Nitrogen, Other Than As Nitro Or Nitroso, Attached Directly To The Six Membered Hetero Ring By Nonionic Bonding Patents (Class 546/159)
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Patent number: 7956185Abstract: Compounds of formula (I) where X1, C1, and D1 are defined herein, are inhibitors of polo-like kinases. The compounds of formula (I) are useful for treatment of diseases of cellular proliferation, such as, for example, cancer.Type: GrantFiled: May 24, 2007Date of Patent: June 7, 2011Assignee: Abbott LaboratoriesInventors: Robert B. Diebold, Stevan W. Djuric, Vincent L. Giranda, Laura A. Hexamer, Nan-Horng Lin, Julie M. Miyashiro, Thomas D. Penning, Magdalena Przytulinska, Thomas J. Sowin, Gerard M. Sullivan, Zhi-Fu Tao, Yunsong Tong, Anil Vasudevan, Le Wang, Keith W. Woods, Zhiren Xia, Henry Q. Zhang
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Patent number: 7956188Abstract: Compounds of the general formula (I); wherein the substituents are as defined in claim 1, are useful as fungicides.Type: GrantFiled: November 29, 2005Date of Patent: June 7, 2011Assignee: Syngenta Crop Protection, Inc.Inventors: Roger Salmon, David Philip Bacon, Ewan James Turner Chrystal, David William Langton, Andrew Jonathan Knee, Gordon Richard Munns, Laura Quaranta, Hans-Georg Brunner, Renaud Beaudegnies, Fredrik Cederbaum, Fiona Murphy Kessabi
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Publication number: 20110130365Abstract: The present invention provides Formula (1A) XN O R 3 HN R 5 O R 4 R 2 R 1 (1A) 5 compounds that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by the glucokinase enzyme, where X, R 1, R 2, R 3, R 4, and R 5 are as described herein.Type: ApplicationFiled: July 15, 2009Publication date: June 2, 2011Inventors: John W. Benbow, Jihong Lou, Jeffrey A. Pferfferkorn, Meihua M. Tu
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Patent number: 7951820Abstract: This invention describes novel triazole compounds of formula IX: wherein Z1 is nitrogen or CR9 and Z2 is nitrogen or CH, provided that at least one of Z1 and Z2 is nitrogen; G is Ring C or Ring D; Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, wherein said Ring C has one or two ortho substituents independently selected from —R1; Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T-R3, or Rx and Ry are taken together with their intervening atoms to form a fused ring; R1, R3, and T are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of GSK-3 and Aurora, for treating diseases such as diabetes, cancer, and Alzheimer's disease.Type: GrantFiled: July 25, 2006Date of Patent: May 31, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Bebbington, Ronald Knegtel, Hayley Binch, Julian M. C. Golec, Pan Li, Jean-Damien Charrier
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Patent number: 7951950Abstract: Disclosed are CRTH2 inhibitors represented by Structural Formula (I): The values for the variables of Structural Formula (I) are provided herein.Type: GrantFiled: February 23, 2006Date of Patent: May 31, 2011Assignee: Millennium Pharmaceuticals, Inc.Inventors: Jeremy D. Little, Shomir Ghosh, Sean Harrison, Amy M. Elder, Christelle C. Renou, Kenneth G. Carson
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Patent number: 7947712Abstract: The present invention relates to 8-Hydroxyquinoline Compounds; compositions comprising an 8-Hydroxyquinoline Compound; and methods for treating or preventing a metalloproteinase-related disorder, such as, an arthritic disorder, osteoarthritis, malignant neoplasm, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, atherosclerosis, age-related macular degeneration, myocardial infarction, a corneal ulceration, an ocular surface disease, hepatitis, an aortic aneurysm, tendonitis, a central nervous system disorder, abnormal wound healing, angiogenesis, restenosis, cirrhosis, multiple sclerosis, glomerulonephritis, graft versus host disease, diabetes, an inflammatory bowel disease, shock, invertebral disc degeneration, stroke, osteopenia or a periodontal disease or comprising administering an effective dose of an 8-Hydroxyquinoline Compound to a mammal in need thereof.Type: GrantFiled: August 23, 2007Date of Patent: May 24, 2011Assignee: Wyeth LLCInventors: Matthew G. Bursavich, Sabrina Lombardi, Adam M. Gilbert, Leif Mark Laakso, Gulnaz Khafizova, David Brian How, Joshua James Sabatini, Phaik-Eng Sum, Jeremy Clemens
