Ring Chalcogen In The Additional Hetero Ring Patents (Class 544/374)
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Publication number: 20110212954Abstract: The present invention concerns an enantiomer R of a compound of Formula (I), wherein X is —NH—R1 or of Formula (V) or (VI), R1 is —(CH2)n—R2, R2 is a linear, branched or cyclic C1C6 aliphatic group, —O—(CH2)n—CH3, —NH—CO—(CH2)n—CH3, a 5- or 6-membered aliphatic or aromatic ring optionally comprising a heteroatom, a 5- or 6-membered aromatic ring substituted by one or two substituents, said substituents being selected from the group consisting of —OH, —O(alkyl C1C3) and —OCO(alkyl C1C3), or of Formula (V), R3 is H or a C1-C3 aliphatic group and R4 is a linear C1-C3 or a branched C3-C12 aliphatic group, or R3 is a C1-C3 aliphatic group and R4 is a linear C1-C12 aliphatic group, Y is O, CH—(CH2)n—CH3 or N(CO)(CH2)n—CH3, and n is an integer from O to 6.Type: ApplicationFiled: November 6, 2009Publication date: September 1, 2011Inventors: Mario Brufani, Ilaria Medici, Rinaldo Marini Bettolo, Luisa Maria Migneco, Rolando Marzella, Rocco Figliola, Angela La Bella
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Patent number: 8008302Abstract: The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof, in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.Type: GrantFiled: July 25, 2005Date of Patent: August 30, 2011Assignee: Merck Serono SAInventors: Dominique Swinnen, Agnes Bombrun, Jerome Gonzalez, Stefano Crosignani, Patrick Gerber, Catherine Jorand-Lebrun
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Publication number: 20110201584Abstract: Chemical entities that are bufalin derivatives, pharmaceutical compositions and methods of treatment of cancer are described.Type: ApplicationFiled: January 14, 2011Publication date: August 18, 2011Inventor: Xiangping Qian
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Publication number: 20110178096Abstract: 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: March 29, 2011Publication date: July 21, 2011Applicant: ABBOTT LABORATORIESInventors: Dawn M. George, Lu X. Wang, Biqin Li, Anna M. Ericsson, Graham K. Ansell
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Patent number: 7943768Abstract: A compound of formula (I) P—W—C(?X)-L-Q??(I) wherein P is an optionally substituted aryl or heteroaryl group; W is an optionally substituted 6 or 7-membered aliphatic ring comprising ring atoms Y1 and Y2 independently selected from Oxygen and Nitrogen, X is selected from Oxygen, Nitrogen and Sulphur; L is an optional C1-4 linker; and Q is an optionally substituted 4-7 membered aliphatic ring: for use in the treatment of chemokine mediated diseases or disorders.Type: GrantFiled: December 18, 2006Date of Patent: May 17, 2011Assignee: AstraZeneca ABInventors: Justin Fairfield Bower, Peter Wedderburn Kenny, Jeffrey Philip Poyser
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Publication number: 20110105522Abstract: The application discloses ketoconazole derivatives that are antagonists of the human pregnane X receptor (PXR), methods of preparing the derivatives, uses of the derivatives with drug therapy, and methods of inhibiting tumor cell proliferation and multidrug resistance using inhibitors of PXR.Type: ApplicationFiled: January 27, 2009Publication date: May 5, 2011Inventors: Sridhar Mani, Bhaskar C. Das
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Publication number: 20110086864Abstract: The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.Type: ApplicationFiled: December 16, 2010Publication date: April 14, 2011Inventors: Dominique Swinnen, Jerome Gonzalez
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Patent number: 7893068Abstract: 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: GrantFiled: October 29, 2007Date of Patent: February 22, 2011Assignees: Mercian Corporation, Eisai R&D Management Co., Ltd.Inventors: Yoshihiko Kotake, Jun Niijima, Yoshio Fukuda, Mitsuo Nagai, Regina Mikie Kanada, Takashi Nakashima, Masahi Yoshida, Toshio Tsuchida
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Publication number: 20110015171Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.Type: ApplicationFiled: April 22, 2010Publication date: January 20, 2011Inventors: Haiyan BIAN, Kristen Chevalier, Jose Clemente, Pete Connolly, Chris Flores, Shu-Chen Lin, Li Liu, John Mabus, Mark Macielag, Mark McDonnell, Philip Pitis, Yue-Mei Zhang, Sui-Po Zhang, Bin Zhu
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Patent number: 7868110Abstract: An initiator compound comprising an aryl or heteroaryl thioacetal including a substituent defined by the formula where x is an integer from 1 to about 5, y is an integer from 1 to about 5, the sum of x and y is from about 3 to about 6, ? is carbon, sulfur, oxygen, silicon, or an amino group, and each R1 is individually hydrogen or a monovalent organic group or where two or more R1 groups may join to form one or more rings.Type: GrantFiled: May 17, 2006Date of Patent: January 11, 2011Assignee: Bridgestone CorporationInventor: Yuan-Yong Yan
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Patent number: 7868009Abstract: The present invention is related to N-hydroxyamide derivatives of Formula (I): and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.Type: GrantFiled: January 27, 2006Date of Patent: January 11, 2011Assignee: Merck Serono, S.A.Inventors: Dominique Swinnen, Jerome Gonzalez
