Chalcogen Double Bonded Directly To A Ring Carbon Of The Seven-membered Hetero Ring Which Is Adjacent To The Ring Nitrogen Patents (Class 514/212.03)
  • Patent number: 9725430
    Abstract: Inhibitors of EYA tyrosine phosphatase having the structure of Formula I are provided herein. The compounds are useful for the treatment of certain proliferative diseases and cancer.
    Type: Grant
    Filed: January 14, 2014
    Date of Patent: August 8, 2017
    Assignee: CHILDREN'S HOSPITAL MEDICAL CENTER
    Inventor: Rashmi Hegde
  • Patent number: 9597312
    Abstract: The present disclosure provides methods of treating a cognitive disorder associated with abnormal dendritic spines, such as Fragile X Syndrome, Fragile X Associated Tremor/Ataxia Syndrome, autism, or mental retardation, using PKC activators.
    Type: Grant
    Filed: August 19, 2011
    Date of Patent: March 21, 2017
    Assignee: Cognitive Research Enterprises, Inc.
    Inventors: Miao-kun Sun, Daniel L. Alkon
  • Patent number: 9511016
    Abstract: Topical compositions having as the active ingredient a lipid, fatty acid ester, natural wax, sterol, or combinations thereof referred to herein as “lipophilic vehicle” or “LV” and methods of use, have been developed for the amelioration or prevention of pain or the sequelae of pain. The composition may be in the form of an ointment, cream, gel, lotion, spray, foam, paste, patch, suspension or dispersion. The composition is variably effective to treat visceral, somatic and neuropathic pain both acute and chronic as well as muscle pain and stiffness and joint pain and stiffness.
    Type: Grant
    Filed: September 6, 2007
    Date of Patent: December 6, 2016
    Assignee: EpicentRx, Inc.
    Inventors: Bryan T. Oronsky, Neil C. Oronsky, Arnold L. Oronsky
  • Patent number: 9006454
    Abstract: The invention relates to compounds of formula (I) wherein R1, R2, X1, X2, Y, Ra, Rb, Q have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis and also in the treatment of cancer disorders.
    Type: Grant
    Filed: March 26, 2010
    Date of Patent: April 14, 2015
    Assignee: Merck Serono S.A.
    Inventors: Siva Sanjeeva Rao Thunuguntla, Hosahalli Subramanya, Satish Reddy Kunnam, Sekhar Reddy Sanivaru Vijay, Chakrapani Bingi, Raviraj Kusanur, Matthias Schwarz, Michael Arlt
  • Publication number: 20150031670
    Abstract: Compounds of the formula (I), in which R1, R3, R5, R6, R7, R, X and Y have the meanings indicated in Claim 1, are inhibitors of methionine aminopeptidase and can be employed for the treatment of tumours.
    Type: Application
    Filed: March 21, 2013
    Publication date: January 29, 2015
    Applicant: MERCK PATENT GmbH
    Inventors: Timo Heinrich, Frank Zenke, Mireille Krier, Manja Friese-Hamim, Jeyaprakashnarayanan Seenisamy
  • Patent number: 8853200
    Abstract: The invention relates to 3-(2?,2?-dimethylpropanoylamino)-tetrahydropyridin-2-one, and its pharmaceutical compositions and its use for preparing a medicament intended to prevent or treat inflammatory disorders.
    Type: Grant
    Filed: August 1, 2008
    Date of Patent: October 7, 2014
    Assignee: Cambridge Enterprise Limited
    Inventors: David John Grainger, David Fox
  • Publication number: 20140286931
    Abstract: The present invention relates to new biphenyl-3-carboxylic acid modulators of beta-3-adrenoceptor activity, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: June 5, 2014
    Publication date: September 25, 2014
    Inventor: Chengzhi Zhang
  • Publication number: 20140256684
    Abstract: The present invention relates to a method for treating ocular inflammatory diseases in a subject in need of such treatment, which comprises administering a pharmaceutical composition comprising a therapeutically effective amount of at least one agonist of Formyl peptide receptor 2.
    Type: Application
    Filed: March 4, 2014
    Publication date: September 11, 2014
    Applicant: Allergan, Inc.