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Patent number: 7943777Abstract: Chemical compounds having a high selectivity for double stranded DNA over RNA and single stranded DNA are disclosed. The chemical compounds are stains that become fluorescent upon illumination and interaction with double stranded DNA, but exhibit reduced or no fluorescence in the absence of double stranded DNA. The compounds can be used in a variety of biological applications to qualitatively or quantitatively assay DNA, even in the presence of RNA.Type: GrantFiled: October 5, 2009Date of Patent: May 17, 2011Assignee: Life Technologies CorporationInventors: Jolene Bradford, Ching-Ying Cheung, Shih-Jung Huang, Patrick Pinson, Stephen Yue
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Patent number: 7943638Abstract: A carboxamide compound represented by the formula (1): [wherein Q represents a nitrogen-containing 6-membered aromatic heterocyclic group optionally fused with a benzene ring, one of ring constitutional atoms of the heterocyclic group is a nitrogen atom and the heterocyclic group may be substituted with a group selected from the group consisting of a C1-C3 alkyl and the like, R1 represents a C1-C3 alkyl group or the like, R2 represents a hydrogen atom or the like, and R3 represents a hydrogen atom or the like] and a plant disease controlling agent comprising this as an active ingredient.Type: GrantFiled: July 12, 2006Date of Patent: May 17, 2011Assignee: Sumitomo Chemical Company, LimitedInventors: Shin-ichiro Souma, Yoshiharu Kinoshita
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Publication number: 20110112092Abstract: The present invention relates to an adenosine A3 receptor ligand of the general formula (I).Type: ApplicationFiled: January 18, 2011Publication date: May 12, 2011Applicant: sanofi-aventisInventors: Peter ARANYI, Sandor BATORI, Geza TIMARI, Kinga BOER, Zoltan KAPUI, Endre MIKUS, Katalin URBAN-SZABO, Katalin GERBER, Judit VARGANE SZEREDI, Michel FINET
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Patent number: 7939667Abstract: Compounds of formula (I): wherein B, X, R3, L0, L1, L2, R2, R1 and RC are defined herein. The compounds are useful as inhibitors of HCV NS3 protease for the treatment of hepatitis C viral infection.Type: GrantFiled: June 21, 2007Date of Patent: May 10, 2011Assignee: Boehringer Ingelheim International GmbHInventors: Montse Llinas-Brunet, Murray Bailey, Punit Bhardwaj, Josee Bordeleau, Pasquale Forgione, Elise Ghiro, Vida Gorys, Nathalie Goudreau, Sylvie Goulet, Teddy Halmos, Jean Rancourt
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Publication number: 20110105513Abstract: Compounds of the Formula (I), where W represents CH or N; and Q represents —CN, —C(?NOH)NH2, —CONHR1 or various herein described heterocyclic radicals; as well as pharmaceutically acceptable salts, solvates, esters and prodrugs thereof. Care adenosine A2a receptor antagonists and, therefore, are useful in the treatment of central nervous system diseases, in particular Parkinson's disease.Type: ApplicationFiled: March 3, 2009Publication date: May 5, 2011Inventors: Joel M. Harris, Bernard R. Neustadt, Hong Liu, Jinsong Hao, Andrew W. Stamford
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Publication number: 20110104110Abstract: The present invention relates to Substituted Indole Derivatives, compositions comprising at least one Substituted Indole Derivative, and methods of using these Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: ApplicationFiled: August 27, 2008Publication date: May 5, 2011Inventors: Gopinadhan N. Anikumar, Frank Bennett, Tin-Yau Chan, Kevin X. Chen, Mousumi Sannigrahi, Francisco Velazquez, Srikanth Venkatraman, Qingbei Zeng, Jose S. Duca, Charles A. Lesburg, Joseph A. Kozlowski, F. George Njoroge, Stuart B. Rosenblum, Neng-Yang Shih
