Ring Oxygen In The Additional Hetero Ring Patents (Class 514/254.1)
  • Publication number: 20100160322
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.
    Type: Application
    Filed: December 4, 2009
    Publication date: June 24, 2010
    Applicant: ABBOTT LABORATORIES
    Inventors: Milan Bruncko, Yujia Dai, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa Hasvold, Laura Hexamer, Aaron Kunzer, Robert A. Mantei, William J. McClellan, Chang H. Park, Cheol-Min Park, Andrew M. Petros, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt
  • Publication number: 20100125075
    Abstract: Compounds of formula (II) are antibacterial agents wherein Q represents a radical of the formula: —N(OH)CH(?O) or the formula: —C(?O)NH(OH); R1 represents hydrogen, C1-C6 alkyl or C1-C6 alkyl substituted by one or more halogen atoms, or, except when Q is a radical of the formula: —N(OH)CH(?O), a hydroxy, C1-C6 alkoxy, C1-C6 alkenyloxy, amino, C1-C6 alkylamino, or di-(C1-C6 alkylamino group; R2 represents a substituted or unsubstituted C1-C6 alkyl, cycloalkyl(C1-C6 alkyl)- or aryl(C1-C6 alkyl)-group; and A represents a group of formula (IIA), or (IIB) wherein R4 represents the side chain of a natural or non-natural alpha amino acid, and R5 and R6 when taken together with the nitrogen atom to which they are attached form a saturated heterocyclic first ring of 5 to 7 atoms as specified in the description.
    Type: Application
    Filed: December 14, 2006
    Publication date: May 20, 2010
    Applicant: British Biotech Pharmaceuticals Ltd.
    Inventors: Lisa Marie Pratt, Kenneth Noel Keavey, Gilles Denis Pain, Laurent Mounier
  • Publication number: 20100124543
    Abstract: The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.
    Type: Application
    Filed: July 16, 2009
    Publication date: May 20, 2010
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Roger Dennis Tung, Michael Robin Hale, Christopher Todd Baker, Eric Steven Furfine, Istvan Kaldor, Wieslaw Mieczylaw Kazmierski, Andrew Spaltenstein
  • Publication number: 20100125071
    Abstract: The present invention relates to compounds of formula (I) with the substituents as defined herein, and uses thereof.
    Type: Application
    Filed: June 4, 2008
    Publication date: May 20, 2010
    Inventors: Neil John Press, Simon James Watson
  • Publication number: 20100120789
    Abstract: There is provided a compound having Formula I R1—Z—R2 ??Formula I wherein R1 is a group selected from optionally substituted fused polycyclic groups, substituted alkyl groups, branched alkyl groups, and optionally substituted cycloalkyl groups Z is a linker which is or comprises a carbonyl group or a isostere of a carbonyl group R2 is selected from optionally substituted aromatic rings and optionally substituted heterocyclic rings wherein (a) R2 is a 2-substituted thiophene group, and/or (b) Z is a group of the formula —C(?O)—CR3R4—X—(CR5R6)n-, wherein X is selected from NR7, S, O, S?O, and S(?O)2, wherein n is 0 or 1 and/or (c) R1 is an adamantyl group and Z is or comprises an amide group, and/or (d) R1 is an adamantyl group and Z is or comprises a group of the formula —(CR8R9)p- NR10—S(?O)2—(CR11R12)q-, wherein p is 0 or 1 and q is 0 or 1 and/or (e) R1 is an adamantyl group and Z is or comprises a group of the formula —(CR13R14)v-Y—(CR15R16)w- where Y is a heteroaryl group in which a bond in the hetero
    Type: Application
    Filed: September 7, 2009
    Publication date: May 13, 2010
    Inventors: Nigel Vicker, Xiangdong Su, Fabienne Praduax, Michael John Reed, Barry Victor Lloyd Potter
  • Publication number: 20100119503
    Abstract: The present invention is directed to compounds of Formula I: which are modulators of chemokine receptors. The compounds of the invention, and compositions thereof, are useful in the treatment of diseases related to chemokine receptor expression and/or activity.