    Inventors: Richard L. Beard, John E. Donello, Veena Viswanath
  • Publication number: 20140235533
    Abstract: The present invention provides compounds of formula I wherein Q is Q1 or Q2; A1, A2, A3 and A4 are independently of each other C—H, C—R7, or nitrogen; R1 is C1-C8haloalkyl; R2 is aryl or aryl substituted by one to five R11, or heteroaryl or heteroaryl substituted by one to five R11; and R3, R4, R5, R6 and R7 are as defined in the claims. The invention also provides methods of controlling insects, acarines, nematodes or molluscs which methods comprise applying to a pest, to a locus of a pest, or to a plant susceptible to attack by a pest an insecticidally, acaricidally, nematicidally or molluscicidally effective amount of a compound of formula (I).
    Type: Application
    Filed: August 10, 2012
    Publication date: August 21, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Tomas Smejkai, Sebastian Volker Wendeborn, Jerome Yves Cassayre, Myriem El Qacemi, Bernhard Breit, Lisa Diab, Regis Jean Georges Mondiere
  • Publication number: 20140024639
    Abstract: Compounds including various oligomers of piperlongumine and/or piperlongumine analogues as well as certain piperlongumine analogues that exhibit improved toxicity to cancer cells are disclosed. Also provided are compositions that comprise the compounds, methods of making compositions comprising the compounds, methods of making the compounds, and the use of compounds in methods for treating cancer.
    Type: Application
    Filed: July 19, 2013
    Publication date: January 23, 2014
    Inventors: Drew Adams, Mingji Dai, Stuart Schreiber, Mahmud Mustaqim Hussain, Zarko Boskovic
  • Publication number: 20140005175
    Abstract: Compounds of formula II are described: wherein D, n, Ra, Rb, and Rc are as herein defined, along with pharmaceutical compositions and methods of using compounds of formula II for treating or reducing the risk of peritoneal carcinomatosis in a patient.
    Type: Application
    Filed: August 26, 2013
    Publication date: January 2, 2014
    Applicants: Cephalon, Inc., University of Utah Research Foundation, University of Hawaii
    Inventors: Bruce D. Dorsey, Scott K. Kuwada, Jay P. Theroff, Craig A. Zificsak
  • Publication number: 20140005176
    Abstract: Provided herein are 2-phenoxy- and 2-phenylsulfonamide derivatives with CCR3 antagonistic activity. These compounds are useful for the treatment of diseases associated with CCR3 activity, including but not limited to, atopic dermatitis, allergic rhinitis, rheumatoid arthritis, Grave's disease, HIV infection, Alzheimer's disease, atherosclerosis and other inflammatory and/or immunological disorders.
    Type: Application
    Filed: August 26, 2013
    Publication date: January 2, 2014
    Applicant: AXIKIN PHARMACEUTICALS, INC.
    Inventors: Yingfu Li, Kevin Bacon, Hiromi Sugimoto, Keiko Fukushima, Kentaro Hashimoto, Makiko Marumo, Toshiya Moriwaki, Noriko Nunami, Naoki Tsuno, Klaus Urbahns, Nagahiro Yoshida
  • Publication number: 20130237525
    Abstract: The present invention relates to lactam derivatives of formula (I) wherein Y, R1, R2 and R3 are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as orexin receptor antagonists.
    Type: Application
    Filed: November 9, 2011
    Publication date: September 12, 2013
    Applicant: ACTELION PHARMACEUTICALS LTD.
    Inventors: Hamed Aissaoui, Christoph Boss, Christine Brotschi, Bibia Heidmann, Thierry Sifferlen, Jodi T. Williams
  • Publication number: 20130203734
    Abstract: Disclosed herein are methods of preventing or treating inflammatory diseases using sulfonamide analogs of 3-aminolactam compounds, each with aromatic “tail groups”. Compounds as defined by formulae (I) and (I?), and the medical uses of the compounds, are described herein.