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Publication number: 20110105530Abstract: The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.Type: ApplicationFiled: June 25, 2009Publication date: May 5, 2011Inventors: Natalie Dales, Zaihui Zhang, Jianmin Fu, Duanjie Hou, Shaoyi Sun, Vishnumurthy Kodumuru, Natalia Pokrovskaia
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Patent number: 7932392Abstract: Compounds of Formula (IA) wherein R1, R2, R3, R4 and R5 are as defined herein for Formula (IA), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.Type: GrantFiled: July 20, 2005Date of Patent: April 26, 2011Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Rajashekhar Betageri, Thomas A. Gilmore, Daniel Kuzmich, John Robert Proudfoot, David S. Thomson
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Patent number: 7928133Abstract: The invention provides a method for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula I.Type: GrantFiled: July 24, 2007Date of Patent: April 19, 2011Assignee: IRM LLCInventors: Dai Cheng, Dong Han, Wenqi Gao, Jiqing Jiang, Shifeng Pan, Yongqin Wan, Qihui Jin
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Patent number: 7928123Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: GrantFiled: September 13, 2007Date of Patent: April 19, 2011Assignee: Boehringer Ingelheim International GmbHInventors: Angela Berry, Pier Francesco Cirillo, Doris Riether, David Thomson, Renee M. Zindell, Nigel Blumire, Chandana Chowdhury, Monika Ermann, James Edward Jenkins, Innocent Mushi, Christopher Francis Palmer, Malcolm Taylor
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Patent number: 7928239Abstract: This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions in such therapy.Type: GrantFiled: February 7, 2001Date of Patent: April 19, 2011Assignee: Bayer Healthcare LLCInventors: Jacques Dumas, Bernd Riedl, Uday Khire, Jill E. Wood, Robert N. Sibley, Mary-Katherine Monahan, Joel Renick, David E. Gunn, Timothy B. Lowinger, William J. Scott, Roger A. Smith
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Patent number: 7923561Abstract: The present invention relates to 2-Aminoquinoline derivatives of general formula I and pharmaceutically-acceptable acid-addition salts thereof, wherein R1, R2 and X are as defined in the specification. The compounds may be used as 5-HT5A receptor antagonists. The present invention relates also to processes for making such a compound and a pharmaceutical composition comprising such a compound. Compounds of the present invention are useful in the prevention and/or treatment of anxiety depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, dementia, disorders of eating behaviors, sexual dysfunction, sleep disorders, withdrawal from abuse of drugs, motor disorders such as Parkinson's disease, psychiatric disorders and gastrointestinal disorders.Type: GrantFiled: November 29, 2007Date of Patent: April 12, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Sabine Kolczewski, Claus Riemer, Lucinda Steward, Juergen Wichmann, Thomas Woltering
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Patent number: 7919505Abstract: The present invention relates to the compound of the formula To methods of treating upper and lower obstructive airway diseases using said compound, to formulations comprising it, and to polymorphs and processes of synthesis of the polymorphic forms.Type: GrantFiled: July 10, 2007Date of Patent: April 5, 2011Assignee: Schering CorporationInventors: Pauline C. Ting, Joe F. Lee, Kung-I Feng, Michael R. Reeder, Scott T. Trzaska, Man Zhu, Chen Mao, Dimitar L. Filipov, Dimitrios N. Zarkadas
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Patent number: 7919625Abstract: Compounds of the formula: wherein: n is an integer from 1-3; X is N, CH, provided that when X is N, n is 2 or 3; R is alkyl of 1 to 3 carbon atoms; R1 is 2,4-diCl, 5-OMe; 2,4-diCl; 3,4,5-tri-OMe; 2-Cl, 5-OMe; 2-Me, 5-OMe; 2,4-di-Me; 2,4-diMe-5-OMe, 2,4-diCl, 5-OEt; R2 is alkyl of 1 to 2 carbon atoms, and pharmaceutically acceptable salts thereof.Type: GrantFiled: June 16, 2008Date of Patent: April 5, 2011Assignee: Wyeth LLCInventors: Frank Boschelli, Jennifer M. Golas, Kim T. Arndt
