Bicyclo Ring System Having The 1,3-diazine As One Of The Cyclos Patents (Class 514/258.1)
  • Publication number: 20110269623
    Abstract: PROBLEM There are provided a composition for controlling plant diseases and a method for controlling plant diseases having excellent control effect for plant diseases. SOLUTION A composition for controlling plant diseases comprising, as active ingredients, a compound represented by formula (1), wherein X1 represents a methyl group, a difluoromethyl group or an ethyl group; X2 represents a methoxy group or a methylamino group; and X3 represents a phenyl group, a 2-methylphenyl group or a 2,5-dimethylphenyl group, and at least one azole compound selected from the group consisting of bromuconazole, cyproconazole, difenoconazole, fenbuconazole, fluquinconazole, hexaconazole, imibenconazole, ipconazole, myclobutanil, prothioconazole, simeconazole, tetraconazole, triticonazole and metconazole.
    Type: Application
    Filed: November 20, 2009
    Publication date: November 3, 2011
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Masanao Takaishi, Masato Soma
  • Patent number: 8044058
    Abstract: Disclosed is the use of merocyanine derivatives of formula Q is hydrogen; C1-C22alkyl; —OH; —OR7; —NR7R8; or —N?R9; R1 is hydrogen; C1-C22alkyl; —OR7, —SR7; —NR7R8; C1-C22alkyl; C2-C12 alkenyl; C2-C12alkinyl; C3-C12cycloalkyl; C3-C12cycloalkenyl; C7-C12aralkyl; C1-C12heteroalkyl, C2-C11heteroaralkyl; C6-C10aryl; or C1-C9heteroaryl; R4 is cyano; COR7, COOR7; CONR7R8; SO2(C6-C12)aryl; C2-C12alk-1-enyl; C3-C12cycloalk-1-enyl; C2-C12alk-1-inyl; C2-C12heteroalkyl; C3-C5heterocycloalkyl; C6-C10aryl; or C1-C9heteroaryl; R5 is —COR7; —COOR7; —OR7; —SR7, —NHR7, —NR7R8; C1-C22alkyl; C2-C12alkenyl; C2-C12alkinyl; C3-C12cycloalkyl; C3-C12cycloalkenyl; C7-C12aralkyl; C1-C12alkylphenyl; C1-C12alkoxy-C6-C10aryl; C1-C12heteroalkyl; C2-C11heteroaralkyl; C3-C12cycloheteroalkyl; C6-C10aryl; C1-C12alkoxy-C6-C10aryl; or C1-C9heteroaryl; R6 is hydrogen; C1-C22alkyl; C1-C22alkoxy; or COR7; R7 and R8 independently from each other are hydrogen; C1-C22alkyl; C2-C12alkenyl; C2-C12alkinyl; C3-C12cycloalkyl; C3-C12cycloalkenyl; —(C
    Type: Grant
    Filed: March 2, 2010
    Date of Patent: October 25, 2011
    Assignee: BASF SE
    Inventors: Barbara Wagner, Frank Bienewald, Heinz Wolleb, Olof Wallquist, Bernd Herzog, Thomas Ehlis, Jürg Haase
  • Publication number: 20110251181
    Abstract: Compounds of Formula I are useful for inhibiting AKT protein kinases. Methods 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. Formula (I).
    Type: Application
    Filed: January 9, 2009
    Publication date: October 13, 2011
    Applicants: Genentech, Inc., Array BoPharma Inc.
    Inventors: Anna Banka, Josef R. Bencsik, James Blake, Martin Hentermann, Stephen T. Schlachter, Eli M. Wallace, Rui Xu
  • Publication number: 20110243911
    Abstract: The present invention is directed to the use of a compound capable of reducing the uric acid level in a mammal for the prevention and/or the treatment of IL-1? driven lung pathology, particularly to treat lung inflammation such as chronic fibrosis, COPD and interstitial fibrosis and other IL-1? driven lung pathologies including those of autoimmune origin. Preferred compounds capable of reducing the uric acid level are selected from the group consisting of xanthine oxidase inhibitors, such as allopurinol, recombinant enzyme uricase and uricosuric compound capable of enhancing uric acid excretion, such as probenecid. The invention further relates to a method for identifying in vitro whether a patient presents an IL-1? driven lung pathology or is at risk to develop an IL-1? driven lung pathology, or for the screening of a compound for treating an IL-1? driven lung pathology.
    Type: Application
    Filed: September 18, 2009
    Publication date: October 6, 2011
    Inventors: Bernhard Ryffel, Isabelle Couillin
  • Publication number: 20110224227
    Abstract: Methods for reducing or preventing the effects of cytotoxic compounds in healthy cells are provided. The methods relate to the use of selective cyclin-dependent kinase (CDK) 4/6 inhibitors to induce transient quiescence in CDK4/6 dependent cells, such as hematopoietic stem cells and/or hematopoietic progenitor cells. Also described is a method of selecting compounds for reducing or preventing the effects of cytotoxic agents compounds in healthy cells.
