiled: June 22, 2010Publication date: March 17, 2011Applicant: Schering CorporationInventors: Michael Sidney Perelman, Madhu Chintala
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Publication number: 20110065671Abstract: The present invention relates to Bicyclic Heterocycle Derivatives of formula (I), compositions comprising a Bi-cyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR1 19 in a patient.Type: ApplicationFiled: May 18, 2009Publication date: March 17, 2011Inventors: Joel M. Harris, Santhosh Francis, Bernard R. Neustadt, Craig D. Boyle, Hong Liu, Jinsong Hao, Andrew Starnford, Samuel Chackalamannil, William J. Greenlee
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Publication number: 20110065733Abstract: Compounds of the following formula are provided for use with MEK: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: October 7, 2010Publication date: March 17, 2011Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Qing Dong, Stephen W. Kaldor
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Patent number: 7906520Abstract: The present invention features methods and compositions for preventing, reducing, or treating a traumatic, metabolic or toxic peripheral nerve lesion or pain including, for example, neuropathic pain, inflammatory and nociceptive pain by administering to a mammal in need thereof a compound that reduces the expression or activity of BH4. According to this invention, this reduction may be achieved by reducing the enzyme activity of any of the BH4 synthetic enzymes, such as GTP cyclohydrolase (GTPCH), sepiapterin reductase (SPR), or dihydropteridine reductase (DHPR); by antagonizing the cofactor function of BH4 on BH4-dependent enzymes; or by blocking BH4 binding to membrane bound receptors. The compounds of the invention may be administered alone or in combination with a second therapeutic agent.Type: GrantFiled: November 12, 2004Date of Patent: March 15, 2011Assignee: The General Hospital CorporationInventors: Clifford J. Woolf, Michael Costigan, Robert Griffin, Irmgard Tegeder
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Publication number: 20110059976Abstract: The present invention provides compounds having the formula: wherein A-B together represent one of the following structures: and n, R1, R2, R3, R4, L1, L2, Y and Z are as defined in classes and subclasses herein, and pharmaceutical compositions thereof, as described generally and in subclasses herein, which compounds are useful as inhibitors of protein kinase (e.g., RAF), and thus are useful, for example, for the treatment of RAF mediated diseases.Type: ApplicationFiled: July 26, 2010Publication date: March 10, 2011Inventors: Johan D. Oslob, Jiang Zhu, Kenneth Barr, Jennifer Cossrow, Brian Raimundo, Hiroko Tanaka
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Patent number: 7901708Abstract: The present invention provides apparatus and processes for producing liposomes. By providing a buffer solution in a first reservoir, and a lipid solution in a second reservoir, continuously diluting the lipid solution with the buffer solution in a mixing chamber produces a liposome. The lipid solution preferably comprises an organic solvent, such as a lower alkanol.Type: GrantFiled: June 30, 2003Date of Patent: March 8, 2011Assignee: Protiva Biotherapeutics, Inc.Inventors: Ian MacLachlan, Lloyd Brian Jeffs, Lorne R. Palmer, Cory Giesbrecht, Noelle Giesbrecht, legal representative
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Publication number: 20110052562Abstract: Compounds useful as Rho kinase inhibitors according to formula IA or IB: wherein A, B, D, E, R1, R2 and Ar1 are as defined herein, and any tautomer, salt, stereoisomer, hydrate, solvent, or prodrug thereof, pharmaceutical compositions, methods of treatment, and synthetic methods are provided.Type: ApplicationFiled: December 18, 2008Publication date: March 3, 2011Applicant: The Scripps Research InstituteInventors: Yangbo Feng, Philip LoGrasso, Thomas Bannister, Thomas Schroeter, Hampton Sessions, Lei Yao, Bo Wang, Michael P. Smolinski, Yen Ting Chen, Yan Yin, Bozena Frackowiak-Wojtasek, Sarwat Chowdhury
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Publication number: 20110053920Abstract: The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions that include substituted heterobicyclic pyrimidines of Formula (I): wherein R1, R2, R3, R4, R5, X, W, and ring A are as defined herein; pharmaceutical compositions of substituted heterobicyclic pyrimidines of Formula (I); and their use in the treatment of chronic neurodegenerative diseases, neurotraumatic diseases, depression and/or diabetes. More particularly, the present invention relates to substituted pyrazolopyrimidines of Formula (I).Type: ApplicationFiled: November 4, 2010Publication date: March 3, 2011Applicant: CEPHALON, INC.Inventors: Edward R. Bacon, Thomas Bailey, Nadine C. Becknell, Diane E. Gingrich, Greg Hostetler, Robert L. Hudkins, Keith S. Learn, Jason C. Wagner