    Type: Application
    Filed: June 8, 2011
    Publication date: August 8, 2013
    Inventors: David John Grainger, David John Fox
  • Patent number: 8497261
    Abstract: The invention provides compounds, compositions and uses of compounds of general formula (I) or pharmaceutically acceptable salts thereof, which are 3-aminocaprolactam derivatives, for the preparation of a medicament intended to treat an inflammatory disorder: wherein X is —CO—Y—(R1)n or SO2—Y—(R1)n; and Y is a cycloalkyl or polycycloalkyl group (such as an adamantyl, adamantanemethyl, bicyclooctyl, cyclohexyl, cyclopropyl group); or is a cycloalkenyl or polycycloalkenyl group.
    Type: Grant
    Filed: March 17, 2010
    Date of Patent: July 30, 2013
    Assignee: Cambridge Enterprise Limited
    Inventors: David J. Grainger, David John Fox
  • Publication number: 20130172319
    Abstract: The invention relates to the generation of a library of compounds enriched in agonist and antagonists for members of the G-protein coupled class of receptors (GPCRs). The library contains compounds of general formula (II) wherein: y is any integer from 1 to 8; X is —CO—R1 or —SO2—R1; each R1 is independently selected from an alkyl, haloalkyl, alkenyl, alkynyl, alkylaminoalkyl, alkylaminodialkyl, or charged alkylaminotrialkyl, radical of 1 to 20 carbon atoms; or each R1 is independently selected from oxyalkyl, aminoalkyl, aminodialkyl, or charged aminotrialkyl radical; and wherein the R1 radical has a “key” carbon next to the carbonyl of the carbon amide or the sulfonyl group of the sulfonamide which is di-substituted with the same or different groups selected from: alkyl, haloalkyl, alkoxy, haloalkoxy, alkenyl, alkynyl and alkylamino radicals.
    Type: Application
    Filed: February 26, 2013
    Publication date: July 4, 2013
    Applicants: CAMBRIDGE ENTERPRISE LIMITED
    Inventors: Cambridge Enterprise Limited, David J. Grainger, David John Fox
  • Publication number: 20120184520
    Abstract: [Problem] The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases. [Means for Solution] The present inventors have conducted intensive studies on a compound having a VAP-1 inhibitory activity, and as a result, they have found that a compound of the present invention or a salt thereof exhibits an excellent VAP-1 inhibitory activity and is useful for preventing and/or treating VAP-1-related diseases, in particular, diabetic nephropathy or diabetic macular edema, thereby completing the present invention. The present invention further relates to a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases, which comprises the compound of the present invention or a salt thereof, and an excipient.
    Type: Application
    Filed: September 15, 2010
    Publication date: July 19, 2012
    Applicant: Astellas Pharma Inc.
    Inventors: Kousei Yoshihara, Daisuke Suzuki, Susumu Yamaki, Yuji Koga, Norio Seki, Jiro Fujiyasu, Masahiro Neya
  • Patent number: 8188069
    Abstract: Compounds of formula (I), pharmaceutical compositions comprising them, and methods for their use are described.
    Type: Grant
    Filed: August 4, 2008
    Date of Patent: May 29, 2012
    Assignee: Eli Lilly and Company
    Inventors: Melinda Joy Hope Miller, Warren Jaye Porter, Jon Kevin Reel, Almudena Rubio-Esteban
  • Publication number: 20120122844
    Abstract: The present invention provides the use of a neutral endopeptidase inhibitor, in the manufacture of a medicament for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The invention also relates to the use of a compound of Formula I: wherein R1, R2, R3, R5, X, A3, B1, s and n are defined herein, for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The present invention further provides a combination of pharmacologically active agents for use in the treatment, amelioration and/or prevention of contrast-induced nephropathy.
    Type: Application
    Filed: November 11, 2011
    Publication date: May 17, 2012
    Applicant: NOVARTIS AG
    Inventor: Shi Yin FOO
  • Publication number: 20120077803
    Abstract: The invention provides the use of a compound of formula (I) or a solvate or hydrate thereof, wherein the substituents are as defined in the description, and combinations thereof, for the treatment of pruritus or a dermatological disorder or disease.