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Patent number: 7915291Abstract: Hepatitis C virus inhibitors are disclosed having the general formula: wherein R1, R2, R3, R?, B, Y and X are described in the description. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.Type: GrantFiled: September 2, 2008Date of Patent: March 29, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Xiangdong Alan Wang, Li-Qiang Sun, Sing-Yuen Sit, Ny Sin, Paul Michael Scola, Yan Chen
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Publication number: 20110071165Abstract: Aza- and polyazanthranyl amides and their use as medicaments in the treatment of diseases caused by persistent angiogenesis are described, as well as the intermediates used in the preparation of the aza- and polyazanthranyl amides.Type: ApplicationFiled: November 24, 2010Publication date: March 24, 2011Applicant: NOVARTIS AGInventors: Dieter SEIDELMANN, Martin KRÜGER, Orlin PETROV, Andreas HUTH, Karl-Heinz THIERAUCH, Andreas MENRAD, Martin HABEREY
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Patent number: 7906650Abstract: This invention provides novel compounds, and pharmaceutically acceptable derivatives thereof, that are useful as caspase inhibitors. These compounds have the general formula I: where R1, R2, and R3 are as described herein, Ring A contains zero to two double bonds, each X is independently selected from nitrogen or carbon, at least one X in Ring A is a nitrogen, Ring A is optionally substituted as described, and may be fused to a saturated or unsaturated five to seven membered ring containing zero to three heteroatoms, and provided that when X3 is a carbon, a substituent on X3 is attached by an atom other than nitrogen.Type: GrantFiled: January 26, 2009Date of Patent: March 15, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: Julian M. C. Golec, Paul S. Charifson, Jean-Damien Charrier, Hayley Marie Binch
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Patent number: 7902225Abstract: The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or the general Formula (Ib) the pharmaceutically acceptable acid or base addition salts thereof, the quaternary amines thereof, the stereochemically isomeric forms thereof the tautomeric forms thereof and the N-oxide forms thereof. The claimed compounds are useful for the treatment of mycobacterial diseases. In particular, compounds are claimed in which, independently from each other, R1 is halo; p=1; R2 is optionally substituted alkyloxy, alkyl, Ar, Het, or a radical of formula R3 is optionally substituted Ar or Het; q=1, R4 and R5 each independently are alkyl; R6 is hydrogen or a radical of formula r is equal to 0 or 1 and R7 is hydrogen or Ar.Type: GrantFiled: January 21, 2005Date of Patent: March 8, 2011Assignee: Janssen Pharmaceutica NVInventors: Jérôme Emile Georges Guillemont, Elisabeth Therese Jeanne Pasquier, David Francis Alain Lancois
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Patent number: 7897774Abstract: The present invention relates to a synthesis study of novel cyclic compounds having a quinolylalkylthio group represented by the formula (1), and pharmacological actions of the compounds. In the formula, the ring X represents: which may have halogen and/or alkyl; R1 and R2 independently represent hydrogen, alkyl, cycloalkyl, aryl or a (non) aromatic heterocycle; R3 represents qinolyl; A represents sulfur, sulfinyl or sulfonyl; and B represents alkylene.Type: GrantFiled: August 30, 2007Date of Patent: March 1, 2011Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Kenji Kawashima, Takahiro Honda, Hisashi Tajima, Kazuyoshi Okamoto, Minoru Yamamoto
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Patent number: 7884104Abstract: The present invention is directed to novel substituted aminopiperidines which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) 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: September 27, 2005Date of Patent: February 8, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Jason M. Cox, Scott D. Edmondson, Bart Harper, Ann E. Weber
