1,2 Diazine Attached Directly Or Indirectly To An Additional Hetero Ring By Nonionic Bonding Patents (Class 514/252.01)
-
Patent number: 8293744Abstract: The present invention is directed to heterocyclic fused cinnoline compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. 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 mediated by the M1 receptor.Type: GrantFiled: April 13, 2010Date of Patent: October 23, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Scott D. Kuduk, Douglas C. Beshore
-
Patent number: 8283351Abstract: The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of the functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a cyclic or acyclic hydrazine derivative including those of formulas II or III: or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.Type: GrantFiled: March 28, 2008Date of Patent: October 9, 2012Assignee: Institute for OneWorld HealthInventors: Michael Geoffrey Neil Russell, Huw David Vater, Jacqueline Anne Macritchie, Kevin James Doyle, David Brown, Joanne Peach
-
Patent number: 8273745Abstract: The present invention relates to a novel compound or a salt thereof, which is useful as a CRTH2 antagonist, especially as a medicament for disorder that participates eosinophil, for example, allergic disorder such as asthma, allergic rhinitis, allergic dermatitis, conjunctival inflammation, hives, eosinophilic bronchitis, food allergy, inflammation of the nasal sinuses, multiple sclerosis, angiitis, or chronic obstructive pulmonary disease (COPD) and the like.Type: GrantFiled: December 13, 2007Date of Patent: September 25, 2012Assignee: Astellas Pharma IncInventors: Tadashi Terasaka, Tatsuya Zenkoh, Hisashi Hayashida, Hiroshi Matsuda, Junji Sato, Yoshimasa Imamura, Hiroshi Nagata, Norio Seki, Yoshiyuki Tenda, Mamoru Tasaki, Masahiro Takeda, Seiichiro Tabuchi, Minoru Yasuda, Kazunori Tsubaki
-
Publication number: 20120238579Abstract: The present invention relates to new compounds of formula (I) and to pharmaceutical composition containing said compounds and to the use of said compounds in therapy. The present invention further relates to processes for the preparation of said compounds and to new intermediates useful in the preparation thereof.Type: ApplicationFiled: March 23, 2012Publication date: September 20, 2012Inventors: Yevgeni Besidki, Inger Kers, Martin Nylôf, Lars Sandberg, Karin Skogholm
-
Patent number: 8268809Abstract: The present invention provides compositions and methods of use thereof to prevent and/or treat pathogenic infection. In particular, the present invention provides the use of kinase inhibitors to inhibit kinases that involve in pathogen-host cell interactions that are associated with or cause pathogenic infections, therefore, to effectively prevent and/or treat pathogenic infections with far less likely to engender resistance as compared to conventional antibiotics and anti-viral drugs. The present invention further provides the use of kinase inhibitors for the treatment of acute pathogenic infections for a short period of time to avoid toxicities that may caused by long term use of these kinase inhibitors.Type: GrantFiled: September 5, 2007Date of Patent: September 18, 2012Assignees: Emory University, M.D. Anderson Cancer CenterInventors: Daniel Kalman, William Bornmann
-
Patent number: 8268827Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts or tautomers thereof which are inhibitors of poly(ADP-ribose)polymerase (PARP) and thus useful for the treatment of cancer, inflammatory diseases, reperfusion injuries, ischaemic conditions, stroke, renal failure, cardiovascular diseases, vascular diseases other than cardiovascular diseases, diabetes mellitus, neurodegenerative diseases, retroviral infections, retinal damage, skin senescence and UV-induced skin damage, and as chemo- or radiosensitizers for cancer treatment.Type: GrantFiled: November 14, 2008Date of Patent: September 18, 2012Assignee: Istituto di Ricerche di Biologia Molecolare P. Angeletti SpA.Inventors: Danila Branca, Gabriella Dessole, Federica Ferrigno, Philip Jones, Olaf Kinzel, Samuele Lillini, Ester Muraglia, Giovanna Pescatore, Carsten Schultz-Fademrecht