    Type: Application
    Filed: February 23, 2010
    Publication date: March 29, 2012
    Applicant: NOVARTIS AG
    Inventors: Anton Stuetz, Barbara Wolff-Winiski, Lina Williamson
  • Patent number: 8076323
    Abstract: The invention provides compounds, pharmaceutical compositions and uses of compounds and salts thereof of general formula (I), for the preparation of a medicament for treatment of an inflammatory disorder, but excluding (S)-3-(1?-methylcyclohexylcarbonylamino)-caprolactam: wherein z is 1, 2, 3 or 4; A is —CO— or —SO2—; Q is linear or branched alkyl, alkenyl, alkynyl, alkoxy, oxyalkyl, aminoalkyl, alkylamino, alklylaminoalkyl, haloalkyl, aryl or substituted aryl; T1 and T2 together constitute a cycloalkyl, cycloalkenyl or polycycloalkyl radical composed of n additional carbon atoms, where n is between 2 and 7; and each hydrogen atom bonded to the carbon atoms in the ring generated by T1 and T2 may be independently be substituted by a group R1, where R1 is independently selected from an alkyl, haloalkyl, alkoxy, haloalkoxy, alkenyl, alkynyl or alkylamino radical of 1 to 20 carbon atoms; or each R1 is independently selected from fluoro, chloro, bromo, iodo, hydroxy, oxyalkyl, amino, aminoalkyl or aminodialky
    Type: Grant
    Filed: September 7, 2010
    Date of Patent: December 13, 2011
    Assignee: Cambridge Enterprise Limited
    Inventors: David J. Grainger, David John Fox
  • Patent number: 8063039
    Abstract: A method for treating pain, migraine, inflammation, gastrointestinal tract disorders, disorders of the genito-urinary tract, ophthalmic diseases or obesity in a subject, the method including administering to the subject an effective amount of a compound of a general formula, specific examples of which include 3-(4-Butyloxy-benzylamino)-pyrrolidin-2-one, 3-[4-(4-trifluorobutyloxy)-benzylamino]-pyrrolidin-2-one, 3-(4-Pentyloxy-benzylamino)-pyrrolidin-2-one, 3-[4-(5-trifluoropentyloxy)-benzylamino]-pyrrolidin-2-one, and 3-(4-Phenylethyl-benzylamino)-pyrrolidin-2-one.
    Type: Grant
    Filed: November 2, 2009
    Date of Patent: November 22, 2011
    Assignee: Newron Pharmaceuticals S.p.A.
    Inventors: Florian Thaler, Cibele Maria Sabido David, Sara Maestroni, Luca Francesco Raveglia, Patricia Salvati
  • Publication number: 20110212920
    Abstract: Disclosed are N-substituted benzenesulfonamides for use in treating or preventing cognitive disorders, such as Alzheimer's Disease. In Formula (I), R1, R2, R3, R4, R3?, R10 and R11 are as described herein. The invention also encompasses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of treating cognitive disorders using compounds of Formula (I).
    Type: Application
    Filed: May 9, 2011
    Publication date: September 1, 2011
    Inventors: Martin Neitzel, Michael S. Dappen, Jennifer Marugg
  • Patent number: 7985746
    Abstract: The invention relates to compounds of formula I: along with pharmaceutical compositions containing the same and methods of use thereof for the treatment of autoimmune disease.
    Type: Grant
    Filed: May 24, 2007
    Date of Patent: July 26, 2011
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Francis Fang, Shawn Schiller, Boris Seletsky, Mark Spyvee
  • Patent number: 7968707
    Abstract: A compound of the formula: is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.
    Type: Grant
    Filed: February 27, 2007
    Date of Patent: June 28, 2011
    Assignee: Abbott Laboratories
    Inventors: Hing Leung Sham, Daniel W. Norbeck, Xiaoqi Chen, David A. Betebenner, Dale J. Kempf, Thomas R. Herrin, Gondi N. Kumar, Stephen L. Condon, Arthur J. Cooper, Daniel A. Dickman, Steven M. Hannick, Lawrence Kolaczkowski, Patricia A. Oliver, Daniel J. Plata, Peter J. Stengel, Eric J. Stoner, Jieh-Heh J. Tien, Jih-Hua Liu, Ketan M. Patel
  • Patent number: 7968592
    Abstract: 3-aminopyrrolidone compounds and pharmaceutically acceptable salts thereof that are active as sodium and/or calcium channel modulators and therefore useful in preventing, alleviating and curing a wide range of pathologies, including, but not limited to cardiovascular, inflammatory, ophthalmic, urologic, metabolic and gastrointestinal diseases.