    Type: Application
    Filed: October 1, 2009
    Publication date: September 15, 2011
    Inventors: Norman E. Sharpless, Jay C. Strum, John E. Bisi, Patrick J. Roberts, Matthew R. Ramsey
  • Publication number: 20110224155
    Abstract: The present invention includes methods for identifying modifiers of chemosensory receptors and their ligands, e.g., by determining whether a test entity is suitable to interact with one or more interacting sites within the Venus flytrap domains of the chemosensory receptors, and modifiers capable of modulating chemosensory receptors and their ligands. The present invention also includes modifiers of chemosensory receptors and their ligands having Formula (I), its subgenus, and specific compounds. Furthermore, the present invention includes ingestible compositions comprising the modifiers of chemosensory receptors and their ligands and methods of using the modifiers of chemosensory receptors and their ligands to enhance the sweet taste of an ingestible composition or treat a condition associated with a chemosensory receptor. In addition, the present invention include processes for preparing the modifiers of chemosensory receptors and their ligands.
    Type: Application
    Filed: June 3, 2008
    Publication date: September 15, 2011
    Applicant: SENOMYX INC.
    Inventors: Catherine Tachdjian, Donald S. Karanewsky, Xiao-Qing Tang, Xiaodong Li, Feng Zhang, Guy Servant, Qing Chen, Vincent Darmohusodo, Richard Fine, Joseph R. Fotsing, Jeffrey Robert Hammaker, Xinshan Kang, Rachel D.A. Kimmich, Boris Klebansky, Haitian Liu, Goran Petrovic, Marketa Rinnova, Sara Adamski-Werner, Jeffrey Yamamoto, Hong Zhang, Albert Zlotnik, Mark Zoller, Karen Zoller
  • Publication number: 20110224197
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinases, such as inhibitors of GSK-3. The invention provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders. The invention provides processes for preparing compounds of the invention. The invention provides methods of identifying compounds useful for treatment of diabetes, diabetic neuropathy, osteoporosis, Alzheimer's disease, Huntington's disease, Parkinson's disease, AIDS-associated dementia, bipolar disorder, amyotrophic lateral sclerosis, multiple sclerosis, schizophrenia, leukocytopenia, cardiomyocyte hypertrophy, stroke, post-stroke, spinal cord injury, traumatic brain injury, Charcot-Marie-Tooth, peripheral nerve regeneration, and rheumatoid arthritis.
    Type: Application
    Filed: September 9, 2010
    Publication date: September 15, 2011
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Gregory William Henkel, Michael Liu, Timothy Neuberger
  • Patent number: 8012950
    Abstract: Disclosed are methods for detecting and treating joint disease. The methods of diagnosis include determining increased expression of enzymes that are upregulated during the progress of joint and ligament inflammation and degeneration. In addition, disclosed are methods of treating the disease including inhibiting the activity of responsible proteases.
    Type: Grant
    Filed: August 30, 2004
    Date of Patent: September 6, 2011
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Peter Muir, Ray Vanderby, Jr., Paolo Pepe Provenzano
  • Publication number: 20110212937
    Abstract: The present disclosure provides a series of compounds of the formula (I) which modulate ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by ?-amyloid peptide (?-AP) production.
    Type: Application
    Filed: July 28, 2010
    Publication date: September 1, 2011
    Inventors: Kenneth M. Boy, Jason M. Guernon, John E. Macor, Richard E. Olson, Jianliang Shi, Lorin A. Thompson, III, Yong-Jin Wu, Li Xu, Yunhui Zhang, Dmitry S. Zuev
  • Publication number: 20110201628
    Abstract: The present invention relates to compounds of Formula (I) and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds provide a treatment for myeloproliferative disorders and cancer.
    Type: Application
    Filed: September 29, 2009
    Publication date: August 18, 2011
    Inventors: Claudio Edmundo Chuaqui, Shan Huang, Stephanos Ioannidis, Jie Shi, Mei Su, Qibin Su
  • Publication number: 20110195965
    Abstract: The present invention relates to the use of tetrahydro- and dihydroquinazolinones of formula (I) as protein kinase activators or inhibitors, a method for their manufacture, their use for the preparation of a medicament for the treatment of diseases, their use for the manufacture of a pharmaceutical composition and new tetrahydro- and dihydroquinazolinones.
    Type: Application
    Filed: April 12, 2011
    Publication date: August 11, 2011
    Inventors: Dirk FINSINGER, Armin De Meijere
  • Publication number: 20110183986
    Abstract: Polycyclic aryl and polycyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl catalytic activity are also disclosed.
