Three Ring Nitrogens In The Bicyclo Ring System Patents (Class 546/118)
-
Publication number: 20110240977Abstract: A heterocyclic compound of formula 1 and an organic light-emitting device including an organic layer containing the heterocyclic compound. The heterocyclic compound of Formula 1 may be suitable as a material for an emission layer, an electron transport layer or an electron injection layer of an organic light-emitting device. Due to the inclusion of the heterocylic group in its molecular structure, the heterocyclic compound of Formula 1 may have a high glass transition temperature (Tg) or a high melting point, and may prevent crystallization. An organic light-emitting device manufactured using the heterocyclic compound of Formula 1, which has a symmetrical structure in which a chrysene group and an indole group are fused, has excellent durability when stored or operated.Type: ApplicationFiled: March 31, 2011Publication date: October 6, 2011Applicant: SAMSUNG MOBILE DISPLAY CO., LTD.Inventors: Hye-Jin JUNG, Seok-Hwan HWANG, Young-Kook KIM, Yoon-Hyun KWAK, Jin-O LIM, Jong-Hyuk LEE
-
Patent number: 8030328Abstract: Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof wherein the variables A, n, R5, R21-R24 and Q are defined herein. These compounds bind VLA-4. Certain of these compound also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: GrantFiled: May 22, 2006Date of Patent: October 4, 2011Assignee: Elan Pharmaceuticals, Inc.Inventors: Frank Stappenbeck, Andrei Konradi, Jacek Jagodzinski, Christopher M. Semko, Ying-zi Xu, Jenifer L. Smith, Kassandra Rossiter
-
Patent number: 8030311Abstract: The invention relates to compounds of the formula (I) wherein the moieties R1, R2, R3, R9, R10 and Q and X, Y and Z are as defined in the specification, and salts thereof, as well as their use, methods of use for them and method of their synthesis, and the like. The compounds are protein kinase inhibitors and can, inter alia, be used in the treatment of various proliferative diseases.Type: GrantFiled: April 12, 2006Date of Patent: October 4, 2011Assignee: Novartis AGInventors: Guido Bold, Pascal Furet, Vito Guagnano, Clive McCarthy, Andrea Vaupel
-
Publication number: 20110237606Abstract: This invention describes the series of compounds based on the 3-deazaneplanocin A (DZNep) core structure designed to inhibit the function of Polycomb repressive complex 2 (PRC2) proteins.Type: ApplicationFiled: September 25, 2009Publication date: September 29, 2011Inventors: Christina L. L. Chai, Eric K.W. Tam, Haiyan Yang, Qiang Yu, Tuan Minh Nguyen
-
Patent number: 8026236Abstract: The present invention relates to 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives having the general Formula I to pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S related diseases such as atherosclerosis, obesity, inflammation and immune disorders, such as rheumatoid arthritis, psoriasis, cancer, and chronic pain, such as neuropathic pain.Type: GrantFiled: January 13, 2010Date of Patent: September 27, 2011Assignee: N.V. OrganonInventors: John Stephen Robinson, Philip Stephen Jones, Jiaqiang Cai, David Jonathan Bennett
-
Publication number: 20110230428Abstract: Certain chemical entities are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.Type: ApplicationFiled: July 22, 2009Publication date: September 22, 2011Inventors: John Wityak, Leticia M. Toledo-sherman, Celia Dominguez, Stephen Martin Courtney, Christopher John Yarnold, Paula C. De Aguiar Pena, Andreas Scheel, Dirk Winkler
-
Publication number: 20110224195Abstract: The present invention is directed to substituted six-membered heterocyclic compounds 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 obesity and diabetes, 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: ApplicationFiled: August 18, 2008Publication date: September 15, 2011Inventors: Tesfaye Biftu, Danqing Feng, Ann E. Weber, Jason M. Cox, Xiaoxia Qian, Jinyou Xu
-