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Patent number: 7884113Abstract: The invention provides for compounds of formula I wherein the substitutents are as described herein. Further provided are methods of using such compounds for the treatment of eating disorders, metabolic disorders, obesity, cognitive disorders, neurological disorders, pain disorders, inflammation disorders, in the promotion of smoking cessation and for the treatment of other psychiatric disorders Also provided are pharmaceutical compositions containing such compounds and pharmaceutical combinations of the compounds of the invention with other therapeutic agents.Type: GrantFiled: April 24, 2008Date of Patent: February 8, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Chongqing Sun, Doree Sitkoff, William R. Ewing, Yanting Huang, Bruce A. Ellsworth, Richard B. Sulsky, Annapurna Pendri, Samuel Gerritz, Natesan Murugesan, Zhengxiang Gu
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Patent number: 7880006Abstract: Disclosed are compounds that have excellent insecticidal activity and are usable as agricultural and horticultural insecticides. Compounds represented by formula (I) or agriculturally and horticulturally acceptable acid addition salts thereof have excellent insecticidal activity and are usable as agricultural and horticultural insecticides.Type: GrantFiled: August 3, 2005Date of Patent: February 1, 2011Assignees: Meiji Seika Kaisha, Ltd., Nippon Kayaku Co., Ltd.Inventors: Kazumi Yamamoto, Ryo Horikoshi, Kazuhiko Oyama, Hiroshi Kurihara, Shizuo Shimano, Takaaki Miyake, Hiroki Hotta, Jun Iwabuchi
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Patent number: 7872126Abstract: A novel compound of the formula (I): wherein R1 is alkoxycarbonyl or the like, R2 is alkyl or the like; R3 is hydrogen or the like; R4 is alkylene or the like; R5 is optionally substituted heterocyclic group; R6, R7, R8 and R9 are independently hydrogen; alkyl, alkoxy, or the like; R10 is optionally substituted aromatic ring, or the like; or a pharmaceutically acceptable salt thereof, which has an inhibitory activity against cholesteryl ester transfer protein (CETP).Type: GrantFiled: September 27, 2006Date of Patent: January 18, 2011Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Hitoshi Kubota, Masakatsu Sugahara, Mariko Furukawa, Mayumi Takano, Daisuke Motomura
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Publication number: 20110009400Abstract: The disclosure relates to compounds of formula (I): wherein X1, X2, X3, X4, Y, n, A, and W are as defined in the disclosure, or a salt thereof, or a hydrate or solvate thereof, and to processes for the preparation of these compounds and the therapeutic use thereof.Type: ApplicationFiled: July 21, 2010Publication date: January 13, 2011Applicant: SANOFI-AVENTISInventors: Laurent Dubois, Yannick Evanno, Catherine Gille, André Malanda
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Patent number: 7868022Abstract: The present invention is directed to 2-amino-quinoline derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD) and related disorders. The compounds of the invention are inhibitors of ?-secretase, also known as ?-site cleaving enzyme and BACE, BACE1, Asp2 and memapsin2.Type: GrantFiled: February 6, 2007Date of Patent: January 11, 2011Assignee: Janssen Pharmaceutica NVInventors: Ellen Baxter, Allen B. Reitz, Umar Saibu Mohomed Maharoof, Yifang Huang, Christopher John Creighton, Charles H. Reynolds, Chi Luo, Brett A. Tounge, Tina Morgan Ross, Tianbao Lu
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Publication number: 20100331324Abstract: Disclosed are fused heterocyclic compounds of Formula (I) or pharmaceutically-acceptable salts or stereoisomers thereof. Also disclosed are methods of using such compounds in the treatment of at least one androgen receptor-associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.Type: ApplicationFiled: June 26, 2008Publication date: December 30, 2010Inventors: Derek J. Norris, Ashvinikumar V. Gavai, James Aaron Balog, Joel F. Austin, Weifang Shan, Yufen Zhao, Andrew James Nation, Wen-Ching Han