    Type: Application
    Filed: April 1, 2011
    Publication date: July 28, 2011
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Dane Goff, Jiaxin Yu, Sacha Holland, Thilo J. Heckrodt, Pingyu Ding, Joane Litvak, Jing Zhang
  • Publication number: 20110178105
    Abstract: Methods are provided for maintaining or lowering lipoprotein-associated phospholipase A2 [“Lp-PLA2”] levels, stabilizing rupture prone-atherosclerotic lesions, decreasing the Inflammatory Index and increasing Total Omega-3 Score™ in humans, by administering an effective amount of eicosapentaecnoic acid [“EPA”], an omega-3 polyunsaturated fatty acid [“PUFA”].
    Type: Application
    Filed: January 10, 2011
    Publication date: July 21, 2011
    Applicant: E.I. DU PONT DE NEMOURS AND COMPANY
    Inventors: PETER JOHN GILLIES, Ernst John Schaefer
  • Publication number: 20110173726
    Abstract: The present invention relates to a method for controlling invertebrate pests which method comprises treating the pests, their food supply, their habitat or their breeding ground or a plant, seed, soil, area, material or environment in which the pests are growing or may grow, or the materials, plants, seeds, soils, surfaces or spaces to be protected from pest attack or infestation with a pesticidally effective amount of a pyrazole compound of formulae I or II or a salt or an N-oxide thereof, wherein A is a pyrazole radical of the formulae A1 or A2, wherein # denotes the binding; D is a 5- or 6-membered heterocyclic radical fused to the pyrazole moiety; Rp1, Rp2 and Rpx are H, halogen, CN, NO2, C1-C10-alkyl, C2-C10-alkenyl, C2-C10-alkynyl, etc.
    Type: Application
    Filed: September 23, 2009
    Publication date: July 14, 2011
    Applicant: BASF SE
    Inventors: Steffen Groß, Karsten Körber, Wolfgang Von Deyn, Florian Kaiser, Ronan Le Vezouet, Sebastian Sörgel, Matthias Pohlman, Prashant Deshmukh, Joachim Dickhaut, Douglas D. Anspaugh, Deborah L. Culbertson, Hassan Oloumi-Sadeghi
  • Publication number: 20110172249
    Abstract: The present invention provides a method for improving absorbability of the active ingredient of an enteric polymer coated preparation, which includes using an organic acid.
    Type: Application
    Filed: September 2, 2009
    Publication date: July 14, 2011
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMTED
    Inventors: Kazuhisa Kamikawa, Takayuki Okabe, Miho Nakamura
  • Patent number: 7977342
    Abstract: The present invention relates to the use of bi-cyclic pyrimidines as inhibitors of HCV replication as well as their use in pharmaceutical compositions aimed to treat or combat HCV infections. In addition, the present invention relates to processes for preparation of such pharmaceutical compositions. The present invention also concerns combinations of the present bi-cyclic pyrimidines with other anti-HCV agents.
    Type: Grant
    Filed: March 9, 2007
    Date of Patent: July 12, 2011
    Assignee: Tibotec-Virco Virology BVBA
    Inventors: Kenneth Alan Simmen, Tse-I Lin, Oliver Lenz, Dominique Louis Nestor Ghislain Surleraux, Pierre Jean-Marie Bernard Raboisson
  • Patent number: 7977343
    Abstract: Novel adenine derivatives of the formula (I), in which R1, R2, R3, X and Y have the meanings indicated in Claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.
    Type: Grant
    Filed: July 20, 2006
    Date of Patent: July 12, 2011
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Hans-Peter Buchstaller, Hans-Michael Eggenweiler, Bertram Cezanne, Michael Wolf
  • Publication number: 20110165183
    Abstract: The invention provides a compound of formula (I): wherein W is a bicyclic heteroaromatic group; or a salt thereof. The compounds and salts thereof have beneficial therapeutic properties (e.g. immunosuppressant properties).
    Type: Application
    Filed: July 31, 2009
    Publication date: July 7, 2011
    Applicant: BioCryst Pharmaceuticals, Inc.
    Inventors: Yarlagadda S. Babu, Pooran Chand, Pravin L. Kotian, V. Satish Kumar
  • Patent number: 7964204
    Abstract: Disclosed are compounds of Formula (1), including all geometric and stereoisomers, N-oxides, and salts thereof, Formula (1): wherein A1, A2, A3, A4, A5 and A6 are independently, selected from the group consisting of CR3 and N; provided that at most 3 of A1, A2, A3; A4, A5 and A6 is N; B1, B2 and B3 are independently selected from the group consisting of CR2. and N; each R3 is independently H, halogen, C1-C6 alkyl, C1-C6 haloalkyl, C3-C6 cycloalkyl, C3-C6 halocycloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 haloalkylthio, C1-C6 alkylsulfinyl, C1-C6 haloalkylsulfinyl, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfo?yl, C1-C6 alkylamino, C2-G6 dialkylamino, —CN or —NO2; and R1, R2, R4, R5, W and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula (1) and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Grant
    Filed: December 28, 2006
    Date of Patent: June 21, 2011
    Assignee: E.I. du Pont de Nemours and Company
    Inventors: George Philip Lahm, Wesley Lawrence Shoop, Ming Xu
  • Patent number: 7960394
    Abstract: This invention provides a compound or its pharmaceutically-acceptable salt of formula (I) wherein R1 represents a lower alkyl group et al; R2 and R3 are same and different and represents hydrogen atm et al; R4 represents the substituent of the formula (II) et al; X1 represents NH, O or S; Y represents N or C; Ar is a divalent substituent derived from aryl et al, by removing two hydrogen atoms therefrom; the ring A represents a 5- or 6-membered heteroaryl group; this compounds has a histamine-H3 receptor antagonistic effect or a histamine-H3 receptor inverse-agonistic effect and is useful for preventive or remedy of metabolic system diseases, circulatory system diseases or nervous system diseases.