    Type: Application
    Filed: September 25, 2008
    Publication date: May 13, 2010
    Applicant: INCYTE CORPORATION
    Inventors: Chu-Biao Xue, Changsheng Zheng, Hao Feng, Michael Xia, Joseph Glenn, Ganfeng Cao, Brian W. Metcalf
  • Patent number: 7700586
    Abstract: The present invention relates to a sulfonamide derivative which is useful as an active ingredient of pharmaceutical preparations. The sulfonamide derivatives of the present invention have CCR3 (CC type chemokine receptor) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with CCR3 activity, in particular for the treatment of asthma, atopic dermatitis, allergic rhinitis and other inflammatory/immunological disorders.
    Type: Grant
    Filed: September 4, 2002
    Date of Patent: April 20, 2010
    Assignee: Axikin Pharmaceuticals, Inc.
    Inventors: Yingfu Li, Akihiko Watanabe, Timothy B. Lowinger, Kevin Bacon, Norihiro Kawamura, Takuya Shintani, Tetsuo Kikuchi, Toshiya Moriwaki, Klaus Urbahns, Keiko Fukushima, Noriko Nunami, Takashi Yoshino, Toshiki Murata, Megumi Yamauchi, Hiroko Yoshino
  • Publication number: 20100086609
    Abstract: Methods are provided for purifying peptides and proteins by incorporating the peptide or protein into a diketopiperazine or competitive complexing agent to facilitate removal one or more impurities, from the peptide or protein. Formulations and methods also are provided for the improved transport of active agents across biological membranes, resulting for example in a rapid increase in blood agent concentration. The formulations include microparticles formed of (i) the active agent, which may be charged or neutral, and (ii) a transport enhancer that masks the charge of the agent and/or that forms hydrogen bonds with the target biological membrane in order to facilitate transport. In one embodiment, insulin is administered via the pulmonary delivery of microparticles comprising fumaryl diketopiperazine and insulin in its biologically active form. This method of delivering insulin results in a rapid increase in blood insulin concentration that is comparable to the increase resulting from intravenous delivery.
    Type: Application
    Filed: December 10, 2009
    Publication date: April 8, 2010
    Applicant: MANNKIND CORPORATION
    Inventors: Solomon S. Steiner, Rodney J. Woods, Joseph W. Sulner
  • Publication number: 20100063040
    Abstract: The present invention provides an sulfonamide derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases. A compound of the general formula (II): wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a nitrogen-containing non-aromatic heterocyclic ring etc.; the ring C is an aromatic carbocyclic ring etc.; R1 is carboxy etc.; R2 is independently a halogen atom etc.; R3 is optionally substituted alkyloxy etc.; R4 is independently a halogen atom etc.; R5 is independently optionally substituted alkyl etc.; M is sulfonyl etc.; Y is a single bond etc.; L1 is a single bond etc.; L2 is a single bond etc.; k is 0, 1, 2, 3 or 4; n is 0, 1 or 2; and q is 0, 1, 2 or 3; provided that a) k is not 0 when the ring B is a 6-membered nitrogen-containing heterocyclic ring containing one or two nitrogen atom(s) and the ring C is a benzene ring, etc.
    Type: Application
    Filed: September 25, 2006
    Publication date: March 11, 2010
    Inventor: Akira Kugimiya
  • Publication number: 20100029607
    Abstract: Compounds of Formula (I): or pharmaceutically acceptable salts, solvates, or esters thereof, are useful in treating diseases or conditions mediated by CB1 receptors, such as metabolic syndrome and obesity, neuroinflammatory disorders, cognitive disorders and psychosis, addiction (e.g., smoking cessation), gastrointestinal disorders, and cardiovascular conditions.
    Type: Application
    Filed: September 22, 2009
    Publication date: February 4, 2010
    Inventors: Eric J. Gilbert, Michael W. Miller, Jack D. Scott, Andrew W. Stamford, William J. Greenlee, Jay Weinstein
  • Publication number: 20090325978
    Abstract: The present invention provides a lyophilized preparation that has excellent stability over time and excellent solubility when reconstituted, and that contains (8E,12E,14E)-7-((4-cycloheptylpiperazin-1-yl)carbonyl)oxy-3,6,16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytricosa-8,12,14-trien-11-olide. The present invention discloses a lyophilized preparation containing 1) (8E,12E,14E)-7-((4-cycloheptylpiperazin-1-yl)carbonyl)oxy-3,6,16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytricosa-8,12,14-trien-11-olide or a pharmaceutically acceptable salt thereof, 2) a pH regulator for adjusting a pH of the preparation to between 5 and 8, and 3) at least one of excipients selected from the groups consisting of sugars and sugar alcohols.