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Patent number: 7858642Abstract: The invention relates to novel compounds and also to methods of treating at least one disease, disorder, or condition associated with amyloidosis using such compounds. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein.Type: GrantFiled: March 3, 2009Date of Patent: December 28, 2010Assignee: Elan Pharmaceuticals, Inc.Inventors: Varghese John, Michel Maillard, John Tucker, Jose Aquino, Barbara Jagodzinska, Louis Brogley, Jay S. Tung, Simeon Bowers, Darren Dressen, Gary Probst, Neerav Shah
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Patent number: 7858793Abstract: The present invention relates to the novel compounds Methyl 2-[(3S)-[3-[(2E)(7-chloro quinolin-2-yl)ethenyl]phenyl]-3-halopropyl]benzoates (IV) wherein the halo is chloro, bromo, iodo, starting from the known compound Methyl 2-[(3S)-[3-[(2E)-(7-chloroquinolin-2-yl)ethenyl]phenyl]-3-hydroxypropyl]benzoate (1). Reaction of Methyl 2-[(3S)-[3-[(2E)-(7-chloroquinolin-2-yl)ethenyl]phenyl]-3-hydroxypropyl]benzoate (1) with thionyl chloride or with methane sulfonyl chloride-lithium bromide or with trimethyl chlorosilane-sodium iodide in presence or absence of base gives Methyl 2-[(3S)-[3-[(2E)-(7-chloro quinolin-2-yl)ethenyl]phenyl]-3-halopropyl]benzoates.Type: GrantFiled: July 19, 2004Date of Patent: December 28, 2010Inventors: Chava Satyanarayana, Gorantla Seeta Ramanjaneyulu, Indukuri Venkata Sunil Kumar, Simhadri Srinivas
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Patent number: 7858640Abstract: Compounds of formula [1] are CRTH2 antagonists, useful in the treatment of conditions having an inflammatory components; in which: R1-R9 are various substituents; A is —CHR10—, —C(O)—, —S(O)n—, —O—, or —NR10— wherein n is an integer from 0-1 and R10 is selected from various substituents; B is a direct bond or a divalent radical; R11 and R12 are selected from cvarious substituents; X is a carboxylic acid, tetrazole, 3-hydroxyisoxazole, hydroxamic acid, phosphinate, phosphonate, phosphonamide, sulfonic acid group, or a group of formula C?(O)NHSO2R6 or SO2NHC(?O)R6; and Y is aryl, heteroaryl, aryl-fused-heterocycloalkyl, heteroaryl-fused-cycloalkyl, heteroaryl-fused-heterocycloalkyl or aryl-fused-cycloalkyl group.Type: GrantFiled: September 29, 2006Date of Patent: December 28, 2010Assignee: Pulmagen Therapeutics (Asthma) LimitedInventors: Michael Colin Cramp, Rosa Arienzo, George Hynd, Peter Crackett, Yann Griffon, Trevor Keith Harrison, Nicholas Charles Ray, Harry Finch, John Gary Montana
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Publication number: 20100324010Abstract: A renin inhibitor comprising a compound represented by the formula: wherein each symbol is as defined in the description, or a salt thereof or a prodrug thereof. The compound of the present invention has a superior renin inhibitory activity, and thus is useful as an agent for the prophylaxis or treatment of hypertension, various organ damages attributable to hypertension and the like.Type: ApplicationFiled: October 14, 2008Publication date: December 23, 2010Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Yasuhiro Imaeda, Takanobu Kuroita, Yoshiyuki Fukase, Shinkichi Suzuki, Michiko Amano
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Patent number: 7855203Abstract: The present invention is directed to novel indazolyl-substituted pyrroline compounds of Formula (I): useful as kinase or dual-kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase or dual-kinase mediated disorder.Type: GrantFiled: December 13, 2007Date of Patent: December 21, 2010Assignee: Ortho-McNeil-Janssen Pharmaceuticals, Inc.Inventors: Han-Cheng Zhang, Bruce Maryanoff, Kimberly White, Hong Ye, Leonard R. Hecker, David F. McComsey
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Publication number: 20100317643Abstract: The invention provides compounds of Formula I, stereoisomers or pharmaceutically acceptable salts thereof, wherein A, B, D, R1, R2, R4 and R5 are defined herein, a pharmaceutical composition that includes a compound of Formula I and methods of use thereofType: ApplicationFiled: June 10, 2010Publication date: December 16, 2010Applicant: GENENTECH, INC.Inventors: SIMON CHARLES GOODACRE, YINGJIE LAI, JUN LIANG, STEVEN R. MAGNUSON, KIRK D. ROBARGE, MARK S. STANLEY, VICKIE HSIAO-WEI TSUI, KAREN WILLIAMS, BIRONG ZHANG, AIHE ZHOU