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Publication number: 20110003991Abstract: The use of a compound of formula I wherein Y is a single bond, C?O, C?S or S(O)m where m is 0, 1 or 2; the ring is a 6-membered aromatic or is a 5 or 6 membered heteroaromatic ring; Ra, R1, R2, R4 and R8 are specified organic groups; n and p are independently 0-4; or salts or N-oxides thereof or compositions containing them in controlling insects, acarines, nematodes or molluscs. Novel compounds are also provided.Type: ApplicationFiled: September 15, 2010Publication date: January 6, 2011Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Jérôme CASSAYRE, Peter MAIENFISCH, Fredrik CEDERBAUM, Louis-Pierre MOLLEYRES, Camilla CORSI, Thomas PITTERNA
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Patent number: 7851471Abstract: The present application relates to new compounds of formula (I), to pharmaceutical compositions comprising the compounds, to processes for their preparation, and to the use of the compounds as leptin receptor modulator mimetics in the preparation of medicaments against conditions associated with weight gain, type 2 diabetes and dyslipidemias.Type: GrantFiled: December 5, 2008Date of Patent: December 14, 2010Assignee: AstraZeneca AB (PUBL)Inventors: Joseph W. Boyd, Giles A. Brown, Michael Higginbottom
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Publication number: 20100311749Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein: A is C1-6alkyl, C3-6cycloalkyl, —CH2—R6, —CHMe-R7, —CMe2-R7, or optionally substituted aryl; wherein, when A is optionally substituted aryl, said aryl group is optionally substituted with 1 to 3 substituents, which may be the same or different, selected from the group consisting of halogen, C1-6alkyl, —CF3, C1-4alkoxy, C1fluoroalkoxy, cyano, NR8R9, and pyridyl wherein the pyridyl is optionally substituted by one methyl; R1 is chlorine, fluorine, —CF3, cyano or C1-6alkyl; R2, R3 and R5 independently are hydrogen, fluorine, chlorine, —CF3, cyano or C1-6alkyl, such that at least one of R2, R3 and R5 is other than hydrogen; R4 is hydrogen. These compounds and salts are thought to be P2X7 receptor antagonists. The invention also provides for the treatment of pain, inflammation, rheumatoid arthritis, osteoarthritis, or a neurodegenerative disease.Type: ApplicationFiled: October 24, 2008Publication date: December 9, 2010Inventors: Laura Jane Chambers, Katharine Laura Collis, David Kenneth Dean, Jorge Munoz-Muriedas, Jon Graham Anthony Steadman, Daryl Simon Walter
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Publication number: 20100311713Abstract: The present invention relates to new azetidine compounds, to pharmaceutical compositions containing them and the use of said compounds in the treatment of functional gastrointestinal disorders, IBS and functional dyspepsia. The compounds are neurokinin (NK) antagonists. The present invention further relates to processes for the preparation of the compounds.Type: ApplicationFiled: September 27, 2006Publication date: December 9, 2010Inventors: Rolf Bergman, Sara Holmqvist, Sverker Von Unge
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Publication number: 20100305078Abstract: The presently disclosed subject matter is directed to metallo-oxidoreductase inhibitors having metal binding moities linked to a targeting moiety through a linking group or a direct bond, methods for screening for metallo-oxidoreductase inhibitors, and methods of treating an oxidoreductase related disorder by administering a metallo-oxidoreductase inhibitor to a subject in need of treatment thereof.Type: ApplicationFiled: November 21, 2007Publication date: December 2, 2010Applicant: Viamet Pharmaceuticals, Inc.Inventors: Robert J. Schotzinger, William J. Hoekstra
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Publication number: 20100298323Abstract: 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: June 3, 2010Publication date: November 25, 2010Applicant: ABBOTT LABORATORIESInventors: Milan Bruncko, Yujia Dai, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa Hasvold, Laura Hexamer, Aaron R. 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, Todd M. Hansen
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Publication number: 20100291222Abstract: The present invention is directed to multiple a-lipoic acid-containing hydrophobic compounds (mALAs) capable of acting as scavengers of free radicals, metals and reactive oxygen species (ROS). Methods of synthesizing novel antioxidant mALAs, spontaneous emulsification or nanoprecipitaion thereof to produce antioxidant nanospheres and their use in preventing or treating diseases or conditions caused by oxidative stress and other free radical mediated conditions are also described. Another aspect of this invention is the use of these antioxidant nanospheres for the preparation of antioxidant particulate delivery system of therapeutic agents.Type: ApplicationFiled: December 30, 2008Publication date: November 18, 2010Applicant: CEDARS-SINAI MEDICAL CENTERInventors: John S. Yu, Bong Seop Lee
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Publication number: 20100286118Abstract: The present invention provides compounds of formula (I) in which y, m, n, R1, R2 and Q are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: May 6, 2010Publication date: November 11, 2010Inventors: Rhonan Ford, Andrew Mather, Antonio Mete, Ian Millichip
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Patent number: 7790887Abstract: 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: GrantFiled: January 28, 2008Date of Patent: September 7, 2010Assignees: Eisai R&D Management Co., Ltd., Mercian CorporationInventors: Hiroshi Ishihara, Manabu Sasho, Keizo Sato, Takashi Kamahara, Masashi Yoshida