    Type: Application
    Filed: August 13, 2007
    Publication date: December 31, 2009
    Inventors: Katsumi Onai, Makoto Yokayama
  • Publication number: 20090264416
    Abstract: The present invention relates to N-benzyl,N?-arylcarbonylpiperazine derivatives having the general formula I to pharmaceutical compositions comprising the same, and to the use of a these N-benzyl,N?-arylcarbonylpiperazine derivatives for the manufacture of a medicament for treating or preventing atherosclerosis and related disorders associated with cholesterol and bile acids transport and metabolism.
    Type: Application
    Filed: August 19, 2008
    Publication date: October 22, 2009
    Inventors: Koc-Kan Ho, Andrew Laird Roughton, Irina Neagu, Jui-Hsiang Chan, Nasrin Ansari, Michelle Lee Morris, Yajing Rong, Michael Ohlmeyer, Andrew John Cooke, Andrew Stanley Edwards, David Jonathan Bennett
  • Publication number: 20090253656
    Abstract: The present invention is directed to a breast cancer resistance protein (BCRP/ABCG2) inhibitor. The BCRP inhibitor contains, as an active ingredient, an acrylonitrile derivative represented by formula (1): wherein one of R1 and R2 represents a cyano group and the other represents a hydrogen atom; Ar1 represents a group selected from among the groups represented by formulas (2) to (4): and Ar2 represents an aromatic hydrocarbon group having a condensed ring which may be substituted by a halogen atom, or a group selected from among the groups represented by the following formulas (5) to (15): or a salt thereof.
    Type: Application
    Filed: March 29, 2006
    Publication date: October 8, 2009
    Applicant: Kabushiki Kaisha Yakult Honsha
    Inventors: Ryuta Yamazaki, Yukiko Nishiyama, Tomio Furuta, Takeshi Matsuzaki, Hiroshi Hatano, Oh Yoshida, Masato Nagaoka, Ritsuo Aiyama, Shusuke Hashimoto, Yoshikazu Sugimoto
  • Publication number: 20090253684
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, COPD.
    Type: Application
    Filed: December 2, 2008
    Publication date: October 8, 2009
    Inventors: Romyr Dominique, Robert Alan Goodnow, JR., Agnieszka Kowalczyk, Qi Qiao, Achyutharao Sidduri, Jefferson Wright Tilley
  • Publication number: 20090247503
    Abstract: Provided herein are 5-demethoxyfumagillol and its derivatives. Also provided herein are methods of making the 5-demethoxyfumagillol and derivatives. Also provided herein are biological activities of the 5-demethoxyfumagillol and derivatives and methods of using same for treating diseases.
    Type: Application
    Filed: March 25, 2009
    Publication date: October 1, 2009
    Applicants: Versitech Limited, Morningside Ventures Limited
    Inventors: Dan Yang, Chengyong Li, Shiwu Chen
  • Patent number: 7592344
    Abstract: 3-cyanonaphthalene-1-carboxylic acid perhydroxyalkylmethyl-piperazine compounds of formula I which are antagonistic to tachykinin receptors, pharmaceutical compositions containing such compounds, methods of using such compounds for the treatment and/or inhibition of various diseases and disorders, processes for preparing such piperazine compounds, and intermediate products of these processes.
    Type: Grant
    Filed: November 30, 2006
    Date of Patent: September 22, 2009
    Assignee: Solvay Pharmaceuticals GmbH
    Inventors: Jochen Antel, Daniel Jasserand, Uwe Schoen, Michael Firnges, Holger Sann, Reinhard Brueckner, Dania Reiche
  • Publication number: 20090233900
    Abstract: To provide a novel and excellent agent for treating or preventing nociceptive pain, neuropathic pain, cancer pain, headache, bladder function disorder and the like, based on the inhibitory action on the capsaicin receptor VR1 activation. The present invention was accomplished by confirming that a benzamide derivative characterized by the possession of a benzene ring in which a single ring is condensed on the nitrogen atom of amido group and possession of a lower alkylamino or an amino group substituted with a ring group at the neighboring position of said amido group has a strong inhibitory action on VR1 activation and excellent pharmacological actions based on this and by finding that it can become an excellent agent for treating or preventing VR1-involved diseases such as nociceptive pain, neuropathic pain, cancer pain, headache, bladder function disorder and the like.