    Type: Grant
    Filed: May 30, 2005
    Date of Patent: June 14, 2011
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Takashi Mizutani, Tsuyoshi Nagase, Nagaaki Sato, Akio Kanatani, Shigeru Tokita
  • Patent number: 7947690
    Abstract: The present invention provides a condensed pyrimidine compound represented by formula (I) or pharmaceutically acceptable salt thereof: where A represents a ring where at least one carbon atom within said ring is optionally substituted with one or more groups selected from the group consisting of lower alkyl, —O-(lower alkyl), halogen atom, carboxyl, —CO2-(lower alkyl), and carbamoyl, R1 represents: (1) phenyl substituted with at least three halogen atoms, which may have at least one additional substituent, or (2) cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl, each of which is optionally substituted; and R2 represents a group represented by formula (II) or an optionally substituted cyclic amino: wherein R21 and R22 may be identical or different and each represents —H, lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, phenyl, heteroaryl, non-aromatic heterocyclyl, or —O-(lower alkyl), each of which is optionally substituted.
    Type: Grant
    Filed: October 17, 2005
    Date of Patent: May 24, 2011
    Assignee: Astellas Pharma Inc.
    Inventors: Yasuhiro Yonetoku, Kenji Negoro, Kenichi Onda, Masahiko Hayakawa, Daisuke Sasuga, Takahiro Nigawara, Kazuhiko Iikubo, Hiroyuki Moritomo, Shigeru Yoshida, Takahide Ohishi
  • Publication number: 20110118257
    Abstract: The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.
    Type: Application
    Filed: November 3, 2010
    Publication date: May 19, 2011
    Applicants: Rhizen Pharmaceuticals SA, Incozen Therapeutics Pvt. Ltd.
    Inventors: Meyyappan MUTHUPPALANIAPPAN, Srikant VISWANADHA, Govindarajulu BABU, Swaroop Kumar V.S. VAKKALANKA
  • Patent number: 7939537
    Abstract: Pyridopyrimidine carboxamide compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein R1, R2, R3, R4, R5 and R6 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Grant
    Filed: September 26, 2006
    Date of Patent: May 10, 2011
    Assignee: Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.p.A.
    Inventors: Vincenzo Summa, Olaf Kinzel, Monica Donghi
  • Publication number: 20110092521
    Abstract: The invention relates to treating a disease or condition in which it is desirable to inhibit 5?-methylthioadenosine phosphorylase (MTAP) and/or 5?-methylthioadenosine nucleosidase (MTAN). The invention particularly relates to the co-administration of 5?-methylthioadenosine (MTA), or a prodrug of MTA, with one or more MTAP/MTAN inhibitors. Included among the diseases treatable are prostate cancer and head and neck cancer.
    Type: Application
    Filed: February 23, 2007
    Publication date: April 21, 2011
    Inventors: Richard Hubert Furneaux, Peter Charles Tyler, Gary Brian Evans, Vern L. Schramm
  • Patent number: 7915265
    Abstract: The invention features pharmaceutical compositions that include dipyridamole and a corticosteroid.
    Type: Grant
    Filed: February 15, 2006
    Date of Patent: March 29, 2011
    Assignee: Zalicus Inc.
    Inventors: Curtis Keith, Alexis Borisy, Grant Zimmermann, Edward Roydon Jost-Price, Palaniyandi Manivasakam, Nicole W. Hurst, Michael A. Foley
  • Publication number: 20110071133
    Abstract: Bicyclic aryl substituted triazoles or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.
    Type: Application
    Filed: December 1, 2010
    Publication date: March 24, 2011
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Pingyu Ding, Thilo J. Heckrodt, Joane Litvak
  • Patent number: 7902202
    Abstract: Provided herein are compounds, compositions and methods for the treatment of liver disorder, including HCV and/or HBV infections. Specifically, compound and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents.