    Type: Grant
    Filed: November 16, 2004
    Date of Patent: June 28, 2011
    Assignee: Newron Pharmaceuticals S.p.A.
    Inventors: Florian Thaler, Cibele Maria Sabido David, Sara Maestroni, Luca Francesco Raveglia, Patricia Salvati
  • Publication number: 20110150873
    Abstract: The invention relates to the use of Broad-Spectrum Chemokine Inhibitors (BSCIs), and in particular members of the acylaminolactam class of pharmaceutical agents, for the prevention, prophylaxis, treatment or amelioration of symptoms of inflammatory diseases. In particular, improved compositions consisting of BSCI agents combined with one or more additional active pharmaceutical agents in order to achieve improved anti-inflammatory efficacy with a reduced side-effect profile are described and claimed.
    Type: Application
    Filed: December 10, 2008
    Publication date: June 23, 2011
    Applicant: CAMBRIDGE ENTERPRISE LIMITED
    Inventor: David John Grainger
  • Publication number: 20110104315
    Abstract: 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: Application
    Filed: January 5, 2011
    Publication date: May 5, 2011
    Inventors: Chongqing Sun, Doree Sitkoff, William R. Ewing, Yanting Huang, Bruce A. Ellsworth, Richard B. Sulsky, Annapurna Pendri, Samuel Gerritz, Natesan Murugesan, Zhengxiang Gu
  • Publication number: 20110003792
    Abstract: The invention provides compounds, pharmaceutical compositions and uses of compounds and salts thereof of general formula (I), for the preparation of a medicament for treatment of an inflammatory disorder, but excluding (S)-3-(1?-methylcyclohexylcarbonylamino)-caprolactam: wherein z is 1, 2, 3 or 4; A is —CO— or —SO2—; Q is linear or branched alkyl, alkenyl, alkynyl, alkoxy, oxyalkyl, aminoalkyl, alkylamino, alklylaminoalkyl, haloalkyl, aryl or substituted aryl; T1 and T2 together constitute a cycloalkyl, cycloalkenyl or polycycloalkyl radical composed of n additional carbon atoms, where n is between 2 and 7; and each hydrogen atom bonded to the carbon atoms in the ring generated by T1 and T2 may be independently be substituted by a group R1, where R1 is independently selected from an alkyl, haloalkyl, alkoxy, haloalkoxy, alkenyl, alkynyl or alkylamino radical of 1 to 20 carbon atoms; or each R1 is independently selected from fluoro, chloro, bromo, iodo, hydroxy, oxyalkyl, amino, aminoalkyl or aminodialky
    Type: Application
    Filed: September 7, 2010
    Publication date: January 6, 2011
    Applicant: CAMBRIDGE ENTERPRISE LIMITED
    Inventors: David J. Grainger, David John Fox
  • Publication number: 20100292213
    Abstract: The invention provides compounds, compositions and uses of compounds of general formula (I) or pharmaceutically acceptable salts thereof, which are 3-aminocaprolactam derivatives, for the preparation of a medicament intended to treat an inflammatory disorder: wherein X is —CO—Y—(R1)n or SO2—Y—(R1)n; and Y is a cycloalkyl or polycyloalkyl group (such as an adamantyl, adamantanemethyl, bicyclooctyl, cyclohexyl, cyclopropyl group); or is a cycloalkenyl or polycycloalkenyl group.
    Type: Application
    Filed: March 17, 2010
    Publication date: November 18, 2010
    Inventors: David J. Grainger, David John Fox
  • Publication number: 20100279986
    Abstract: This invention provides novel heterocyclic derived matrix metalloprotease inhibitors of the formula: and pharmaceutical compositions comprising same, useful for treating disorders ameliorated by antagonizing matrix metalloproteases. This invention also provides therapeutic and prophylactic methods using the instant pharmaceutical compositions.