-
Publication number: 20120232059Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: ApplicationFiled: May 18, 2012Publication date: September 13, 2012Applicant: Vertex Pharmaceuticals IncorporatedInventors: Sara Hadida-Ruah, Matthew Hamilton, Mark Miller, Peter D.J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou, Frederick van Goor
-
Publication number: 20120225873Abstract: The invention provides novel compounds useful for the treatment of neurodegenerative disorders including Alzheimer's disease and dementia. The compounds have a substituents chosen from -L-C(?O)OH, -L-CH?CHC(?O)OH, -L-C(?O)NH2, -L-C(?O)NH(C1-3 alkyl), -L-C(?O)N(C1-3 alkyl)2, -L-S(?O)2(C1-3alkyl), -L-S(?O)2NH2, -L-S(?O)2N(C1-3 alkyl)2, -L-S(?O)2NH(C1-3 alkyl), -L-C(?O)NHOH, -L-C(?O)CH2NH2, -L-C(?O)CH2OH, -L-C(?O)CH2SH, -L-C(?O)NHCN, -L-NHC(?O)ORo, -L-C(?O)NHRo, -L-NH(C?O)NHRo, -L-C(?O)N(Ro)2, -L-NH(C?O)N(Ro)2, -L-sulfo, -L-(2,6 difluorophenol), -L-phosphono, and -L-tetrazolyl, where L is a linker.Type: ApplicationFiled: April 13, 2012Publication date: September 6, 2012Applicant: Myrexis, Inc.Inventors: Rachel Slade, Yevgeniya Klimova, Robert J. Halter, Ashantai J. Yungai, Warren S. Weiner, Ruth J. Walton, Jon Adam Willardsen, Mark B. Anderson, Kenton Zavitz
-
Publication number: 20120208823Abstract: Disubstituted tetrahydrofuranyl compounds of general formula I of which the following are exemplary:Type: ApplicationFiled: August 12, 2011Publication date: August 16, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Norbert HAUEL, Angelo CECI, Henri DOODS, Birgit JUNG, Raimund KUELZER
-
Patent number: 8217043Abstract: The present invention relates to novel compounds capable of modulating the stability and/or activity of hypoxia inducible factor (HIF) by inhibiting the activity of at least one HIF hydroxylase enzyme.Type: GrantFiled: August 20, 2009Date of Patent: July 10, 2012Assignee: Fibrogen, Inc.Inventors: Shaojiang Deng, Wen-Bin Ho, Lee A. Flippin
-
Patent number: 8207168Abstract: The present invention is directed to novel pyridazinone derivatives that mediate enzymatic activity. In particular, the compounds may be effective in the treatment of diseases or disease states related to the activity of the histamine H3 receptor, including, for example, neurodegenerative disorders, sleep/wake disorders, attention deficit hyperactivity disorder and cognition disorders.Type: GrantFiled: June 15, 2010Date of Patent: June 26, 2012Assignee: Cephalon, Inc.Inventors: Nadine C. Becknell, Derek Dunn, Robert L. Hudkins, Kurt A. Josef, Lars J. S. Knutsen, Ming Tao, Allison L. Zulli
-
Publication number: 20120157410Abstract: The invention relates to compositions, conjugates and methods comprising pyridazine compounds and cholinesterase inhibitors for modulation of cellular pathways (e.g., signal transduction pathways), for treatment or prevention of inflammatory diseases (e.g., Alzheimer's disease), for research, drug screening, and therapeutic applications.Type: ApplicationFiled: February 17, 2012Publication date: June 21, 2012Applicants: U.S. Government, National Institute of Health (NIH), U.S. Department of Health and Human Services (DHSS),Inventors: D. Martin WATTERSON, Linda VAN ELDIK, Wenhui HU
-
Publication number: 20120142695Abstract: Compounds of the formula I wherein n, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and X are defined as described in the specification, which are bradykinin B1 antagonists, and their use as medicaments.Type: ApplicationFiled: February 22, 2011Publication date: June 7, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Norbert HAUEL, Angelo CECI, Henri DOODS, Ingo KONETZKI, Juergen MACK, Henning PRIEPKE, Annette SCHULER-METZ, Rainer WALTER, Dieter WIEDENMAYER
-
Patent number: 8193192Abstract: The present invention relates to compounds which bind to the NR1H4 receptor (FXR) and act as agonists or partial agonists of the NR1H4 receptor (FXR). The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds, and to a process for the synthesis of said compounds.Type: GrantFiled: August 29, 2007Date of Patent: June 5, 2012Assignee: Phenex Pharmaceuticals AGInventors: Claus Kremoser, Ulrich Deuschle, Ulrich Abel, Andreas Schulz