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Publication number: 20100317862Abstract: Use of the general formula compound (I), or any salt thereof, for preparation of a pharmaceutical compound for the treatment of infections illnesses, in particular for the treatment of Helicobacter. Y is NO2, COOH or SO3H; Z is O, N or S; X1 and X2 are halogen atoms which may be the same or different; and m and n take values from 0 to 3 and may be equal or different.Type: ApplicationFiled: February 20, 2008Publication date: December 16, 2010Inventors: Javier Sancho Sanz, Adrián Velazquez Campoy, Nunilo Cremades Casasin
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Publication number: 20100305065Abstract: There is provided the use of compounds of formula wherein R1, R2, R3 and E have meanings given in the description, for the preparation of a medicament for killing clinically latent microorganisms. There is also provided the use of compounds of formula I for treating microbial infections, as well as certain compounds of formula (I) per se.Type: ApplicationFiled: May 16, 2008Publication date: December 2, 2010Applicant: HELPERBY THERAPEUTICS LIMITEDInventors: Mandy Christine Beswick, Susan Mary Cramp, Yanmin Hu, Thomas David Pallin, Hazel Joan Dyke, Anthony Coates
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Patent number: 7842811Abstract: Cyanine dye compounds having a negatively charged substituent that are nucleic acid stains, particularly for fluorescent staining of DNA, including compounds having the formula wherein W forms one or two fused 5- or 6-membered aromatic rings, ? has a value of 0 or 1, n has a value of 0, or 1, X is O, S, or Se, and D is a pyridinium, or quinolinium moiety, provided that the compound has at least one negatively charged substituent.Type: GrantFiled: January 12, 2010Date of Patent: November 30, 2010Assignee: Life Technologies CorporationInventors: Jason Dallwig, David Hagen, Shih-Jung Huang, Gerald Thomas, Stephen Yue
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Patent number: 7838127Abstract: Provided are organic electronic devices comprising at least one layer comprising at least one complex of the formula: where M is Ti, Zr, Hf, Nb, Re, Sn, and Ge; R1, R2, R3, R4, R5, R6, R7, and R8 are each independently F, Cl, CF3, diarylamine, carbazolyl, alkoxy, cyano, alkyl or aryl, wherein at least one of R1, R2, R3, R4, R5, R6, R7, and R8 is carbazolyl; and a, b, c, d, e, f, g, and h are each 0, 1, 2, or 3, at least one of which is other than zero.Type: GrantFiled: December 15, 2005Date of Patent: November 23, 2010Assignee: E. I. du Pont de Nemours and CompanyInventors: Ying Wang, Norman Herron
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Patent number: 7829578Abstract: Aromatic ketones having an extended fluoro-alkyl or fluoro-alkoxy moiety are disclosed. In particular aspects, the compounds comprise substituted 9-acridone, 9-xanthone, 4(1H)-quinolone, 4(1H) pyridone, 1,4-naphthoquinone, 9,10-anthraquinone derivatives. These preparations possess potent pharmacological activity for inhibiting malaria and mosquito-borne (Plasmodium) diseases. The haloalkyl/alkoxy aromatic compounds possess significant pharmacological activity, with IC50 values in the nanomolar and sub-nanomolar range, and reduced toxicity against host derived cells and tissues. Methods of using the fluoro-alkyl/alkoxy aromatic compounds in the treatment of malaria and other human and animal diseases are also disclosed. Agricultural uses of the fluoro-alkyl/alkoxy aromatic compounds, such as in control of fungal diseases and in the production of important commercial crops (apples, etc.), are also presented.Type: GrantFiled: December 5, 2006Date of Patent: November 9, 2010Assignees: Oregon Health & Science University, U.S. Department of Veterans AffairsInventors: Michael K. Riscoe, Rolf W. Winter, Jane X. Kelly, Martin J. Smilkstein, David J. Hinrichs
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Patent number: 7825253Abstract: The present invention relates to compounds of the formula (I): or pharmaceutically acceptable salts thereof, wherein X, Y, Ar1, and Ar2 are as defined in the specification.Type: GrantFiled: September 21, 2007Date of Patent: November 2, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Sabine Kolczewski, Claus Riemer, Lucinda Steward, Juergen Wichmann, Thomas Woltering