Patent number: 8017605Abstract: Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: are inhibitors of p38 and are useful in the treatment of inflammation such as in the treatment of asthma, COPD, ARDS, rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis, gouty arthritis and other arthritic conditions; inflamed joints, eczema, psoriasis or other inflammatory skin conditions such as sunburn; inflammatory eye conditions including conjunctivitis; pyresis, pain and other conditions associated with inflammation.Type: GrantFiled: June 10, 2009Date of Patent: September 13, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Soumya P. Sahoo, Meng-Hsin Chen, Kevin D. Dykstra, Hiroo Koyama, Peter T. Meinke, Stephen J. O'Keefe, Ginger Xu-qiang Yang
-
Patent number: 8017780Abstract: The invention provides novel therapeutic compounds, pharmaceutical compositions comprising these compounds, and methods for using these compounds and compositions to treat diseases and disorders such as cancer.Type: GrantFiled: October 9, 2009Date of Patent: September 13, 2011Assignee: Myrexis, Inc.Inventors: Ashok Bajji, Se-Ho Kim, Rajendra Tangallapally
-
Publication number: 20110217290Abstract: Compositions and methods for the treatment of food allergies, particularly peanut allergy are provided. The compositions and methods are based on the observation that agents which interfere with the association of platelet activating fact (PAF) with its receptor (PAF-R) significantly reduce the severity and duration of anaphylaxis. Combination therapy with a PAF inhibitor and a histamine inhibitor provided an increased beneficial effect compared to treatment alone.Type: ApplicationFiled: August 18, 2009Publication date: September 8, 2011Inventors: Manel Jordana, Susan Waserman, Katherine Arias
-
Publication number: 20110218197Abstract: The present invention is directed to substituted aza-bicyclic imidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by TRP M8, including for example, inflammatory pain, inflammatory hyperalgesia, inflammatory hypersensitivity condition, neuropathic pain, neuropathic cold allodynia, inflammatory somatic hyperalgesia, inflammatory visceral hyperalgesia, cardiovascular disease aggravated by cold and pulmonary disease aggravated by cold.Type: ApplicationFiled: February 25, 2011Publication date: September 8, 2011Inventors: Mark R. PLAYER, Raul Calvo, Jinsheng Chen, Sanath Meegalla, Daniel Parks, William Parsons, Scott Ballentine, Shawn Branum
-
Publication number: 20110207750Abstract: This invention provides compounds of Formula I which are PAFR antagonists: I and the pharmaceutically acceptable salts thereof. The compounds are useful for treating PAF-mediated disorders, and can be used in methods for treating atherosclerosis and preventing or reducing risk for atherosclerotic disease events. The compounds are also useful for treating or ameliorating pain, e.g. inflammatory pain and/or nociceptive pain, and for treating or ameliorating autoimmune and/or inflammatory diseases, among other conditions.Type: ApplicationFiled: October 26, 2009Publication date: August 25, 2011Inventors: Lin Chu, Anthony Ogawa, Hyun O. Ok, Feroze Ujjainwalla
-
Publication number: 20110207746Abstract: The present invention relates to compounds of formula (I), and their pharmaceutically acceptable salts, solvates, hydrates, geometrical isomers, tautomers, optical isomers or N-oxides, which are inhibitors of SSAO activity. The invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the treatment of medical conditions wherein inhibition of SSAO activity is beneficial, such as inflammatory diseases and immune disorders.Type: ApplicationFiled: September 16, 2009Publication date: August 25, 2011Applicant: PROXIMAGEN LIMITEDInventors: Edward Daniel Savory, Michael Higginbottom, Kathryn Oliver, VietAnh Anne Horgan
-
Publication number: 20110201808Abstract: The invention relates to a compound which has affinity with amyloid, shows sufficiently rapid clearance from normal tissues and is suppressed in toxicity such as mutagenicity, and also relates to a low-toxic diagnostic agent for Alzheimer's disease containing the compound. The compound is represented by the following formula (1) or a salt thereof: wherein A1, A2, A3 and A4 independently represent a carbon or a nitrogen, and R3 is a group represented by the following formula: wherein R1 is a radioactive halogen substituent; m is an integer of 0 to 4; and n is an integer of 0 or 1, provided that at least one of A1, A2, A3 and A4 represents a carbon, and R3 binds to a carbon represented by A1, A2, A3 or A4.Type: ApplicationFiled: April 28, 2011Publication date: August 18, 2011Applicant: NIHON MEDI-PHYSICS CO., LTD.Inventors: Shigeyuki TANIFUJI, Daisaku NAKAMURA, Shinya TAKASAKI