-
Patent number: 8188083Abstract: The present invention is directed to novel compounds of formula (I) wherein the variables are defined as herein. The compounds of formula (I) are useful as kinase inhibitors and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, cancers.Type: GrantFiled: June 26, 2008Date of Patent: May 29, 2012Assignee: Abbott LaboratoriesInventors: David J. Calderwood, Dominique F. Bonafoux, Andrew Burchat, Ping Ding, Kristine E. Frank, Michael Z. Hoemann, Kelly D. Mullen, Heather M. Davis
-
Patent number: 8183371Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, R2, R3, L, X, and Y are defined herein.Type: GrantFiled: October 28, 2010Date of Patent: May 22, 2012Assignee: Janssen Pharmaceutica NVInventors: Peter J. Connolly, Shu-Chen Lin, Mark J. Macielag, Yue-Mei Zhang
-
Patent number: 8178131Abstract: Compounds of Formula (I) are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula (I) and stereoisomers 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: GrantFiled: May 13, 2009Date of Patent: May 15, 2012Assignee: Array BioPharma Inc.Inventors: Yvan Le Huerou, James F. Blake, Indrani W. Gunawardana, Peter J. Mohr, Eli M. Wallace, Bin Wang, Mark Joseph Chicarelli, Michael Lyon
-
Patent number: 8178538Abstract: The present invention is concerned with novel pyridazinones of formula (I) wherein R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used for the treatment of CNS disorders.Type: GrantFiled: November 30, 2009Date of Patent: May 15, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Daniela Alberati, Luca Gobbi, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Rosa Maria Rodriguez-Sarmiento, Mark Rogers-Evans, Markus Rudolph
-
Publication number: 20120101103Abstract: Compounds of Formula I: (I) in which A, A1, R1, R7a, R7b, R8 and R10 have the meanings given in the specification, are DP2 receptor inhibitors useful in the treatment of useful in the treatment and prevention of immunologic diseases, allergic diseases such as asthma, allergic rhinitis and atopic dermatitis, and other inflammatory diseases mediated by prostaglandin D2 (PGD2). The compounds of Formula I may also be useful in treating diseases or medical conditions involving the Th2 T cell via production of IL-4, IL-5 and/or IL-13.Type: ApplicationFiled: December 18, 2009Publication date: April 26, 2012Applicant: ARRAY BIOPHARMA INC.Inventors: Adam Cook, Kevin W. Hunt, Robert Kirk Delisle, Todd Romoff, Christopher T. Clark, Ganghyeok Kim, Christopher P. Corrette, George A. Doherty, Laurence E. Burgess
-
Patent number: 8163749Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, R3 and R11 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.Type: GrantFiled: December 13, 2006Date of Patent: April 24, 2012Assignee: Bristol-Myers Squibb CompanyInventor: James R. Corte
-
Patent number: 8129388Abstract: The present invention discloses compounds of formula: where Ar1, Ar2, X, R3, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a “Phenylene Compound”); compositions comprising an effective amount of a Phenylene Compound; and methods for treating pain and other conditions in an animal comprising administering to an animal in need thereof an effective amount of a Phenylene Compound.Type: GrantFiled: June 10, 2011Date of Patent: March 6, 2012Assignee: Purde Pharma L.P.Inventor: Qun Sun
-
Publication number: 20120040991Abstract: Disclosed are 3-azabicyclo[4.1.0]heptane derivatives of formula (I) and their use as orexin receptor antagonists.Type: ApplicationFiled: April 23, 2010Publication date: February 16, 2012Applicant: Glaxo Group LimitedInventors: David Amantini, Romano Di Fabio, Massimo Gianotti, Francesca Pavone, Francesco Ferroni
-