    Type: Application
    Filed: November 29, 2006
    Publication date: September 17, 2009
    Applicant: Astellas Pharma Inc.
    Inventors: Takahiro Kuramochi, Ryoji Hirabayashi, Yohei Koganemaru, Ryosuke Munakata, Koichi Yonezawa, Tetsuo Kiso
  • Patent number: 7576204
    Abstract: A compound represented by the following general formula (I): (I) wherein R7 and R21 are the same or different and each represents optionally substituted C2-22 alkoxy, etc.; a pharmaceutically acceptable salt thereof or hydrates of the same. The compound (1) inhibits angiogenesis and inhibits the production of VEGF particularly under hypoxic conditions, which makes it useful as a remedy for solid cancer.
    Type: Grant
    Filed: July 31, 2003
    Date of Patent: August 18, 2009
    Assignees: Mercian Corporation, Eisai R&D Management Co., Ltd.
    Inventors: Mitsuo Nagai, Masashi Yoshida, Toshio Tsuchida
  • Publication number: 20090203696
    Abstract: Disclosed are compounds according to formula (I): wherein A, Q, X, Y, Z, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as defined herein. The disclosure also relates to pharmaceutical compositions containing a compound of formula (I), to processes for preparing the compounds of formula (I), and to methods of using the compounds of formula (I).
    Type: Application
    Filed: December 15, 2008
    Publication date: August 13, 2009
    Applicant: SANOFI-AVENTIS
    Inventors: Jozsef Zsolt BOCSKEI, Gary MCCORT, Hans MATTER, Henning STEINHAGEN, Berangere THIERS
  • Publication number: 20090192136
    Abstract: A compound of formula wherein the substituents are as described in the specification for the treatment of psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.
    Type: Application
    Filed: July 22, 2008
    Publication date: July 30, 2009
    Inventors: Daniela Alberati-Giani, Synese Jolidon, Robert Narquizian, Matthias Heinrich Nettekoven, Roger David Norcross, Emmanuel Pinard, Henri Stalder
  • Publication number: 20090176768
    Abstract: Diaza heterocyclic amide derivatives according to Formula (I) have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders: where R5, R6, R7, R8, R9, R10, m, Q, X, and Y are set forth in the description.
    Type: Application
    Filed: March 17, 2009
    Publication date: July 9, 2009
    Inventors: JAY P. POWERS, Daqing Sun, Xuelei Yan
  • Publication number: 20090170869
    Abstract: The present invention relates to 1-(1-methylethyl)-4-{[4-(tetrahydro-2H-pyran-4-yloxy)phenyl]carbonyl}piperazine or a pharmaceutically acceptable salt thereof, in particular the hydrochloride salt thereof and crystalline forms of the hydrochloride salt; to processes for the preparation of the compound or its salt; to compositions containing it; and to its use in the treatment or prophylaxis of neurological or psychiatric diseases, such as cognitive impairment, fatigue or a sleep disorder, for example in a mammal such as a human. The compound or a salt thereof has affinity for and is an antagonist and/or inverse agonist of the histamine H3 receptor.
    Type: Application
    Filed: September 4, 2008
    Publication date: July 2, 2009
    Inventors: Desmond John BEST, Sing Yeung Mak, Barry Sidney Orlek, Geracimos Rassias, Pamela Joan Theobald
  • Publication number: 20090162439
    Abstract: The present invention is directed to compositions and methods for preventing or inhibiting biofilm formation on a solid substrate comprising an antimicrobial agent and a biofilm-degrading enzyme embedded in a matrix material.
    Type: Application
    Filed: December 22, 2008
    Publication date: June 25, 2009
    Applicant: University of Louisville Research Foundation
    Inventor: Andrea S. Gobin
  • Publication number: 20090156611
    Abstract: The disclosure relates to compositions for and methods of inhibiting the mammalian Hedgehog signaling pathway.
