Ring Oxygen In The Additional Hetero Ring Patents (Class 514/254.1)
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Publication number: 20100160322Abstract: 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: ApplicationFiled: December 4, 2009Publication date: June 24, 2010Applicant: ABBOTT LABORATORIESInventors: 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
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Publication number: 20100125075Abstract: 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: ApplicationFiled: December 14, 2006Publication date: May 20, 2010Applicant: British Biotech Pharmaceuticals Ltd.Inventors: Lisa Marie Pratt, Kenneth Noel Keavey, Gilles Denis Pain, Laurent Mounier
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Publication number: 20100124543Abstract: 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: ApplicationFiled: July 16, 2009Publication date: May 20, 2010Applicant: Vertex Pharmaceuticals IncorporatedInventors: Roger Dennis Tung, Michael Robin Hale, Christopher Todd Baker, Eric Steven Furfine, Istvan Kaldor, Wieslaw Mieczylaw Kazmierski, Andrew Spaltenstein
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Publication number: 20100125071Abstract: The present invention relates to compounds of formula (I) with the substituents as defined herein, and uses thereof.Type: ApplicationFiled: June 4, 2008Publication date: May 20, 2010Inventors: Neil John Press, Simon James Watson
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Publication number: 20100120789Abstract: 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 heteroType: ApplicationFiled: September 7, 2009Publication date: May 13, 2010Inventors: Nigel Vicker, Xiangdong Su, Fabienne Praduax, Michael John Reed, Barry Victor Lloyd Potter
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Publication number: 20100119503Abstract: 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: ApplicationFiled: September 25, 2008Publication date: May 13, 2010Applicant: INCYTE CORPORATIONInventors: Chu-Biao Xue, Changsheng Zheng, Hao Feng, Michael Xia, Joseph Glenn, Ganfeng Cao, Brian W. Metcalf
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Patent number: 7700586Abstract: 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: GrantFiled: September 4, 2002Date of Patent: April 20, 2010Assignee: 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
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Publication number: 20100086609Abstract: 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: ApplicationFiled: December 10, 2009Publication date: April 8, 2010Applicant: MANNKIND CORPORATIONInventors: Solomon S. Steiner, Rodney J. Woods, Joseph W. Sulner
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Publication number: 20100063040Abstract: 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: ApplicationFiled: September 25, 2006Publication date: March 11, 2010Inventor: Akira Kugimiya
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Publication number: 20100029607Abstract: 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: ApplicationFiled: September 22, 2009Publication date: February 4, 2010Inventors: Eric J. Gilbert, Michael W. Miller, Jack D. Scott, Andrew W. Stamford, William J. Greenlee, Jay Weinstein
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Publication number: 20090325978Abstract: 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: ApplicationFiled: August 13, 2007Publication date: December 31, 2009Inventors: Katsumi Onai, Makoto Yokayama
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Publication number: 20090264416Abstract: 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: ApplicationFiled: August 19, 2008Publication date: October 22, 2009Inventors: 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
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Publication number: 20090253656Abstract: 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: ApplicationFiled: March 29, 2006Publication date: October 8, 2009Applicant: Kabushiki Kaisha Yakult HonshaInventors: Ryuta Yamazaki, Yukiko Nishiyama, Tomio Furuta, Takeshi Matsuzaki, Hiroshi Hatano, Oh Yoshida, Masato Nagaoka, Ritsuo Aiyama, Shusuke Hashimoto, Yoshikazu Sugimoto
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Publication number: 20090253684Abstract: 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: ApplicationFiled: December 2, 2008Publication date: October 8, 2009Inventors: Romyr Dominique, Robert Alan Goodnow, JR., Agnieszka Kowalczyk, Qi Qiao, Achyutharao Sidduri, Jefferson Wright Tilley
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Publication number: 20090247503Abstract: 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: ApplicationFiled: March 25, 2009Publication date: October 1, 2009Applicants: Versitech Limited, Morningside Ventures LimitedInventors: Dan Yang, Chengyong Li, Shiwu Chen
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Patent number: 7592344Abstract: 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: GrantFiled: November 30, 2006Date of Patent: September 22, 2009Assignee: Solvay Pharmaceuticals GmbHInventors: Jochen Antel, Daniel Jasserand, Uwe Schoen, Michael Firnges, Holger Sann, Reinhard Brueckner, Dania Reiche