Publication number: 20120028951Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on. A compound of formula (I0), wherein R1 represents a substituent; R2 represents a hydrogen atom, or a substituent; R3 represents a hydrogen atom, or a substituent; Ring A represents an aromatic ring which can be substituted, and Ring B represents a 5-membered heteroaromatic ring which can be substituted, or a salt thereof.Type: ApplicationFiled: February 4, 2010Publication date: February 2, 2012Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Takahiko Taniguchi, Akira Kawada, Mitsuyo Kondo, John F. Quinn, Jun Kunitomo, Masato Yoshikawa, Makoto Fushimi
-
Publication number: 20120028988Abstract: Since a pyridazinone compound shown by formula (I) has an activity for controlling arthropod pests, the pyridazinone compound is effective for a use for controlling arthropod pests.Type: ApplicationFiled: March 24, 2010Publication date: February 2, 2012Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Norihisa Sakamoto, Takafumi Fusaka
-
Patent number: 8106053Abstract: To find a compound having a tissue fibrinosis-inhibitory activity and a fibrinolytic activity, and to provide a novel compound that is useful for preventing and/or treating tissue fibrinosis diseases (pulmonary fibrosis, renal fibrosis etc.), diseases caused by pathological blood clots such as ischemic heart diseases (myocardial infarction, angina), intraatrial thrombus, pulmonary embolism, deep venous thrombosis, disseminated intravascular coagulation, ischemic cerebral diseases (cerebral infarction, cerebral bleeding) and arteriosclerosis and the like. To provide a pharmaceutical drug comprising a 5-phenyl-3-pyridazinone derivative represented by the following general formula (I): and an optical isomer thereof, or a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof, useful for preventing and/or treating disease conditions or symptoms mediated by plasminogen activator inhibitor-1.Type: GrantFiled: June 19, 2008Date of Patent: January 31, 2012Assignee: Kowa Company, Ltd.Inventors: Noriaki Gomi, Shinji Ina, Kenjirou Yamana, Yoshio Kaneko
-
Patent number: 8076370Abstract: Provided herein are substituted aromatic compounds, which are tRNA synthetase inhibitors, and hence can be used as antimicrobial agents. Compounds described herein can be used for the treatment or prevention of a condition caused by or contributed to by gram positive, gram negative, anaerobic bacteria or fungal organisms, more particularly against bacterium, for example, Staphylococci, Enterococci, Streptococci, Haemophilus, Moraxalla, Escherichia, Chlamydia, Mycoplasm, Legionella, Mycobacterium, Helicobacter, Clostridium, Bacteroides, Corynebacterium, Bacillus or Enterobactericeae, and fungal organisms, for example, Aspergillus, Blastomyces, Candida, Coccidiodes, Cryptococcus, Epidermophyton, Hendersonula, Histoplasma, Microsporum, Paecilomyces, Paracoccidiodes, Pneumocystis, Trichophyton, or Trichosporium. Processes for the preparation of these compounds, pharmaceutical compositions thereof, and methods of treating microbial infections are also provided.Type: GrantFiled: May 3, 2006Date of Patent: December 13, 2011Assignee: Ranbaxy Laboratories LimitedInventors: Biswajit Das, Jasbir Singh Arora, Shahadat Ahmed, Anish Bandyopadhyay, Rita Katoch, Santosh Haribhau Kurhade, Sujata Rathy, Soma Ghosh, Abhijit Datta Khoje, Arti Gujrati, Dilip J. Upadhyay
-
Publication number: 20110301110Abstract: A method for diagnosing a chronic myelomonocytic leukemia (CMML) in a subject includes the steps of (i) determining the level of expression of the Trim33 (tripartite motif-containing 33) gene in a biological sample from the subject, and (ii) comparing the level of expression of the Trim33 gene in the biological sample with its normal level of expression; wherein an under-expression of the Trim33 gene is associated with CMML, and to a kit for diagnosing CMML in a subject including at least one nucleic acid probe or oligonucleotide or at least one antibody, which can be used in a such a method.Type: ApplicationFiled: June 2, 2011Publication date: December 8, 2011Inventors: Aucagne Romain, Bastie Jean Noël, Delva Laurent, Droin Nathalie, Solary Eric
-