    Type: Application
    Filed: November 10, 2006
    Publication date: June 18, 2009
    Applicant: Licentia Ltd.
    Inventors: Antti Oinas, Jussi Taipale, Juhani Lahdenperä
  • Publication number: 20090156589
    Abstract: A compound represented by the following general formula (1) or (100), a salt thereof or a hydrate of the foregoing has excellent cell adhesion inhibitory action and cell infiltration inhibitory action. wherein R10 represents 5- to 10-membered cycloalkyl etc. optionally substituted with hydroxyl etc., R30, R31 and R32 may be the same or different and each represents hydrogen etc., R40 represents C1-10 alkyl etc. optionally substituted with hydroxyl etc., n represents an integer of 0, 1 or 2, X1 represents CH or nitrogen, and R20, R21, R22 and R23 may be the same or different and each represents hydrogen etc.
    Type: Application
    Filed: June 14, 2006
    Publication date: June 18, 2009
    Applicant: EISAI R&D MANAGEMENT CO., LTD.
    Inventors: Tetsuya Kawahara, Makoto Kotake, Naoki Yoneda, Shinsuke Hirota, Masayoshi Ohkuro
  • Publication number: 20090131343
    Abstract: The invention provides methods utilizing bridged macrolide or tylosin derivatives for the treatment of patients with inflammatory bowel diseases. The methods of the invention provide for the administration to a patient of a therapeutically effective amount of a bridged macrolide or a tylosin derivative, pharmaceutically acceptable derivatives thereof, and combinations thereof for a period of time sufficient to obtain a desired alleviation of one or more symptoms of the inflammatory bowel disease.
    Type: Application
    Filed: November 14, 2008
    Publication date: May 21, 2009
    Inventors: Ly Tam Phan, Yat Sun Or
  • Publication number: 20090118298
    Abstract: The present invention is directed to novel compounds of Formula (I) pharmaceutically acceptable salts thereof, pro-drugs thereof, biologically active metabolites thereof, isomers thereof or stereoisomers thereof wherein the variables are as defined herein. The compounds of Formula (I) are useful as chemokine receptor antagonists and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, rheumatoid arthritis, osteoarthritis, multiple sclerosis and asthma.
    Type: Application
    Filed: September 25, 2008
    Publication date: May 7, 2009
    Inventors: Dawn M. George, Lu Wang, Biqin Li, Anna M. Ericsson, Graham K. Ansell
  • Patent number: 7524848
    Abstract: Diaza heterocyclic amide derivatives according to Formula (I) have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders: where R5, R6, R7, R8, R9, R10, m, Q, X, and Y are set forth in the description.
    Type: Grant
    Filed: March 22, 2007
    Date of Patent: April 28, 2009
    Assignee: Amgen Inc.
    Inventors: Jay P. Powers, Daqing Sun, Xuelei Yan
  • Publication number: 20090105208
    Abstract: Compounds of Formula (I): or pharmaceutically acceptable salts, solvates, or esters thereof, are useful in treating diseases or conditions mediated by CB1 receptors, such as metabolic syndrome and obesity, neuroinflammatory disorders, cognitive disorders and psychosis, addiction (e.g., smoking cessation), gastrointestinal disorders, and cardiovascular conditions.
    Type: Application
    Filed: June 25, 2008
    Publication date: April 23, 2009
    Inventors: Eric J. Gilbert, Michael W. Miller, Jack D. Scott, Duane Eugene DeMong, Andrew Stamford, William J. Greenlee, Chander Shekher Celly
  • Publication number: 20090099186
    Abstract: The embodiments provide compounds of the general Formulas I-IV, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.
    Type: Application
    Filed: October 10, 2006
    Publication date: April 16, 2009
    Inventors: Leonid Beigelman, Steven W. Andrews, Kevin R. Condroski, Indrani Gunawaradana, Julia Haas
  • Publication number: 20090069335
    Abstract: The invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein R1-3, R5-7, a, X, Y, Y?, Y?, and Z are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.