    Type: Grant
    Filed: April 25, 2008
    Date of Patent: March 8, 2011
    Assignees: Idenix Pharmaceuticals, Inc., L'Université Montpellier II
    Inventors: Jean-Pierre Sommadossi, Gilles Gosselin, Claire Pierra, Christian Perigaud, Suzanne Peyrottes
  • Patent number: 7902203
    Abstract: The present invention provides an HCV polymerase inhibiting compound having the formula (I) and a composition comprising a therapeutically effective amount of said compound. The present invention also provides a method for inhibiting hepatitis C virus (HCV) polymerase, a method for inhibiting HCV viral replication, and a method for treating or preventing HCV infection. Processes for making said compounds, and synthetic intermediates employed in said processes, are also provided.
    Type: Grant
    Filed: October 31, 2003
    Date of Patent: March 8, 2011
    Assignee: Abbott Laboratories, Inc.
    Inventors: John K. Pratt, David A. Betebenner, Pamela L. Donner, Brian E. Green, Dale J. Kempf, Keith F. McDaniel, Clarence J. Maring, Vincent S. Stoll, Rong Zhang, Hui-Ju Chen, William J. Flosi, Larry L. Klein, Allan C. Krueger, Dachun Liu, Darold L. Madigan, Laura M. Maymon, Todd W. Rockway, Kent D. Stewart, Ming C. Yeung, Qinghua Xie
  • Publication number: 20110053959
    Abstract: The present invention provides compounds of Formula (I) including tautomers, resolved enantiomers, resolved diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. Also provided are methods of using the compounds of this invention as Akt protein kinase inhibitors and for the treatment of Akt-mediated diseases, for example, hyperproliferative diseases such as cancer.
    Type: Application
    Filed: January 9, 2009
    Publication date: March 3, 2011
    Applicant: ARRAY BIOPHARMA INC.
    Inventors: Anna Banka, Josef R. Bencsik, James F. Blake, Kin Chiu Fong, Martin F. Hentemann, Ian S. Mitchell, Douglas McCord Sammond, Tony P. Tang, Eli M. Wallace, Rui Xu
  • Publication number: 20110046162
    Abstract: The present application relates to novel substituted fused cyanopyridine derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, preferably for the treatment and/or prevention of cardiovascular disorders.
    Type: Application
    Filed: December 9, 2008
    Publication date: February 24, 2011
    Applicant: BAYER SCHERING PHARMA
    Inventors: Peter Nell, Alexandros Vakalopoulos, Frank Süssmeier, Barbara Albrecht-Küpper, Katja Zimmermann, Jörg Keldenich, Daniel Meibom
  • Patent number: 7888359
    Abstract: The invention relates to antibiotic cyclohexyl or piperidinyl carboximide derivatives of formula (I) wherein R1 represents hydrogen, halogen, (C1-C4)alkyl, (C1-C4)alkoxy, cyano or COOR2, R2 being (C1-C4)alkyl; one or two of U, V, W and X represent(s) N and the remaining represent each CH, or, in the case of X, may also represent CRX, RX being a halogen atom; either B represents N and A represents CH2CH2 or CH(OR3)CH2, or B represents CH or C(OR4) and A represents OCH2, CH2CH(OR5), CH(OR6)CH2, CH(OR7)CH(OR8), CH?CH or CH2CH2; each of R3, R4, R5, R6, R7, and R8 represents independently hydrogen, SO3H, PO3H2, CH2OPO3H2 or COR9, R9 being either CH2CH2COOH or such that R9—COOH is naturally occurring amino acid or dimethylaminoglycine; and to salts of such compounds of formula (I).
    Type: Grant
    Filed: March 22, 2007
    Date of Patent: February 15, 2011
    Assignee: Actelion Pharmaceutical Ltd.
    Inventors: Christian Hubschwerlen, Rueedi Georg, Jean-Philippe Surivet, Cornelia Zumbrunn Acklin
  • Patent number: 7879861
    Abstract: A series of new chemical agents that demonstrate anti-tumor activity are described. The new chemical agents combine two major mechanisms of anti-tumor action. In an embodiment, the agents are capable of both inhibiting EGFR and damaging DNA while also, upon degradation, degrading to an inhibitor of EGFR and to an agent capable of damaging DNA. Moreover, a novel series of molecules capable of releasing two moles of EGFR inhibitor and a potent bi-functional alkylating agent are also described.
    Type: Grant
    Filed: June 14, 2005
    Date of Patent: February 1, 2011
    Inventors: Bertrand Jean-Claude, Zakaria Rachid, Fouad Brahimi
  • Patent number: 7879863
    Abstract: The present invention provides a novel compound having a kininogenase-inhibitory action and its pharmaceutical use. The compounds are represented by the formulas (A), (B), (C), (E) and (H): wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: September 29, 2006
    Date of Patent: February 1, 2011
    Assignee: Ajinomoto Co., Inc.