    Type: Application
    Filed: July 12, 2010
    Publication date: November 4, 2010
    Inventors: Yue-Mei ZHANG, Bangping Xiang, Shyh-Ming Yang, Kenneth Rhodes, Robert Scannevin, Paul Jackson, Davraj Chakravarty, Xiaodong Fan, Lawrence J. Wilson, Prabha Karnachi
  • Patent number: 7825264
    Abstract: The invention relates to compounds of formula I in which A, R1, R2, R3, R4, R5, R6, R7 and n have the meanings stated in the claims. The compounds are particularly suitable as antiarrhythmic active ingredients, in particular for the treatment and prophylaxis of atrial arrhythmias, for example atrial fibrillation (AF) or atrial flutter.
    Type: Grant
    Filed: December 12, 2007
    Date of Patent: November 2, 2010
    Assignee: sanofi-aventis
    Inventors: Joachim Brendel, Heinrich Christian Englert, Stefan Peukert, Klaus Wirth, Michael Wagner, Jean-Marie Ruxer, Fabienne Pilorge
  • Patent number: 7803794
    Abstract: The invention provides compounds, pharmaceutical compositions and uses of compounds and salts thereof of general formula (I), for the preparation of a medicament for treatment of an inflammatory disorder, but excluding (S)-3-(r-methylcyclohexyl-carbonylamino)-caprolactam: wherein z is 1, 2, 3 or 4; A is —CO— or —SO2-; Q is linear or branched alkyl, alkenyl, alkynyl, alkoxy, oxyalkyl, aminoalkyl, alkylamino, alkylaminoalkyl, haloalkyl, aryl or substituted aryl; T1 and T2 together constitute a cycloalkyl, cycloalkenyl or polycycloalkyl radical composed of n additional carbon atoms, where n is between 2 and 7; and each hydrogen atom bonded to the carbon atoms in the ring generated by T1 and T2 may be independently be substituted by a group R1, where R1 is independently selected from an alkyl, haloalkyl, alkoxy, haloalkoxy, alkenyl, alkynyl or alkylamino radical of 1 to 20 carbon atoms; or each R1 is independently selected from fluoro, chloro, bromo, iodo, hydroxy, oxyalkyl, amino, aminoalkyl or aminodialkyl radi
    Type: Grant
    Filed: June 14, 2006
    Date of Patent: September 28, 2010
    Assignee: Cambridge Enterprise Limited
    Inventors: David J. Grainger, David John Fox
  • Patent number: 7803793
    Abstract: This invention provides novel heterocyclic derived matrix metalloprotease inhibitors of the formula: and pharmaceutical compositions comprising same, useful for treating disorders ameliorated by antagonizing matrix metalloproteases. This invention also provides therapeutic and prophylactic methods using the instant pharmaceutical compositions.
    Type: Grant
    Filed: September 21, 2007
    Date of Patent: September 28, 2010
    Assignee: Janssen Pharmaceutica NV
    Inventors: Yue-Mei Zhang, Bangping Xiang, Shyh-Ming Yang, Kenneth Rhodes, Robert Scannevin, Paul Jackson, Davraj Chakravarty, Xiaodong Fan, Lawrence J. Wilson, Prabha Karnachi
  • Publication number: 20100204204
    Abstract: Co-crystals comprising at least one nutraceutical compound and at least one co-crystal former with or without impurities. These co-crystals may be included in compositions (optionally also including other components such as pharmaceutically acceptable excipients, other nutritional supplements, etc.) having utility as pharmaceuticals, nutraceuticals, nutritional supplements, and foodstuffs.
    Type: Application
    Filed: June 6, 2008
    Publication date: August 12, 2010
    Applicant: UNIVERSITY OF SOUTH FLORIDA
    Inventors: Michael Zaworotko, Heather Clarke, Arora Kapildev, Padmini Kavuru, Roland Douglas Shytle, Twarita Pujari, Lissette Marshall, Tien Teng Ong
  • Publication number: 20100197660
    Abstract: Compounds of formula (I), pharmaceutical compositions comprising them, and methods for their use are described.