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Patent number: 7825252Abstract: The invention provides synthetic processes and synthetic intermediates that can be used to prepare 4-oxoquinolone compounds having useful integrase inhibiting properties.Type: GrantFiled: September 11, 2007Date of Patent: November 2, 2010Assignee: Gilead Sciences, Inc.Inventors: Eric Dowdy, Xi Chen, Steven Pfeiffer
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Patent number: 7820663Abstract: The present invention is related substituted enaminones represented by a compound of Formula I that are novel allosteric modulators of ?7 nAChRs. The invention also discloses the treatment of disorders that are responsive to enhancement of acetylcholine action on ?7 nAChRs in a mammal by administering an effective amount of a compound of Formula I.Type: GrantFiled: June 15, 2006Date of Patent: October 26, 2010Assignee: The Regents of the University of CaliforniaInventors: Derk J. Hogenkamp, Timothy B. C. Johnstone, Kelvin W. Gee
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Patent number: 7820824Abstract: Chemically reactive carbocyanine dyes incorporating an indolium ring moiety that is substituted at the 3-position by a reactive group or by a conjugated substance, and their uses, are described. Conjugation through this position results in spectral properties that are uniformly superior to those of conjugates of spectrally similar dyes wherein attachment is at a different position. The invention includes derivative compounds having one or more benzo nitrogens.Type: GrantFiled: February 14, 2007Date of Patent: October 26, 2010Assignee: Life Technologies CorporationInventors: Wai-Yee Leung, Ching-Ying Cheung, Stephen Yue
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Publication number: 20100266621Abstract: Psoralen compounds of Formula (I): wherein (N+ Aryl) is a member selected from the group consisting of nitrogen containing aromatic heterocycles of formulae (i)-(iii): wherein Z is a group of formula: wherein R is C1-C30 hydrocarbyl, which may be linear, branched or cyclic and contains from 1 to 15 carbon-carbon double bonds, which may be conjugated or unconjugated with one another or may include an aryl ring, and may contain one or more substituents; R1 is hydrogen, aryl, heteroaryl, alkyl, cycloalkyl, heterocyclyl, alkenyl, alkynyl, alkene-aryl, alkene-heteroaryl, alkene-heterocyclyl, alkene-cycloalkyl, fused cycloalkylaryl, fused cycloalkylheteroaryl, fused heterocyclylaryl, fused heterocyclyheteroaryl, alkylene-fused cycloalkylaryl, alkylene-fused cycloalkylheteroaryl, alkylene-fused heterocyclylaryl, alkylene-fused heterocyclyheteroaryl; n is an integer from 1 to 8 and X is a pharmaceutically acceptable counter ion; and their use in methods for the treatment of a cell proliferatType: ApplicationFiled: April 20, 2010Publication date: October 21, 2010Applicants: Duke University, Immunolight, LLCInventors: Eric Toone, David Gooden, Tuan Vo-Dinh, Frederic A. Bourke, JR.
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Patent number: 7816372Abstract: The present invention is directed to compounds, pharmaceutical compositions, and methods for modulating processes mediated by AR. Also provided are methods of making such compounds and pharmaceutical compositions.Type: GrantFiled: August 23, 2004Date of Patent: October 19, 2010Assignee: Ligand Pharmaceuticals IncorporatedInventors: Lin Zhi, Esther Martinborough, Yixing Shen, Thomas Lot Stevens Lau, Min Wu, Yun Oliver Long
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Patent number: RE42376Abstract: This invention provides compounds of formula I having the structure wherein G1, G2, R1, R4, Z, n, and X are defined in the specification or a pharmaceutically acceptable salt thereof which are useful as antineoplastic agents and in the treatment of polycystic kidney disease.Type: GrantFiled: May 21, 2010Date of Patent: May 17, 2011Assignee: Wyeth Holdings CorporationInventors: Allan Wissner, Hwei-Ru Tsou, Dan M. Berger, Middleton B. Floyd, Jr., Philip R. Hamann, Nan Zhang, Philip Frost