    Inventors: Munetaka Tokumasu, Masayuki Sugiki, Haruko Hirashima, Hideki Matsumoto, Toshihiko Yoshimura, Yasuko Nogi, Mitsuo Takahashi, Manabu Kitazawa, Akiko Oonuki, Naoyuki Fukuchi, Yoichiro Shima
  • Publication number: 20110009435
    Abstract: The present invention relates to compounds of Formula I and pharmaceutically acceptable salts thereof, processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds as anti-inflammatory agents.
    Type: Application
    Filed: May 19, 2008
    Publication date: January 13, 2011
    Applicant: Pfizer, Inc.
    Inventors: Mark E. Schnute, Peter G. Ruminski, Cathleen E. Hanau, Joseph W. Stobach, Jeffery Carroll, Kirby Sample
  • Patent number: 7851468
    Abstract: The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions that include substituted heterobicyclic pyrimidines of Formula (I): wherein R1, R2, R3, R4, R5, X, W, and ring A are as defined herein; pharmaceutical compositions of substituted heterobicyclic pyrimidines of Formula (I); and their use in the treatment of chronic neurodegenerative diseases, neurotraumatic diseases, depression and/or diabetes. More particularly, the present invention relates to substituted pyrazolopyrimidines of Formula (I).
    Type: Grant
    Filed: May 14, 2007
    Date of Patent: December 14, 2010
    Assignee: Cephalon, Inc.
    Inventors: Edward R. Bacon, Thomas Bailey, Nadine C. Becknell, Diane E. Gingrich, Greg Hostetler, Robert L. Hudkins, Keith S. Learn, Jason C. Wagner
  • Publication number: 20100298289
    Abstract: The present invention concerns heterobicyclic compounds of formula (I) processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
    Type: Application
    Filed: October 7, 2008
    Publication date: November 25, 2010
    Applicant: UCB PHARMA, S.A.
    Inventors: Gilles Raphy, Cecile Pegurier, Hans Meissner, Roland Knight, David Alan Owen
  • Publication number: 20100298318
    Abstract: The present invention provides methods and compositions comprising compounds useful for stimulating neurogenesis. The methods and compositions comprising compounds are also useful for inhibiting neuronal degeneration. Thus, the present invention can be used in the treatment of diseases and conditions characterized by neuronal loss and reduced neurogenesis including Alzheimer's disease, stroke, traumatic brain injury, traumatic nerve injury, and depression. This invention is useful for resear products including single agents or mixtures of agents to promote, proliferate, differentiate, or maintain neurons from stem or progenitor cells.
    Type: Application
    Filed: June 20, 2008
    Publication date: November 25, 2010
    Applicant: NEURONASCENT, INC.
    Inventor: Judith Kelleher-Andersson
  • Publication number: 20100286175
    Abstract: The invention relates to 2-(pyridin-2-yl)-pyrimidine compounds of general formula (I) and their use for controlling pathogenic fungi and as plant protection products that, as an active constituent, contain compounds of this type: In general formula (I), k represents 0, 1, 2, 3; m represents 0, 1, 2, 3, 4 or 5; n represents 1, 2, 3, 4 or 5; R1, independent of one another, represents halogen, OH, CN, NO2, C1-C4 alkyl, C1-C4 alkyl halide, C1-C4 alkoxy, C1-C4 alkoxy halide, C2-C4 alkenyl, C2-C4 alkynyl, C3-C8 cycloalkyl, C1-C4 alkoxy-C1-C4 alkyl, amino, phenoxy, which is optionally substituted by halogen or C1-C4 alkyl, NHR, NR2, C(Ra)?N—ORb, S(?O)pA1 or C(?O)A2, or two radicals R1 bound to adjacent carbon atoms can, together, also represent a group —O-Alk-O—, wherein Alk represents a linear or branched C1-C4 alkylene, and 1, 2, 3 or 4 hydrogen atoms can also be replaced by halogen; R2 represents C1-C4 alkyl halide, C1-C4 alkoxy, C1-C4 alkoxy halide, hydroxy, halogen, CN or NO2; whereby R2 can also represent
    Type: Application
    Filed: July 21, 2010
    Publication date: November 11, 2010
    Inventors: Wassilios Grammenos, Thomas Grote, Carsten Blettner, Markus Gewehr, Udo Hünger, Bernd Müller, Joachim Rheinheimer, Peter Schäfer, Frank Schieweck, Anja Schwögler, Ulrich Schöfl, Harald Köhle, Siegfried Strathmann, Maria Scherer, Reinhard Stierl, Jan Rether
  • Patent number: 7829708
    Abstract: The present invention provides compositions and methods for the treatment of disorders of abnormal cell proliferation and/or inflammation, such as psoriasis and inflammatory bowel disease, in a human or other host animals.
    Type: Grant
    Filed: September 8, 2005
    Date of Patent: November 9, 2010
    Assignee: Chelsea Therapeutics, Inc.