-
Publication number: 20110201604Abstract: Substituted fused imidazole derivatives, methods of their preparation, pharmaceutical compositions comprising a substituted fused imidazole derivative, and methods of use in treating inflammation are provided. The substituted fused imidazole derivatives may control the activity or the amount or both the activity and the amount of heme-oxygenase.Type: ApplicationFiled: February 16, 2011Publication date: August 18, 2011Applicant: HIGH POINT PHARMACEUTICALS, LLCInventors: Adnan M. M. Mjalli, Dharma Rao Polisetti, Jareer Nabeel Kassis, Matthew J. Kostura, Mustafa Guzel, Otis Clinton Attucks, Robert Carl Andrews, Samuel Victory, Suparna Gupta
-
Publication number: 20110201640Abstract: Provided is a tricyclic compound having a PPAR ? agonist activity, which is represented by the general formula (I) wherein Z represents a single bond or the like, Y represents a hydrogen atom, lower alkyl optionally having substituent(s) or the like, X represents a hydrogen atom or the like, A represents aryl or the like, B and C are the same or different and each represents an aromatic carbocycle or the like, R4-R9 are the same or different and each represents hydrogen or the like, V represents a single bond or the like, R10 and R11 are the same or different and each represents hydrogen or the like, or a pharmaceutically acceptable salt thereof or the like:Type: ApplicationFiled: August 6, 2009Publication date: August 18, 2011Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Arata Yanagisawa, Keiji Uehara, Masahiro Matsubara, Kimihisa Ueno, Michihiko Suzuki, Takeshi Kuboyama, Keisuke Yamamoto, Tomohiro Tamura
-
Patent number: 7998976Abstract: Provided are certain chemical entities, and methods of use to modulate skeletal myosin, skeletal actin, skeletal tropomyosin, skeletal troponin C, skeletal troponin I, skeletal troponin T, and skeletal muscle, including fragments and isoforms thereof, as well as the skeletal sarcomere, and methods of use in the treatment of obesity, sarcopenia, wasting syndrome, frailty, cachexia, muscle spasm, post-surgical and post-traumatic muscle weakness, neuromuscular disease, and other indications.Type: GrantFiled: January 23, 2009Date of Patent: August 16, 2011Assignee: Cytokinetics, Inc.Inventors: Alex R. Muci, Gustave Bergnes, Bradley P. Morgan
-
Publication number: 20110195408Abstract: A labeling dye of the present invention includes a coloring portion comprising an organic EL-dye, a bonding portion to be bonded with a biomolecule and a spacer portion for linking the coloring portion and the bonding portion. The present invention provides a high incorporation ratio and also high fluorescence intensity in solid state.Type: ApplicationFiled: July 28, 2006Publication date: August 11, 2011Inventor: Shinichiro Isobe
-
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
-
Publication number: 20110190336Abstract: Compounds are provided having the general structure of formula I: In formula I, one member of the group (W, X, Y and Z) is a nitrogen atom and the remaining three members of the group are each independently a carbon atom covalently bonded to a radical, R4. The radicals, R1, R2, R3 and R4 are each defined herein, and n is an integer from 1 to 4. Also provided are stereoisomers, prodrugs, pharmaceutically acceptable salts, hydrates, salt hydrates, acid salt hydrates, and polymorphs of the compounds having the structure of formula I. The compounds bind the prostaglandin D2 receptor and are useful in the prophylaxis and treatment of prostaglandin D2-mediated diseases and conditions, including pain and inflammation, as well as asthma and allergic diseases and conditions.Type: ApplicationFiled: October 14, 2009Publication date: August 4, 2011Applicant: CARA THERAPEUTICS, INC.Inventors: Robert Zhiyong Luo, Mary-Margaret Zablocki
-