    Type: Application
    Filed: August 4, 2008
    Publication date: August 5, 2010
    Applicant: ELI LILLY AND COMPANY
    Inventors: Melinda Joy Hope Miller, Warren Jaye Porter, Jon Kevin Reel, Almudena Rubio-Esteban
  • Patent number: 7767664
    Abstract: The present invention relates to a new class of plant growth regulators. In particular, the invention relates to fused azepinone derivative of general formula (I) or an agriculturally acceptable salt thereof wherein X is CO2R2 or H; Y is OH; NHNR3R4, NHNHC(?Z)NR5R6 or NHNHC(?Z)CR7R8R9; or X and Y together with the two carbon atoms to which they are attached form a ring of formula (A) and a method for treatment of plants with such compounds in order to induce growth regulating responses.
    Type: Grant
    Filed: April 30, 2005
    Date of Patent: August 3, 2010
    Assignee: Bayer CropScience AG
    Inventors: Henricus M. M. Bastiaans, Günter Donn, Nathalie Knittel, Arianna Martelletti, Richard Rees, Michael Schwall, Ryan Whitford
  • Publication number: 20100190753
    Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-+related disease.
    Type: Application
    Filed: August 27, 2009
    Publication date: July 29, 2010
    Applicant: BELLUS Health (International) Limited
    Inventors: Xianqi KONG, Walter A. Szarek, Francine Gervais
  • Patent number: 7691845
    Abstract: The invention provides compounds, compositions and uses of compounds of general formula (I) or (I?), or pharmaceutically acceptable salts thereof, which are 3-aminocaprolactam derivatives, for the preparation of a medicament intended to treat an inflammatory disorder.
    Type: Grant
    Filed: August 10, 2005
    Date of Patent: April 6, 2010
    Assignee: Cambridge Enterprise Limited
    Inventors: David J. Grainger, David John Fox
  • Patent number: 7691846
    Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I: P4-P-M-M4??I or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
    Type: Grant
    Filed: March 10, 2009
    Date of Patent: April 6, 2010
    Assignee: Bristol-Myers Squibb Company
    Inventor: Donald J. P. Pinto
  • Publication number: 20100016286
    Abstract: The invention provides compounds, pharmaceutical compositions and uses of compounds and salts thereof of general formula (I), for the preparation of a medicament for treatment of an inflammatory disorder, but excluding (S)-3-(r-methylcyclohexyl-carbonylamino)-caprolactam: wherein z is 1, 2, 3 or 4; A is —CO— or —SO2-; Q is linear or branched alkyl, alkenyl, alkynyl, alkoxy, oxyalkyl, aminoalkyl, alkylamino, alkylaminoalkyl, haloalkyl, aryl or substituted aryl; T1 and T2 together constitute a cycloalkyl, cycloalkenyl or polycycloalkyl radical composed of n additional carbon atoms, where n is between 2 and 7; and each hydrogen atom bonded to the carbon atoms in the ring generated by T1 and T2 may be independently be substituted by a group R1, where R1 is independently selected from an alkyl, haloalkyl, alkoxy, haloalkoxy, alkenyl, alkynyl or alkylamino radical of 1 to 20 carbon atoms; or each R1 is independently selected from fluoro, chloro, bromo, iodo, hydroxy, oxyalkyl, amino, aminoalkyl or aminodialkyl radi
    Type: Application
    Filed: June 14, 2006
    Publication date: January 21, 2010
    Inventors: David J. Grainger, David John Fox
  • Publication number: 20100015225
    Abstract: Solid dispersion comprising (4R)-4-[N?-methyl-N?-(3,5-bistrifluoromethyl-benzoyl)-amino]-4-(3,4-dichlorobenzyl)-but-2-enoic acid N—[(R)-epsilon-caprolactam-3-yl]-amide or a pharmaceutically acceptable salt or solvate thereof and a carrier. Pharmaceutical compositions comprising such solid dispersion are useful to treat patients who have functional motility disorders of the viscera, especially irritable bowel syndrome or functional dyspepsia, or urinary bladder disorders, especially urinary incontinence.
    Type: Application
    Filed: December 20, 2007
    Publication date: January 21, 2010
    Inventors: Anke Diederich, Carsten Timpe, Angelika Ries, Isabel Ottinger, Irene Mueller, Michael Herbig, Helmut Schuetz, Jay Parthiban Lakshman, Oskar Kalb
  • Publication number: 20100009965
    Abstract: This invention relates to novel cyclic malonamides having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to ?-amyloid production such as Alzheimer's disease and Down's Syndrome.