Patent number: 8067590Abstract: The present invention relates to compounds of general formula I wherein the groups and radicals B, k, L, U, V, W, X, Y, Z, R1, R2, have the meanings given in claim 1. Moreover the invention relates to pharmaceutical compositions containing at least one compound according to the invention. By virtue of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.Type: GrantFiled: August 24, 2007Date of Patent: November 29, 2011Assignee: Boehringer Ingelheim International GmbHInventors: Dirk Stenkamp, Stephan Georg Mueller, Gerald Juergen Roth, Joerg Kley, Klaus Rudolf, Armin Heckel, Marcus Schindler, Ralf Lotz, Thorsten Lehmann-Lintz
-
Publication number: 20110281883Abstract: The present invention relates to the use of compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, R7, r, Y and G have the meanings given above as insecticides and/or acaricides and/or fungicides.Type: ApplicationFiled: January 14, 2010Publication date: November 17, 2011Applicant: Bayer Cropscience AGInventors: Reiner Fischer, Stefan Lehr, Arnd Voerste
-
Publication number: 20110275625Abstract: Disclosed are compounds and compositions of the formula (I) as described herein which are inhibitors of MMP-13. Also disclosed are methods of using and making compounds of the formula (I).Type: ApplicationFiled: November 5, 2009Publication date: November 10, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Neil Alexander Farrow, Donghong Amy Gao, Alexander Heim-Riether, Shuang Liang, Sabine Schlyer, Lana Louise Smith Keenan, Steven John Taylor, Bernd Wellenzohn, Dieter Wiedenmayer, Zhaoming Xiong, Qiang Zhang
-
Patent number: 8048885Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I) wherein the substituents are as defined in the specification and to processes for their production to pharmaceutical compositions comprising them and to their use in the manufacture of a medicament for the treatment and/or delay of progression of psychotic and nemodegenerative disorders.Type: GrantFiled: March 26, 2010Date of Patent: November 1, 2011Assignee: Novartis AGInventors: Dominik Feuerbach, Mathias Frederiksen, Konstanze Hurth, Bernard Lucien Roy, Beatrix Wagner
-
MODULATORS OF THE PROSTACYCLIN (PGI2) RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
Publication number: 20110245251Abstract: Cyclohexane derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.Type: ApplicationFiled: December 7, 2009Publication date: October 6, 2011Applicant: Arena Pharmaceuticals, Inc.Inventors: Thuy-Anh Tran, Rena Hayashi, Jason B. Ibarra, Brett Ullman, Ning Zou -
Patent number: 8026370Abstract: According to the present invention, a compound represented by the following formula (I) having a superior PPAR? agonist action and concurrently showing a hypolipidemic action can be provided, and further, a compound useful as a synthetic intermediate for the compound can be provided.Type: GrantFiled: November 4, 2005Date of Patent: September 27, 2011Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Takashi Tozawa, Osamu Tsuruta, Hiroshi Kitajima, Yoshiyuki Aoki, Naoko Ando, Hiroki Tamakawa
-
Patent number: 8022221Abstract: The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R3, R4, R6, R7 and R8 are defined herein, which are capable of modulating Aurora kinase protein activity, thereby influencing various disease states and conditions related to the activities of Aurora kinase proteins. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, processes of preparing compounds of the invention, synthetic intermediates and methods of treatment of conditions related to the activity of Aurora kinase.Type: GrantFiled: February 12, 2009Date of Patent: September 20, 2011Assignee: Amgen Inc.Inventors: Victor J. Cee, Holly L. Deak, Bingfan Du, Stephanie D. Geuns-Meyer, Brian L. Hodous, Hanh Nho Nguyen, Philip R. Olivieri, Vinod F. Patel, Karina Romero, Laurie Schenkel
-
Patent number: 8022073Abstract: A pyridazine compound of the formula: has an excellent plant disease controlling effect.Type: GrantFiled: November 28, 2006Date of Patent: September 20, 2011Assignee: Sumitomo Chemical Company, LimitedInventors: Shin-ichiro Souma, Akio Manabe
-