Patent number: 7989469Abstract: Provided are certain chemical entities, and methods of use to modulate skeletal myosin, skeletal actin, skeletal tropomyosin, skeletal troponin C, skeletal troponin I, skeletal troponin T, and skeletal muscle, including fragments and isoforms thereof, as well as the skeletal sarcomere, and methods of use in the treatment of neuromuscular disorders, conditions having muscle wasting, claudication, frailty, metabolic syndrome, muscle atrophy associated with disuse, and muscle fatigue, and other indications.Type: GrantFiled: February 2, 2009Date of Patent: August 2, 2011Assignee: Cytokinetics, IncorporatedInventors: Zhe Yang, Scott Collibee, Alex R. Muci, Jianchao Wang, Luke W. Ashcraft, Jeff Gardina, Brian Stoltz, Gustave Bergnes, Bradley P. Morgan
-
Publication number: 20110184015Abstract: Pyrroloindoles of formula (I) are provided wherein Het is an aromatic or partially unsaturated, monocyclic or bicyclic heterocycle containing between 1 and 4 heteroatoms N, O or S, optionally substituted by R1 or R?1 which are the same or different; R is X-(A-B)n-CONH2, X-(A-B)n-O—CONH2, X-(A-B)n-NH—CONH2, X—(CH2)m-heterocycloalkyl, X(CH2)m-aryl and X—(CH2)m-heteroaryl wherein X is —O—C(O), —NH—C(O), NH—CS, —NH—CO—CH2-O—; —NH—COCH2-S—CH2-CO—NH—; —NH—CO—(CH2)2-SO2-; and —NH—CO—CH2-N(CH3)-CO—; A and B are the same or different and are each independently a single bond, CH2, CH-alkyl, and CH-aralkyl; n=1,2 and m=0, 1; R1 and/or R?1 are H, halogen, CF3, nitro, cyano, alkyle, hydroxy, mercapto, amino, alkylamino, dialkylamino, alkoxy, alkylthio, and carboxy, free or esterified by an alkyl, carboxamide, CONH(alkyl), CON(alkyl)2, NH—CO-alkyl, sulfonamide, NH—SO2-alkyl, S(O)2-NHalkyl, and S(O2)-N(alkyl)2 group, all of said alkyl, alcoxy and alkylthio groups being optionally substituted themselves, said products beingType: ApplicationFiled: December 16, 2010Publication date: July 28, 2011Applicant: SANOFI-AVENTISInventors: Marcel Alasia, Hervé Minoux, Jean-Marie Ruxer
-
Publication number: 20110178057Abstract: Compounds represented by the formulas (I) (II) wherein each symbol is as defined in the specification, and a pro-drug thereof have a superior renin inhibitory activity, and are useful as agents for the prophylaxis or treatment of hypertension, various organ damages attributable to hypertension and the like.Type: ApplicationFiled: June 17, 2009Publication date: July 21, 2011Inventors: Takanobu Kuroita, Yasuhiro Imaeda, Kouichi Iwanaga, Naohiro Taya, Hidekazu Tokuhara, Yoshiyuki Fukase
-
Publication number: 20110172209Abstract: The present invention is directed to certain 3H-imidazo[4,5-b]pyridin-5-ol derivatives of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the GPR81 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of GPR81 associated disorders, for example, dyslipidemia, atherosclerosis, atheromatous disease, hypertension, coronary heart disease, stroke, insulin resistance, impaired glucose tolerance, type 2 diabetes, syndrome X, obesity, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type 1 diabetes and acne.Type: ApplicationFiled: September 10, 2009Publication date: July 14, 2011Applicants: ARENA PHARMACEUTICALS, INC., MERCK & CO., INC.Inventors: P. Douglas Boatman, Benjamin R. Johnson, Jae-Kyu Jung, Michelle Kasem, Thomas O. Schrader, Philip J. Skinner, Steven Colletti
-
Publication number: 20110172203Abstract: The present invention relates to substituted imidazopyridinyl-aminopyridine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazopyridinyl-aminopyridine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: ApplicationFiled: December 29, 2010Publication date: July 14, 2011Applicant: ArQule, Inc.Inventors: Mark A. Ashwell, Chris Brassard, Anton Filikov, Jason Hill, Steffi Koerner, Jean-Marc Lapierre, Yanbin Liu, Nivedita Namdev, Robert Nicewonger, Rocio Palma, Manish Tandon, David Vensel, Akihisa Matsuda, Shin Iimura, Yuko Yamamoto
-
Patent number: 7977353Abstract: Novel heterocyclic aromatic compounds are provided that are useful in stimulating endogenous production or release of growth hormone, said compounds having the general structure of formula I wherein R1, R1?, R2, R3, R4, Xa, Y, Z and n are as described herein. The compounds provided herein are useful in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength.Type: GrantFiled: August 9, 2010Date of Patent: July 12, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Guixue Yu, Jun Li, William R. Ewing, Richard B. Sulsky, James J. Li, Joseph Anthony Tino
-