    Type: Application
    Filed: September 5, 2008
    Publication date: March 12, 2009
    Inventors: YuHua Ji, Craig Husfeld, YongQi Mu, Rick Lee, Li Li
  • Publication number: 20090062284
    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 biaryl-methanesulfinyl acetamides of Formula (I): wherein Ar, Y, R1, R2, R4, R5, q and x are as defined herein; and their use in the treatment of diseases, including treatment of sleepiness associated with narcolepsy, obstructive sleep apnea, or shift work disorder; Parkinson's disease; Alzheimer's disease; attention deficit disorder; attention deficit hyperactivity disorder; depression; or fatigue associated with a neurological disease; as well as the promotion of wakefulness.
    Type: Application
    Filed: August 27, 2008
    Publication date: March 5, 2009
    Applicant: Cephalon, Inc.
    Inventors: Edward R. Bacon, Sankar Chatterjee, Derek Dunn, Marie-Edith Gourdel, Greg A. Hostetler, Mohamed Iqbal, Brigitte Lesur, Philippe Louvet, Eric Riguet, Dominique Schweizer, Christophe Yue
  • Publication number: 20090036439
    Abstract: The present invention provides a compound of formula I and the use thereof for the inhibition of bacterial cell wall biosynthesis and for the therapeutic treatment of bacterial infection or disease in a patient in need thereof. The present invention also provides the use of the formula I compound for the control of ecto- or endoparasites in homeothermic animals.
    Type: Application
    Filed: September 19, 2008
    Publication date: February 5, 2009
    Applicant: Wyeth
    Inventors: Craig Eugene Caufield, Schuyler Adam Antane, Koi Michele Morris, Shaughnessy McGrath Naughton, Dominick Anthony Quagliato, Patrick Michael Andrae, Annmarie Enos, John F. Chiarello
  • Patent number: 7485644
    Abstract: The invention provides compounds of formula (I): or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein ring B represents a monocyclic aryl ring having six ring atoms or a monocyclic heteroaryl ring having up to six ring atoms and containing one or more ring heteroatoms wherein each said heteroatom is nitrogen; R2 represents a group selected from C1-6 alkyl or aryl, which said group is substituted by one or more fluorine groups; n is 1, 2 or 3; and R1 represents an optionally substituted group selected from C1-6 alkyl, C5-7 cycloalkyl, heterocycloalkyl, aryl, heteroaryl, C1-6 alkyl-aryl, C1-6 alkyl-heteroaryl, C1-6 alkyl-cycloalkyl or C1-6 alkyl-heterocycloalkyl. Processes for their preparation; pharmaceutical compositions containing them; and their use in the treatment of a disease condition mediated by one or more metalloproteinase enzymes.
    Type: Grant
    Filed: June 23, 2004
    Date of Patent: February 3, 2009
    Assignee: AstraZeneca AB
    Inventors: Maurice Raymond Verschoyle Finlay, David Waterson
  • Publication number: 20080317671
    Abstract: Certain non-imidazole heterocyclic compounds are histamine H3 modulators useful in the treatment of histamine H3 receptor mediated diseases.
    Type: Application
    Filed: August 20, 2008
    Publication date: December 25, 2008
    Inventors: Nicholas I. Carruthers, Chandravadan R. Shah, Devin M. Swanson
  • Publication number: 20080287430
    Abstract: Compounds of formula (I) or a pharmaceutically acceptable derivative thereof wherein X, Z, R1, R2a, R2b, R3, and Rx are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.
    Type: Application
    Filed: April 24, 2006
    Publication date: November 20, 2008
    Inventors: Rino Antonio Bit, Gerard Martin Paul Giblin, Adrian Hall, David Nigel Hurst, Ian Reginald Kilford, Tiziana Scoccitti
  • Publication number: 20080275059
    Abstract: The present invention relates to a compound represented by the formula (I): (wherein, R3, R6, R7 and R21 are the same as or different from one another and each represents a hydroxyl group etc.), a pharmacologically acceptable salt thereof or a hydrate of them. The compound (I) of the present invention suppresses angiogenesis, in particular, suppresses VEGF production in a hypoxic condition and is useful as a therapeutic agent for treating solid cancer.