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Publication number: 20090233900Abstract: 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: ApplicationFiled: November 29, 2006Publication date: September 17, 2009Applicant: Astellas Pharma Inc.Inventors: Takahiro Kuramochi, Ryoji Hirabayashi, Yohei Koganemaru, Ryosuke Munakata, Koichi Yonezawa, Tetsuo Kiso
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Patent number: 7576204Abstract: 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: GrantFiled: July 31, 2003Date of Patent: August 18, 2009Assignees: Mercian Corporation, Eisai R&D Management Co., Ltd.Inventors: Mitsuo Nagai, Masashi Yoshida, Toshio Tsuchida
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Publication number: 20090203696Abstract: 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: ApplicationFiled: December 15, 2008Publication date: August 13, 2009Applicant: SANOFI-AVENTISInventors: Jozsef Zsolt BOCSKEI, Gary MCCORT, Hans MATTER, Henning STEINHAGEN, Berangere THIERS
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Publication number: 20090192136Abstract: 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: ApplicationFiled: July 22, 2008Publication date: July 30, 2009Inventors: Daniela Alberati-Giani, Synese Jolidon, Robert Narquizian, Matthias Heinrich Nettekoven, Roger David Norcross, Emmanuel Pinard, Henri Stalder
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Publication number: 20090176768Abstract: 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: ApplicationFiled: March 17, 2009Publication date: July 9, 2009Inventors: JAY P. POWERS, Daqing Sun, Xuelei Yan
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Publication number: 20090170869Abstract: 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: ApplicationFiled: September 4, 2008Publication date: July 2, 2009Inventors: Desmond John BEST, Sing Yeung Mak, Barry Sidney Orlek, Geracimos Rassias, Pamela Joan Theobald
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Publication number: 20090162439Abstract: 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: ApplicationFiled: December 22, 2008Publication date: June 25, 2009Applicant: University of Louisville Research FoundationInventor: Andrea S. Gobin
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Publication number: 20090156611Abstract: The disclosure relates to compositions for and methods of inhibiting the mammalian Hedgehog signaling pathway.Type: ApplicationFiled: November 10, 2006Publication date: June 18, 2009Applicant: Licentia Ltd.Inventors: Antti Oinas, Jussi Taipale, Juhani Lahdenperä
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Publication number: 20090156589Abstract: 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: ApplicationFiled: June 14, 2006Publication date: June 18, 2009Applicant: EISAI R&D MANAGEMENT CO., LTD.Inventors: Tetsuya Kawahara, Makoto Kotake, Naoki Yoneda, Shinsuke Hirota, Masayoshi Ohkuro
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Publication number: 20090131343Abstract: 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: ApplicationFiled: November 14, 2008Publication date: May 21, 2009Inventors: Ly Tam Phan, Yat Sun Or
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Publication number: 20090118298Abstract: 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: ApplicationFiled: September 25, 2008Publication date: May 7, 2009Inventors: Dawn M. George, Lu Wang, Biqin Li, Anna M. Ericsson, Graham K. Ansell
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Patent number: 7524848Abstract: 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: GrantFiled: March 22, 2007Date of Patent: April 28, 2009Assignee: Amgen Inc.Inventors: Jay P. Powers, Daqing Sun, Xuelei Yan
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Publication number: 20090105208Abstract: 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: ApplicationFiled: June 25, 2008Publication date: April 23, 2009Inventors: Eric J. Gilbert, Michael W. Miller, Jack D. Scott, Duane Eugene DeMong, Andrew Stamford, William J. Greenlee, Chander Shekher Celly
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Publication number: 20090099186Abstract: 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: ApplicationFiled: October 10, 2006Publication date: April 16, 2009Inventors: Leonid Beigelman, Steven W. Andrews, Kevin R. Condroski, Indrani Gunawaradana, Julia Haas
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Publication number: 20090069335Abstract: 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: ApplicationFiled: September 5, 2008Publication date: March 12, 2009Inventors: YuHua Ji, Craig Husfeld, YongQi Mu, Rick Lee, Li Li
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Publication number: 20090062284Abstract: 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: ApplicationFiled: August 27, 2008Publication date: March 5, 2009Applicant: 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
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Publication number: 20090036439Abstract: 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: ApplicationFiled: September 19, 2008Publication date: February 5, 2009Applicant: WyethInventors: Craig Eugene Caufield, Schuyler Adam Antane, Koi Michele Morris, Shaughnessy McGrath Naughton, Dominick Anthony Quagliato, Patrick Michael Andrae, Annmarie Enos, John F. Chiarello
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Patent number: 7485644Abstract: 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: GrantFiled: June 23, 2004Date of Patent: February 3, 2009Assignee: AstraZeneca ABInventors: Maurice Raymond Verschoyle Finlay, David Waterson