Patent number: 7977338Abstract: Compounds of formula wherein the residues R1, R2, R3, R9, R10 and Q and X, Y and Z are as defined in the specification, salts thereof; their use, methods of their use, processes for their production, pharmaceutical compositions comprising them, their combinations with second drug substances and the use thereof and the like. The compounds are protein kinase inhibitors and can be used for the treatment of diseases mediated by protein kinase inhibitors, e.g. for the treatment of various proliferative diseases.Type: GrantFiled: October 15, 2007Date of Patent: July 12, 2011Assignee: Novartis AGInventors: Pascal Furet, Vito Guagnano
-
Publication number: 20110166169Abstract: The invention relates to the novel substances in Formula (I): wherein Het is a heterocycle optionally substituted by one or a plurality of radicals R1 or R?1; R is selected from the group comprising Formula (A?), (B), (C), (D), or (E), with R1 and/or R?1 selected from H, halogen, CF3, nitro, cyano, alkyl, hydroxyl, mercapto, amino, alkylamino, dialkylamino, alkoxy, phenylalcoxy, alkylhio, or carboxy that is free or esterified by an alkyl, carboxamide, CO—NH(alkyl), CON(alkyl)2, NH—CO-alkyl, sulfonamide, NH—S02-alkyl, S(0)2-NHalkyl, or S(02)-N(alkyl)2 radical; all these radicals are optionally substituted; W1, W2, and W3 independently are CH or N; X is 0, S, NR2, C(O), S(O), or S(0)2; Z is optionally substituted H, Hal, -0-R2 or —NH—R2 with R2 being H, alkyl, cycloalkyl, or heterocycloalkyl; and these substances are all isomeric forms and salts thereof, used as drugs.Type: ApplicationFiled: September 14, 2010Publication date: July 7, 2011Applicant: sanofi-aventisInventors: Jean-Marie RUXER, Victor CERTAL, Marcel ALASIA, Luc BERTIN, Herve MINOUX, Patrick MAILLIET, Frank HALLEY, Maria MENDEZ-PEREZ
-
Publication number: 20110166138Abstract: Disclosed are compounds and compositions that inhibit the action of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MGL), methods of inhibiting FAAH and MGL, methods of modulating cannabinoid receptors, and methods of treating various disorders related to modulation of cannabinoid receptors.Type: ApplicationFiled: March 17, 2009Publication date: July 7, 2011Inventors: Alexandros Makriyannis, Lakshmipathi Pandarinathan, Nikolai Zvonok, Teija Parkkari, Lauren Chapman
-
Publication number: 20110166116Abstract: New compounds are disclosed which have utility in the treatment of a variety of metabolic related conditions in a patient. The compounds of this invention have the structure (I): wherein R1, R2, R3, n, p, q, and Ar are as defined herein, including stereoisomers, and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions comprising a compound of this invention, as well as methods relating to the use thereof in a patient in need thereof.Type: ApplicationFiled: June 23, 2010Publication date: July 7, 2011Applicants: BOEHRINGER INGELHEIM INTERNATIONAL GMBH, NEUROCRINE BIOSCIENCES, INC.Inventors: Brian DYCK, Joe A. TRAN, Junko TAMIYA, Florence JOVIC, Troy VICKERS, Chen CHEN, Nicole HARRIOTT, Timothy COON, Neil J. ASHWEEK
-
Publication number: 20110160229Abstract: The present invention is directed to AHCY inhibitors of formula (I): which are useful in the treatment of diseases characterized by high homocysteine levels, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases characterized by high homocysteine levels.Type: ApplicationFiled: August 31, 2009Publication date: June 30, 2011Inventors: Antonella Converso, Timothy J. Hartingh, Mark E. Fraley
-
Publication number: 20110152313Abstract: The invention describes a one pot process for synthesizing a compound of structure (I), or a tautomer thereof. A compound of structure (II), or a tautomer thereof, and an aldehyde of structure RdCHO are condensed to form a condensation product. The resulting condensation product is then oxidized in the same reaction mixture to produce the compound of structure (I) or a tautomer thereof.Type: ApplicationFiled: June 19, 2009Publication date: June 23, 2011Applicant: MACQUARIE UNIVERSITYInventors: Peter Helmuth Karuso, Sudhir Ramnathrao Shengule
-
Publication number: 20110152278Abstract: This invention provides for compounds, compositions, and methods that involve anti-proliferative and anti-neoplastic activity in cancer cells. In particular, a series of benzimidazole, purine, imidazopyridine, and imidazopyrizine compounds having selected substitution patterns are disclosed, and the activity of various subject compounds is demonstrated.Type: ApplicationFiled: March 3, 2011Publication date: June 23, 2011Applicant: SPELMAN COLLEGEInventor: Leyte L. Winfield