    Inventors: Michael J. Roberts, Simon Pedder
  • Publication number: 20100280012
    Abstract: An azaazulene compound is provided. The azaazulene compound has formula (I) shown below. Each variable in formula (I) is defined in the specification. The compound can be used to treat cancer. The invention also provides a method for treating cancer. The method includes administering to a subject in need thereof an effective amount of one or more azaazulene compounds of formula (I).
    Type: Application
    Filed: April 28, 2010
    Publication date: November 4, 2010
    Applicant: INDUSTRIAL TECHNOLOGY RESEARCH INSTITUTE
    Inventor: On LEE
  • Publication number: 20100234351
    Abstract: A compound of the formula: wherein ring A is a 7-membered or 8-membered nitrogen-containing ring optionally further substituted, ring B is an optionally substituted aryl group or an optionally substituted heteroaryl group, X1 is a group represented by —NR3—Y1—, —O—, —S—, —SO—, —SO2— or —CHR3— wherein R3 is a hydrogen atom or an optionally substituted aliphatic hydrocarbon group, or R3 may be bonded to the carbon atom of ring B to form an optionally substituted ring structure, and Y1 is a bond or an optionally substituted alkylene, R1 is a hydrogen atom, or an optionally substituted group bonded via a carbon atom or a sulfur atom, the formula shows a single bond or a double bond, when R2 is —R2, R2 is a hydrogen atom, or an optionally substituted group bonded via a carbon atom, a nitrogen atom, an oxygen atom or a sulfur atom, and when R2 is ?R2, R2 is an oxo group, an optionally substituted alkylidene group, or an optionally substituted imino group.
    Type: Application
    Filed: February 22, 2007
    Publication date: September 16, 2010
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Masaki Seto, Tomohiro Ohashi
  • Patent number: 7790719
    Abstract: This invention provides compounds and methods for treating melanocortin receptor associated disorders, such as weight loss disorders including cachexia resulting from cancer and other chronic illnesses. The compounds are represented by formula I: wherein X is oxygen or sulfur; G is G1 or G2: L1, L2, L3 and Q are linker groups, and Rings A, B and C, and R1-R14 are described in the specification. The compounds are antagonists of melanocortin receptors.
    Type: Grant
    Filed: July 26, 2007
    Date of Patent: September 7, 2010
    Assignee: Ore Pharmaceuticals, Inc.
    Inventors: Tricia J. Vos, Michael Patane, Michael E. Solomon, Christopher Blackburn, Mihaela D. Danca
  • Patent number: 7790729
    Abstract: The invention relates to the inhibition of VEGF receptor signaling and HGF receptor signaling. The invention provides compounds and methods for inhibiting VEGF receptor signaling and HGF receptor signaling. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
    Type: Grant
    Filed: May 19, 2006
    Date of Patent: September 7, 2010
    Assignee: Methylgene Inc.
    Inventors: Oscar Mario Saavedra, Stephen William Claridge, Lijie Zhan, Franck Raeppel, Arkadii Vaisburg, Stephane Raeppel, Robert Deziel, Michael Mannion, Nancy Z. Zhou, Ljubomir Isakovic
  • Patent number: 7772242
    Abstract: Disclosed is the use of the compounds of formula ?wherein Q is —OH; —OR7; —NH2; —NHR7; —NR7R8; or —N?R9; T is —COR5; —CN; or —SO2—(C6-C12)aryl; R1 is hydrogen; —OR7, —SR7; —NHR7; —NR7R8; C1-C22alkyl; C2-C12Alkenyl; C2-C12alkinyl; C3-C12cycloalkyl; C3-C12cycloalkenyl; C7-C12aralkyl; C1-C12heteroalkyl, C2-C11heteroaralkyl; C6-C10aryl; or C1-C9heteroaryl; R2 and R3 independently from each other are C1-C22alkyl; C2-C12alkenyl; C2-C12alkinyl; C3-C12cycloalkyl, C3-C12cycloalkenyl; C7-C12aralkyl; C1-C12heteroalkyl; C3-C12cycloheteroalkyl; C2-C11heteroaralkyl, C6-C10aryl; or C1-C9heteroaryl; R4 is cyano; COR7, COOR7; CONH2; CONHR7; CONR7R8; SO2(C6-C12)aryl, C2-C12alk-1 -enyl; C3-C12cycloalk-1-enyl; C2-C12alk-1-inyl; C2-C12heteroalkyl, C3-C5heterocycloalkyl, C6-C10aryl; or C1-C9heteroaryl; R5 is —COR7; —COOR7; —OR7; —SR7, —NHR7, —NR7R8; C1-C22alkyl; C2-C12alkenyl; C2-C12alkinyl; C3-C12cycloalkyl; C3-C12cycloalkenyl; C7-C12aralkyl; C1-C12alkylphenyl; C1-C12alkoxy-C6-C10aryl; C1-C12heteroalkyl; C2-C11heteroaralk
    Type: Grant
    Filed: June 20, 2005
    Date of Patent: August 10, 2010
    Assignee: Ciba Specialty Chemicals Corp.