Patent number: 8003806Abstract: The invention relates to compounds of the Formula 1 and to pharmaceutically acceptable salts and solvates thereof, wherein A, X2, X4, X5 and X1 are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals by administering the compounds of Formula 1 and to pharmaceutical compositions for treating such disorders which contain the compounds of Formula 1.Type: GrantFiled: November 9, 2005Date of Patent: August 23, 2011Assignee: OSI Pharmaceuticals, LLCInventors: Jason Bloxham, Gary V. Borzillo, Eric William Collington, Shazia Sadiq, Colin Peter Sambrook Smith, Chris L. Waller, Graham M. Wynne
-
Patent number: 7994171Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.Type: GrantFiled: March 10, 2010Date of Patent: August 9, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Kap-Sun Yeung, Kyle E. Parcella, John A. Bender, Brett R. Beno, Katharine A. Grant-Young, Ying Han, Piyasena Hewawasam, John F. Kadow, Andrew Nickel
-
Publication number: 20110178058Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.Type: ApplicationFiled: January 14, 2011Publication date: July 21, 2011Applicant: Gilead Sciences, Inc.Inventors: Eda CANALES, Lee S. Chong, Michael O' Neil Hanrahan Clarke, Edward Doerffler, Scott E. Lazerwith, Willard Lew, Michael Mertzman, Philip A. Morganelli, William J. Watkins
-
Publication number: 20110178092Abstract: Described are novel protease inhibitors and methods for using said protease inhibitors in the treatment of human immunodeficiency virus (HIV) infection.Type: ApplicationFiled: December 19, 2007Publication date: July 21, 2011Inventors: Akbar Ali, Michael D. Altman, Saima G. Anjum, Hong Cao, Sripriya Chellappan, Miguel X. Fernandes, Michael K. Gilson, Visvaldas Kairys, Nancy King, Ellen Nalivaika, Moses Prabu, Tariq M. Rana, Kiran Kumar Sai, Celia A. Schiffer, Bruce Tidor
-
Patent number: 7981890Abstract: A compound of the formula (I): wherein RH represents one or more optional substituents on the fused cyclohexene ring; R1 is selected from H and halo; RN is selected from H and optionally substituted C1-10 alkyl; and RC1 and RC2 are independently selected from H, R, C(?O)OR, where R is optionally substituted C1-10 alkyl, optionally substituted C5-20 aryl or optionally substituted C3-20 heterocyclyl; RC1 and RC2 together with the carbon atom to which they are attached may form an optionally substituted spiro-fused C5-7 carbocylic or heterocyclic ring.Type: GrantFiled: September 12, 2008Date of Patent: July 19, 2011Assignee: AstraZeneca ABInventors: Muhammad Hashim Javaid, Keith Allan Menear, Niall Morrison Barr Martin
-
Publication number: 20110166142Abstract: 2-Substituted isoflavonoid compounds and pharmaceutical compositions containing same are useful as anti-inflammatory agents and antioxidants and for the treatment of related diseases and conditions.Type: ApplicationFiled: June 30, 2008Publication date: July 7, 2011Inventors: Eleanor Eiffe, Andrew Heaton, Catherine Walker, Alan James Husband
-
Patent number: 7951805Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): Formula (I) where x, y, G, J, L, M, V, W, R2, R3, R4, R5, R5a, R6, R6a, R7, R7a, R8, and R8a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.Type: GrantFiled: September 20, 2005Date of Patent: May 31, 2011Assignee: Xenon Pharmaceuticals Inc.Inventors: Rajender Kamboj, Zaihui Zhang, Jianmin Fu, Serguei Sviridov, Shaoyi Sun, Mehran Seid Bagherzadeh, Vandna Raina, Duanjie Hou, Sultan Chowdhury, Shifeng Liu, Vishnumurthy Kodumuru, Nagasree Chakka
-
Publication number: 20110118272Abstract: Novel 3?-deoxy-3?-acylaminospectinomycin compounds are described. Also described are methods of using the 3?-deoxy-3-acylaminospectinomycin compounds and other spectinomycin analogs in treating tuberculosis and in treating microbial infections.Type: ApplicationFiled: July 26, 2010Publication date: May 19, 2011Inventors: Richard E. Lee, Jianjun Qi, Juilian G. Hurdle, Bernd Meibohm, Vnr Pavan Kumar Vaddady, Rakesh, Jiuyu Liu
-