-
Patent number: 7960407Abstract: The invention relates to the essentially pure ?/-[({2-[4-(2-Ethyl-4,6-dimethyl-1H-imidazo[4,5-c]pyridin-1-yl)phenyl]ethyl}amino)carbonyl]-4-methylbenzenesulfonamide Polymorph Forms A and B and to processes for the preparation of, compositions containing and to the uses of, such crystal forms.Type: GrantFiled: March 1, 2006Date of Patent: June 14, 2011Assignee: Requalia Pharma Inc.Inventors: Naoaki Haruta, Tomoki Kato, Zheng Jane Li, Toyoharu Numata, Andrew Vincent Trask
-
Publication number: 20110136752Abstract: The invention relates generally to novel antibiotics and their analogs, to processes for the preparation of these novel antibiotics, to pharmaceutical compositions comprising the novel antibiotics; and to methods of using the novel antibiotics to treat or inhibit various disorders.Type: ApplicationFiled: December 6, 2010Publication date: June 9, 2011Applicant: NOVOBIOTIC PHARMACEUTICALS LLCInventors: Aaron PEOPLES, Lucy Losee LING, Kim LEWIS, Zhizhen ZHANG
-
Publication number: 20110130381Abstract: Inhibitors of dihydroorotate dehydrogenase (DHODH) for the Plasmodium enzyme have been identified and characterized. The inhibitors have high specificity, submicromolar efficacy against cultured parasite strains, exhibit drug-like properties, and are not overtly cytotoxic.Type: ApplicationFiled: May 7, 2009Publication date: June 2, 2011Inventors: Cecilia Bastos, Michael L. Booker, Cassandra A. Celatka, Jon C. Clardy, Joseph Cortese, Vishal P. Patel, Renato Skerlj, Roger C. Wiegand, Dyann F. Wirth
-
Patent number: 7951819Abstract: The present invention pertains to certain imidazo[4,5-b]pyridin-2-one and oxazolo[4,5 b]pyridin-2-one compounds and analogs thereof, which, inter alia, inhibit RAF (e.g., B RAF) activity, inhibit cell proliferation, treat cancer, etc. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., B-RAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and conditions that are ameliorated by the inhibition of RAF, RTK, etc., proliferative conditions such as cancer (e.g., colorectal cancer, melanoma), etc.Type: GrantFiled: April 26, 2007Date of Patent: May 31, 2011Assignees: Cancer Research Technology Limited, The Institute of Cancer Research: Royal Cancer Hospital, Astex Therapeutics LimitedInventors: Dan Niculescu-Duvaz, Caroline Joy Springer, Richard Malcolm Marais, Harmen Dijkstra, Delphine Menard, Ion Niculescu-Duvaz, Lawrence Davies, Arnaud Nourry
-
Publication number: 20110124624Abstract: Compounds of Formula I: in free or salt form, wherein Ra, Rb, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.Type: ApplicationFiled: February 3, 2011Publication date: May 26, 2011Inventors: Graham Charles Bloomfield, Ian Bruce, Judy Fox Hayler, Catherine LeBlanc, Darren Mark Le Grand, Clive McCarthy
-
Publication number: 20110124637Abstract: Provided herein are sirtuin-modulating compounds of formula (II). The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders relating to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: July 2, 2009Publication date: May 26, 2011Inventors: Chi B Vu, Jeremy S. Disch, Pui Yee Ng, Charles A. Blum, Robert B. Perni
-
Patent number: 7947709Abstract: Compounds of formula I, wherein R1, R2, R3, X and Ar, are as defined herein or pharmaceutically acceptable salts thereof, inhibit HIV-1 reverse transcriptase and afford a method for prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC. The present invention also relates to compositions containing compounds of formula I useful for the prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC.Type: GrantFiled: June 20, 2008Date of Patent: May 24, 2011Assignee: Roche Palo Alto LLCInventors: Todd Richard Elworthy, Joan Heather Hogg, Joshua Kennedy-Smith, Counde O'Yang, Mark Smith, Zachary Kevin Sweeney, Jeffrey Wu
-
Publication number: 20110112080Abstract: The invention relates to compounds of formula I wherein the definitions of X, R and R1 are as defined herein. The compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds can be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.Type: ApplicationFiled: November 3, 2010Publication date: May 12, 2011Inventors: Guido Galley, Roger Norcross, Alessandra Polara