    Type: Application
    Filed: September 2, 2009
    Publication date: January 14, 2010
    Applicant: BRISTOL-MYERS SQIBB PHARMA COMPANY
    Inventors: Richard E. Olson, Michael G. Yang
  • Publication number: 20090286771
    Abstract: Provided herein are 2-phenoxy- and 2-phenylsulfonamide derivatives with CCR3 antagonistic activity. These compounds are useful for the treatment of diseases associated with CCR3 activity, including but not limited to, atopic dermatitis, allergic rhinitis, rheumatoid arthritis, Grave's disease, HIV infection, Alzheimer's disease, atherosclerosis and other inflammatory and/or immunological disorders.
    Type: Application
    Filed: July 16, 2009
    Publication date: November 19, 2009
    Inventors: Yingfu Li, Kevin Bacon, Hiromi Sugimoto, Keiko Fukushima, Kentaro Hashimoto, Makiko Marumo, Toshiya Moriwaki, Noriko Nunami, Naoki Tsuno, Klaus Urbahns, Nagahiro Yoshida
  • Patent number: 7585855
    Abstract: The invention relates to the preparation of substituted caprolactams, a method for the preparation thereof, compositions containing them and the use thereof as a medicament, particularly as anticancer agents.
    Type: Grant
    Filed: August 19, 2008
    Date of Patent: September 8, 2009
    Assignee: Aventis Pharma SA
    Inventors: Jidong Zhang, Neerja Bhatnagar
  • Publication number: 20090181944
    Abstract: The present invention provides a method for treating a patient having cancer comprising administering to the patient a therapeutically effective amount of compound (1), or a pharmaceutically acceptable salt thereof, having the formula: The present invention also provides a kit containing the above compound.
    Type: Application
    Filed: January 5, 2009
    Publication date: July 16, 2009
    Inventors: John Frederick Boylan, Leopoldo Ladores Luistro, III, Kathyrn Elizabeth Packman
  • Patent number: 7501406
    Abstract: The invention relates to compounds of general formula wherein R1, R2, R3/R3?, R4/R4? and R5/R5? are as defined in the specification and to pharmaceutically acceptable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. The compounds are ?-secretase inhibitors which can be useful in the treatment of Alzheimer's disease or common cancers including, but not limited to, cervical carcinomas and breast carcinomas and malignancies of the hematopoietic system.
    Type: Grant
    Filed: August 8, 2006
    Date of Patent: March 10, 2009
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alexander Flohr, Guido Galley, Roland Jakob-Roetne, Eric Argirios Kitas, Wolfgang Wostl
  • Publication number: 20090054398
    Abstract: The invention provides a new method for treating disorders associated with activation of the Notch signal transduction pathway comprising administering an effective amount of a compound of Formula (I), in free form or in a pharmaceutically acceptable salt form or in the form of a pharmaceutically acceptable solvate of the compound or the salt, to a human or animal patient in need thereof.
    Type: Application
    Filed: March 9, 2007
    Publication date: February 26, 2009
    Applicant: ASTRAZENECA AB
    Inventors: Kevin Hudson, Naomi Laing, Paula Lewis
  • Publication number: 20090042858
    Abstract: The present invention discloses novel methods and compositions for viral inhibition, particularly inhibition of HCV and SARS. The invention also provides compositions including novel oxoazepanylacetamide derivatives useful for viral inhibition.
    Type: Application
    Filed: June 16, 2006
    Publication date: February 12, 2009
    Inventors: Paul Barsanti, Nathan Brammier, Bryan Chang, Zhi-Jie Ni, Weibo Wang, Amy Weiner
  • Publication number: 20080318928
    Abstract: The invention relates to the preparation of substituted caprolactams, a method for the preparation thereof, compositions containing them and the use thereof as a medicament, particularly as anticancer agents.
    Type: Application
    Filed: August 19, 2008
    Publication date: December 25, 2008
    Applicant: AVENTIS PHARMA S.A.
    Inventors: Jidong ZHANG, Neerja Bhatnagar