    Type: Application
    Filed: October 29, 2007
    Publication date: November 6, 2008
    Inventors: Yoshihiko KOTAKE, Jun Niijima, Yoshio Fukuda, Mitsuo Nagai, Regina Mikie Kanada, Takashi Nakashima, Masahi Yoshida, Toshio Tsuchida
  • Publication number: 20080269245
    Abstract: In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel compounds of general formula (I): and pharmaceutically acceptable derivatives thereof, wherein R1, R2, R3, n, X and Y are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I) and a pharmaceutically acceptable carrier. The present invention further provides compounds capable of inhibiting histone deacetylatase activity and methods for treating disorders regulated by histone deacetylase activity (e.g., cancer and protozoal infections) comprising administering a therapeutically effective amount of a compound of formula (I) to a subject in need thereof. The present invention additionally provides methods for modulating the glucose-sensitive subset of genes downstream of Ure2p. The present invention also provides methods for preparing compounds of the invention.
    Type: Application
    Filed: July 17, 2007
    Publication date: October 30, 2008
    Inventors: Stuart L. Schreiber, Scott M. Sternson, Jason C. Wong, Christina M. Grozinger, Stephen J. Haggarty, Kathryn M. Koeller
  • Publication number: 20080255146
    Abstract: The present invention relates to a compound represented by the formula (I): (wherein, R3, R6, R7 and R21 are the same as or different from one another and each represents a hydroxyl group etc.), a pharmacologically acceptable salt thereof or a hydrate of them. The compound (I) of the present invention suppresses angiogenesis, in particular, suppresses VEGF production in a hypoxic condition and is useful as a therapeutic agent for treating solid cancer.
    Type: Application
    Filed: October 29, 2007
    Publication date: October 16, 2008
    Inventors: Yoshihiko KOTAKE, Jun Niijima, Yoshio Fukuda, Mitsuo Nagai, Regina Mikie Kanada, Takashi Nakashima, Masahi Yoshida, Toshio Tsuchida
  • Publication number: 20080255137
    Abstract: The present invention relates to certain N-biaryl and N-arylheteroaryl 2-substituted piperazine derivatives of Formula (Ia) that are modulators of the 5HT2C receptor. Accordingly, compounds of the present invention are useful for the treatment of 5HT2C receptor associated diseases or disorders, such as, obesity, Alzheimer Disease, erectile dysfunction and related disorders.
    Type: Application
    Filed: December 9, 2005
    Publication date: October 16, 2008
    Applicant: Arena Pharmaceuticals, Inc.
    Inventors: Brian M Smith, Vincent J. Santora, Rena Hayashi, Jason B. Ibarra, Jeffrey A. Schultz, Scott A. Estrada
  • Publication number: 20080255144
    Abstract: The invention provides a compound of formula (I) or a salt or solvate thereof: wherein R1, n, X, Y and Z are as defined in the specification, and uses of such compounds. The compounds inhibit GlyT1 transporters and are useful in the treatment of certain neurological and neuropsychiatric disorders, including schizophrenia.
    Type: Application
    Filed: March 9, 2006
    Publication date: October 16, 2008
    Inventors: Daniel Marcus Bradley, Clive Leslie Branch, Wai Ngor Chan, Steven Coulton, Anthony William Dean, Paul Martin Doyle, Brian Evans, Martin Leonard Gilpin, Sharon Lisa Gough, Jacqueline Anne Macritchie, Howard Robert Marshall, David John Nash, Roderick Alan Porter, Simon Edward Ward
  • Publication number: 20080234272
    Abstract: The invention relates to novel piperazine derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including pharmaceutical compositions containing one or more of those compounds and their use as medicaments for the treatment or prevention of protozoal infections, especially malaria.
    Type: Application
    Filed: October 20, 2006
    Publication date: September 25, 2008
    Applicant: Actelion Pharmaceuticals Ltd.
    Inventors: Christoph Binkert, Christoph Boss, Olivier Corminboeuf, Corinna Grisostomi, Solange Meyer
  • Publication number: 20080214564
    Abstract: The present invention provides the compound of formula (I) in a solid form which, as a bulk medicament for pharmaceutical manufacture, is uniform, has a high purity, and is easy to work with. The invention further provides a process for preparing this compound, and pharmaceutical compositions containing the same. A solid form of (8E,12E,14E)-7-{(4-cycloheptylpiperazin-1-yl)carbonyl}oxy-3,6,16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytricosa-8,12,14-trien-11-olide which has uniform specifications and is easy to work with was developed.