    Inventors: Barbara Wagner, Frank Bienewald, Heinz Wolleb, Olof Wallquist, Bernd Herzog, Thomas Ehlis, Jürg Haase
  • Patent number: 7772285
    Abstract: A benzophenone derivative represented by the following formula: wherein R1 represents, for example, an optionally substituted heterocyclic group, or a substituted phenyl group; Z represents, for example, an alkylene group; R2 represents, for example, a carboxyl group optionally protected with alkyl; R3 represents, for example, an optionally protected hydroxyl group; R4 represents, for example, an optionally substituted cycloalkyloxy group; and R5 represents, for example, a hydrogen atom, or a salt thereof has anti-arthritic activity, inhibits bone destruction caused by arthritis, and provides high safety and excellent pharmacokinetics and thus is useful as therapeutic agent for arthritis. These compounds have inhibitory effect on AP-1 activity and are useful as preventive or therapeutic agent for diseases in which excessive expression of AP-1 is involved.
    Type: Grant
    Filed: November 13, 2002
    Date of Patent: August 10, 2010
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Hisaaki Chaki, Hironori Kotsubo, Tadashi Tanaka, Yukihiko Aikawa, Shuichi Hirono, Shunichi Shiozawa
  • Patent number: 7759353
    Abstract: Disclosed are certain substituted spiro iminopyrimidinones and other compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein U, W, A, R, R1, R2, R6a and R7, are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of using such compounds and compositions to inhibit aspartyl protease, and to treat a variety of disease and indications including (but not limited) to cardiovascular disease and cognitive and neurodegenerative disease. The compounds of the present invention are disclosed for use alone or in combination with one or more additional active ingredients such as cholinesterase inhibitors and a muscarinic m1 agonist and/or m2 antagonists.
    Type: Grant
    Filed: June 12, 2006
    Date of Patent: July 20, 2010
    Assignees: Schering Corporation, Pharmacopeia LLC.
    Inventors: Zhaoning Zhu, Brian McKittrick, Andrew Stamford, Tao Guo, Thuy X. H. Le
  • Patent number: 7732446
    Abstract: Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV inhibitors comprising Formulae: where the substituents are as described herein.
    Type: Grant
    Filed: March 9, 2005
    Date of Patent: June 8, 2010
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Stephen L. Gwaltney, Jeffrey A. Stafford, Michael B. Wallace, Laurence E. Burgess, Scott D. Cowen, Stephen S. Gonzales, Ellen R. Laird, Xiaodong Wang
  • Patent number: 7723328
    Abstract: Methods and compounds for treating neurodegenerative and other disorders. Included is the administering to a subject in need thereof an effective amount of a compound having binding specificity for a p75NTR receptor molecule. Enhanced survival of neural and other cells has been observed.
    Type: Grant
    Filed: April 3, 2006
    Date of Patent: May 25, 2010
    Assignees: The University of North Carolina at Chapel Hill, The Regents of the University of California, The United States of America as represented by the Department of Veterans Affairs
    Inventors: Frank M. Longo, Stephen M. Massa
  • Patent number: 7718660
    Abstract: The invention relates to compounds of the formula I, or pharmaceutically acceptable salts thereof: wherein: Z=O or S; n=1?3; R3?—CO2R8, —C(O)SR8, —C(O)NHR8, —C(S)OR8, —C(S)SR8, —C(S)NHR8, —C(NH)SR8 or —C(NH)NHR8, wherein R8 is —H or alkyl; R4?.H, —CH2R5 or —CH2CH2R5, wherein R5 independently has one of the meanings of R3; B?—NR2—, —CH2NR2—, —CH2CH2NR2, —CH2CHR7— or —CH2O—, wherein R2 is H or a C1-3 alkyl, alkenyl or alkynyl group, and R7 is H or a C13 alkyl or alkoxy group; A= wherein R1?—NH2 or —OH, and C and D are each, independently, a 5- or 6-membered, substituted or unsubstituted, aromatic or non-aromatic ring which may also contain one or more heteroatoms, and C is connected to group B in any available position.
    Type: Grant
    Filed: August 16, 2006
    Date of Patent: May 18, 2010
    Inventor: Dan Stoicescu
  • Publication number: 20100113460
    Abstract: Disclosed are compounds having the ability to inhibit cytochrome P450 2A6, 2A13, and/or 2B6 and tobacco products comprising them. Also disclosed are pharmaceutical compositions comprising them.
    Type: Application
    Filed: March 20, 2008
    Publication date: May 6, 2010
    Applicant: Givaudan SA
    Inventors: Boris Schilling, Wolf D. Woggon, Antoinette Chougnet, Thierry Granier, Georg Frater, Andreas Hanhart