-
Publication number: 20110105430Abstract: Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: (A) are inhibitors N of p38 and are useful in the treatment of inflammation such as in the treatment of asthma, rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis, gouty arthritis and other arthritic conditions; inflamed joints, eczema, psoriasis or other inflammatory skin conditions such as sunburn; inflammatory eye conditions including conjunctivitis; pyresis, pain and other conditions associated with inflammation.Type: ApplicationFiled: June 8, 2009Publication date: May 5, 2011Inventors: Soumya P. Sahoo, Meng-Hsin Chen, Kevin D. Dykstra, Hiroo Koyama, Peter T. Meinke, Stephen J. O'keefe, Ginger Xu-Qiang Yang
-
Publication number: 20110098248Abstract: The present application includes novel modulators of TLRs, compositions containing such compounds, therapeutic methods that include the administration of such compounds.Type: ApplicationFiled: October 15, 2010Publication date: April 28, 2011Applicant: Gilead Sciences, Inc.Inventors: Randall L. Halcomb, Paul A. Roethle
-
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
-
Patent number: 7932251Abstract: The present invention relates to 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives having the general Formula I to pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S related diseases such as atherosclerosis, obesity, inflammation and immune disorders, such as rheumatoid arthritis, psoriasis, cancer, and chronic pain, such as neuropathic pain.Type: GrantFiled: July 15, 2008Date of Patent: April 26, 2011Assignee: N.V. OrganonInventors: Jiaqiang Cai, Zoran Rankovic, Philip Stephen Jones, David Jonathan Bennett, Xavier Fradera
-
Publication number: 20110092479Abstract: Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Type: ApplicationFiled: February 27, 2009Publication date: April 21, 2011Applicants: Array BioPharma Inc., Genentech, Inc.Inventors: Kateri A. Ahrendt, Alexandre J. Buckmelter, Jason De Meese, Jonas Grina, Joshua D. Hansen, Ellen R. Laird, Paul Lunghofer, David Moreno, Brad Newhouse, Li Ren, Jeongbeob Seo, Hongqi Tian, Steven M. Wenglowsky, Bainian Feng, Janet Gunzner, Kim Malesky, Simon Mathieu, Joachim Rudolph, Zhaoyang Wen, Wendy B. Young
-
Publication number: 20110092475Abstract: The present invention provides 2-substituted-ethynylthiazole derivatives of formula (I): wherein R1, R2 and X are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods of using same.Type: ApplicationFiled: October 20, 2010Publication date: April 21, 2011Applicant: H. LUNDBECK A/SInventors: Allen Hopper, Anette Graven Sams, Gitte Kobberoee Mikkelsen, Mathivanan Packiarajan, Michel Grenon
-
Patent number: 7928119Abstract: Methods of treating IL-6 involved diseases with EP4 receptor ligands, including EP4 receptor antagonists. Assays to determine the effect of test compounds on PGE2-induced whole blood cells activation.Type: GrantFiled: November 3, 2006Date of Patent: April 19, 2011Assignee: Pfizer Inc.Inventors: Masato Shimojo, Kana Taniguchi
-
Publication number: 20110086817Abstract: Embodiments herein provide compounds and methods of making and using such compounds for prevention and treatment of multidrug resistant bacteria. In particular, embodiments are directed to anti-bacterial agents from benzo[d]heterocyclic scaffolds for prevention and treatment of multidrug resistant bacteria.Type: ApplicationFiled: May 29, 2009Publication date: April 14, 2011Applicant: University of Notre Dame du LacInventors: Marvin J. Miller, Garrett C. Moraski
-
Patent number: 7923560Abstract: The present invention provides immune response modifiers (IRMs) associated with (typically, attached to, and preferably, covalently attached to) macromolecular support materials. The IRM compounds in such IRM-support complexes retain biological activity. Such attachment of an IRM to a macromolecular support material provides for the localized biological activity of the IRM.Type: GrantFiled: April 9, 2004Date of Patent: April 12, 2011Assignee: 3M Innovative Properties CompanyInventors: Paul D. Wightman, Isidro Angelo E. Zarraga, Naiyong Jing, Jie J. Liu