    Type: Application
    Filed: January 28, 2008
    Publication date: September 4, 2008
    Applicants: Eisai R&D Management Co., Ltd., MERCIAN CORPORATION
    Inventors: Hiroshi ISHIHARA, Manabu Sasho, Keizo Sato, Takashi Kamahara, Masashi Yoshida
  • Patent number: 7419980
    Abstract: The present invention is directed to fused-aryl and heteroaryl derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.
    Type: Grant
    Filed: October 12, 2004
    Date of Patent: September 2, 2008
    Assignee: Wyeth
    Inventors: Eugene John Trybulski, Paige Erin Mahaney, Lori Krim Gavrin, Joseph Peter Sabatucci, Gary Paul Stack
  • Publication number: 20080176841
    Abstract: Provided herein are novel epoxide inhibitors of cysteine proteases, compositions comprising the epoxide inhibitors, and packaged pharmaceuticals. Also provided are methods of inhibiting a papain-family cysteine protease and methods of treating or preventing a disease by administering a composition containing an epoxide inhibitor of the invention. The compositions may be administered in combination with another therapeutic agent.
    Type: Application
    Filed: June 13, 2007
    Publication date: July 24, 2008
    Applicant: THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITY
    Inventors: Matthew S. Bogyo, Amir M. Sadaghiani, Steven Verhelst
  • Patent number: 7396834
    Abstract: Compounds of general formula: wherein R1 and R2 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
    Type: Grant
    Filed: November 5, 2003
    Date of Patent: July 8, 2008
    Assignee: AstraZeneca AB
    Inventors: William Brown, Andrew Griffin, Niklas Plobeck, Christopher Walpole
  • Publication number: 20080161319
    Abstract: The present invention relates to compounds and pharmaceutically acceptable salts thereof and formulations comprising tenilsetam or pharmaceutically acceptable salts thereof that are useful in modulating inflammation. In particular, the compounds or pharmaceutically acceptable salts thereof are useful for treating or preventing a disease or disorder involving inflammation, including, but not limited to, delayed type hypersensitivity and contact hypersensitivity.
    Type: Application
    Filed: November 9, 2007
    Publication date: July 3, 2008
    Applicant: MELIOR DISCOVERY, INC.
    Inventors: Andrew Reaume, Heather Hain, Michael Saporito
  • Publication number: 20080128315
    Abstract: Biodegradable and resorbable polymer pouches are described for use with cardiac rhythm mamagent devices (CRMs) and other implantable medical devices (IMDs), i.e., a pouch, covering, or other receptacle capable of encasing, surrounding and/or holding the CRM or other IMD for the purpose of securing it in position, inhibiting or reducing bacterial growth, providing pain relief and/or inhibiting scarring or fibrosis on or around the CRM or other IMD. Optionally, the biodegradable and resorbable pouches of the invention include one or more drugs in the polymer matrix to provide prophylactic effects and alleviate side effects or complications associated with the surgery or implantation of the CRM or other IMD.
    Type: Application
    Filed: November 6, 2007
    Publication date: June 5, 2008
    Applicant: TyRx Pharma, Inc.
    Inventors: Fatima Buevich, Frank Do, William McJames, William Edelman, Arikha Moses, Mason Diamond
  • Publication number: 20080119477
    Abstract: The present invention relates to certain biarylz and arylheteroaryl piperazine derivatives of Formula (Ia) that are modulators of the 5HT2c receptor. Accordingly, compounds of the present invention are useful for the treatment of 5HT2c receptor associated diseases or disorders, such as, obesity, Alzheimer Disease, erectile dysfunction and related disorders.
    Type: Application
    Filed: December 9, 2005
    Publication date: May 22, 2008
    Inventors: Brian M. Smith, Vincent J. Santora, Rena Hayashi, Jason B. Ibarra, Jeffrey A. Schultz, Scott A. Estrada
  • Patent number: 7354919
    Abstract: Described herein are compounds that are useful as protein kinase inhibitors, especially inhibitors of ERK, having the formula: where A, B, R1, R2, T and Ht are described in the specification. The compounds are useful for treating diseases in mammals that are alleviated by a protein, kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.
    Type: Grant
    Filed: July 24, 2003
    Date of Patent: April 8, 2008
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Michael R. Hale, James W. Janetka, Francois Maltais, Jingrong Cao