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Publication number: 20080317671Abstract: Certain non-imidazole heterocyclic compounds are histamine H3 modulators useful in the treatment of histamine H3 receptor mediated diseases.Type: ApplicationFiled: August 20, 2008Publication date: December 25, 2008Inventors: Nicholas I. Carruthers, Chandravadan R. Shah, Devin M. Swanson
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Publication number: 20080287430Abstract: 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: ApplicationFiled: April 24, 2006Publication date: November 20, 2008Inventors: Rino Antonio Bit, Gerard Martin Paul Giblin, Adrian Hall, David Nigel Hurst, Ian Reginald Kilford, Tiziana Scoccitti
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Publication number: 20080275059Abstract: 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: ApplicationFiled: October 29, 2007Publication date: November 6, 2008Inventors: Yoshihiko KOTAKE, Jun Niijima, Yoshio Fukuda, Mitsuo Nagai, Regina Mikie Kanada, Takashi Nakashima, Masahi Yoshida, Toshio Tsuchida
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Publication number: 20080269245Abstract: 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: ApplicationFiled: July 17, 2007Publication date: October 30, 2008Inventors: Stuart L. Schreiber, Scott M. Sternson, Jason C. Wong, Christina M. Grozinger, Stephen J. Haggarty, Kathryn M. Koeller
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Publication number: 20080255146Abstract: 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: ApplicationFiled: October 29, 2007Publication date: October 16, 2008Inventors: Yoshihiko KOTAKE, Jun Niijima, Yoshio Fukuda, Mitsuo Nagai, Regina Mikie Kanada, Takashi Nakashima, Masahi Yoshida, Toshio Tsuchida
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Publication number: 20080255137Abstract: 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: ApplicationFiled: December 9, 2005Publication date: October 16, 2008Applicant: Arena Pharmaceuticals, Inc.Inventors: Brian M Smith, Vincent J. Santora, Rena Hayashi, Jason B. Ibarra, Jeffrey A. Schultz, Scott A. Estrada
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Publication number: 20080255144Abstract: 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: ApplicationFiled: March 9, 2006Publication date: October 16, 2008Inventors: 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
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Publication number: 20080234272Abstract: 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: ApplicationFiled: October 20, 2006Publication date: September 25, 2008Applicant: Actelion Pharmaceuticals Ltd.Inventors: Christoph Binkert, Christoph Boss, Olivier Corminboeuf, Corinna Grisostomi, Solange Meyer
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Publication number: 20080214564Abstract: 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: ApplicationFiled: January 28, 2008Publication date: September 4, 2008Applicants: Eisai R&D Management Co., Ltd., MERCIAN CORPORATIONInventors: Hiroshi ISHIHARA, Manabu Sasho, Keizo Sato, Takashi Kamahara, Masashi Yoshida
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Patent number: 7419980Abstract: 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: GrantFiled: October 12, 2004Date of Patent: September 2, 2008Assignee: WyethInventors: Eugene John Trybulski, Paige Erin Mahaney, Lori Krim Gavrin, Joseph Peter Sabatucci, Gary Paul Stack
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Publication number: 20080176841Abstract: 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: ApplicationFiled: June 13, 2007Publication date: July 24, 2008Applicant: THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITYInventors: Matthew S. Bogyo, Amir M. Sadaghiani, Steven Verhelst
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Patent number: 7396834Abstract: 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: GrantFiled: November 5, 2003Date of Patent: July 8, 2008Assignee: AstraZeneca ABInventors: William Brown, Andrew Griffin, Niklas Plobeck, Christopher Walpole
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Publication number: 20080161319Abstract: 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: ApplicationFiled: November 9, 2007Publication date: July 3, 2008Applicant: MELIOR DISCOVERY, INC.Inventors: Andrew Reaume, Heather Hain, Michael Saporito
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Publication number: 20080128315Abstract: 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: ApplicationFiled: November 6, 2007Publication date: June 5, 2008Applicant: TyRx Pharma, Inc.Inventors: Fatima Buevich, Frank Do, William McJames, William Edelman, Arikha Moses, Mason Diamond
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Publication number: 20080119477Abstract: 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: ApplicationFiled: December 9, 2005Publication date: May 22, 2008Inventors: Brian M. Smith, Vincent J. Santora, Rena Hayashi, Jason B. Ibarra, Jeffrey A. Schultz, Scott A. Estrada
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Patent number: 7354919Abstract: 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: GrantFiled: July 24, 2003Date of Patent: April 8, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael R. Hale, James W. Janetka, Francois Maltais, Jingrong Cao