Publication number: 20110118250Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A, B, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula I, or compositions including them, to a subject. The invention also comprises further embodiments of Formulas II and III, intermediates and processes useful for the preparation of compounds of the invention.Type: ApplicationFiled: October 21, 2010Publication date: May 19, 2011Applicant: Amgen Inc.Inventors: Brian K. Albrecht, Denise Lyn Andersen, Michael Bartberger, James Brown, Ryan Brown, Stuart C. Chaffee, Yuan Cheng, Michael Croghan, Russell Graceffa, Scott Harried, Stephen Hitchcock, Randall Hungate, Ted Judd, Matthew Kaller, Charles Kreiman, Daniel La, Patricia Lopez, Craig Masse, Holger Monenschein, Thomas Nguyen, Thomas Nixey, Vinod F. Patel, Lewis Pennington, Matthew Weiss, Qiufen Xue, Bryant Yang, Wenge Zhong
-
Patent number: 7943618Abstract: This application discloses pyridine and pyrimidine compounds according to formula I wherein R1, R2, R3, R4, R5, X1 and A are as described herein which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of formula I and at least one carrier, diluent or excipient.Type: GrantFiled: October 23, 2008Date of Patent: May 17, 2011Assignee: Roche Palo Alto LLCInventors: Nolan James Dewdney, Rama K. Kondru, Yan Lou, Michael Soth, Tobias Gabriel
-
Publication number: 20110112061Abstract: The present invention relates to a class of pyridazinones of formula I, which comprises 6-[3-(trifluoromethyl)phenyl]pyridazin-3(2H)-one as a mother nucleus, the preparation method thereof and the use thereof in manufacturing medicaments against tumors, especially liver cancer.Type: ApplicationFiled: March 18, 2009Publication date: May 12, 2011Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCESInventors: Youhong Hu, Liguang Lou, Shijun Lin, Hongbing Zhao, Zhende Liu, Yongping Xu, Bo Chao
-
Patent number: 7919487Abstract: This invention relates to compounds of formula (I): their compositions and methods of use thereof. The compounds (and compositions) are useful in modulating IL-12 production and processes mediated by IL-12.Type: GrantFiled: November 10, 2005Date of Patent: April 5, 2011Assignee: Synta Pharmaceuticals CorporationInventors: Lijun Sun, Shijie Zhang, Keizo Koya, Dinesh Chimmanamada, Hao Li, David James, Elena Kostik
-
Patent number: 7915246Abstract: The present invention provides a method of treating fibromyalgia syndrome (FMS), chronic fatigue syndrome (CFS), and pain in an animal subject. The method generally involves administering a therapeutically effective amount of a dual serotonin norepinephrine reuptake inhibitor compound or a pharmaceutically acceptable salt thereof, wherein said dual serotonin norepinephrine reuptake inhibitor compound is characterized by a non-tricyclic structure and an equal or greater inhibition of norepinephrine reuptake than serotonin reuptake. In particular, the use of milnacipran to treat FMS, CFS, and pain is disclosed.Type: GrantFiled: February 22, 2008Date of Patent: March 29, 2011Assignee: Cypress Bioscience, Inc.Inventors: Jay D. Kranzler, Srinivas G. Rao
-
Publication number: 20110070317Abstract: Compounds of Formula (I) are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula (I) and stereoisomers 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: May 13, 2009Publication date: March 24, 2011Applicant: ARRAY BIOPHARMA INC.Inventors: Yvan Le Huerou, James F. Blake, Indrani W. Gunawardana, Peter J. Mohr, Eli M. Wallace, Bin Wang, Mark Joseph Chicarelli, Michael Lyon
-
Patent number: 7888342Abstract: The present invention provides a method of treating fibromyalgia syndrome (FMS), chronic fatigue syndrome (CFS), and pain in an animal subject. The method generally involves administering a therapeutically effective amount of a dual serotonin norepinephrine reuptake inhibitor compound or a pharmaceutically acceptable salt thereof, wherein said dual serotonin norepinephrine reuptake inhibitor compound is characterized by a non-tricyclic structure and an equal or greater inhibition of norepinephrine reuptake than serotonin reuptake. In particular, the use of milnacipran to treat FMS, CFS, and pain is disclosed.Type: GrantFiled: December 22, 2009Date of Patent: February 15, 2011Assignee: Cypress Bioscience, Inc.Inventors: Jay D. Kranzler, Srinivas G. Rao