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Publication number: 20100204242Abstract: 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: August 12, 2010Inventors: Desmond John Best, Sing Yeung Mak, Barry Sidney Orlek, Geracimos Rassias, Pamela Joan Theobald
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Publication number: 20100197919Abstract: The present invention provides a method for producing a 12-membered ring macrolide compound expected as a prophylactic or therapeutic agent for solid tumors and the like, and a production intermediate thereof. In detail, by acetalizing hydroxyl groups at 6- and 7-positions of a 12-membered ring macrolide compound being a raw material with dialkyl tin (IV) oxide and, after that, reacting the product with a carbamoyl halide derivative, the 7-position urethane derivative of the 12-membered ring macrolide compound being the target is effectively produced, without protecting hydroxyl groups at other positions.Type: ApplicationFiled: July 4, 2008Publication date: August 5, 2010Inventors: Toshio Tsuchida, Masashi Yoshida, Kazuo Ohta, Katsura Kaneko, Kaichiro Kominato
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Publication number: 20100184766Abstract: 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: January 18, 2010Publication date: July 22, 2010Applicant: ABBOTT LABORATORIESInventors: Aaron R. Kunzer, Steven W. Elmore, Laura A. Hexamer, Cheol-Min Park, Andrew J. Souers, Gerard M. Sullivan, Gary T. Wang, Xilu Wang, Michael D. Wendt
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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: 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: 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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Publication number: 20100098653Abstract: The present invention describes polymers containing 1,2-dithiolanes capable of acting as scavengers of free radicals, metals and reactive oxygen species. Also described are methods of synthesizing the antioxidant 1,2-dithiolane derivatives and polymerization thereof to produce biodegradable antioxidant polymers. The antioxidant polymers of the present invention may be used to treat diseases or conditions caused by oxidative stress and other free radical mediated conditions. The antioxidant polymers may also be used for the preparation of antioxidant particulate delivery devices of therapeutic agents.Type: ApplicationFiled: February 29, 2008Publication date: April 22, 2010Applicant: CEDARS-SINAI MEDICAL CENTERInventors: John S. Yu, Bong Seop Lee
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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: 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: 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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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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Publication number: 20090227795Abstract: A method of measuring the binding activity of a test compound to a splicing factor 3b (SF3b), which comprises the following steps of: (a) contacting a labeled pladienolide compound and a test compound with a cell or a cell fraction; and (b) measuring the distribution of the bound labeled compound. The method enables to screen for a novel active compound capable of acting on (binding to) a pladienolide target molecule or the like.Type: ApplicationFiled: August 2, 2007Publication date: September 10, 2009Applicant: Eisai R & D Management Co., Ltd.Inventors: Yoshihiko Kotake, Koji Sagane, Takashi Owa, Yoshiharu Mizui, Hajime Shimizu, Yuko Kiyosue
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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: 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: 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: 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: 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: 7528130Abstract: A cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for killing selected cell populations comprising: (A) a cytotoxic amount of one or more taxanes covalently bonded to a cell binding agent through a linking group, and (B) a pharmaceutically acceptable carrier, diluent or excipient. A method for killing selected cell populations comprising contacting target cells or tissue containing target cells with an effective amount of a cytotoxic agent comprising one or more taxanes linked to a cell binding agent. Novel sulfur-containing taxanes.Type: GrantFiled: January 6, 2006Date of Patent: May 5, 2009Assignee: Immunogen Inc.Inventors: Ravi V. J. Chari, Walter A. Blättler
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Patent number: 7524846Abstract: The present invention is directed to arylalkyl- and cycloalkylalkyl-piperazine 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: April 28, 2009Assignee: WyethInventor: Paige Erin Mahaney
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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: 20090099199Abstract: The invention relates to compound of the formula I wherein the substituents are as defined in the specification; in free base form or in acid addition salt form; to its preparation, to its use as medicament and to medicaments comprising it.Type: ApplicationFiled: October 15, 2008Publication date: April 16, 2009Inventors: Joachim Nozulak, David Orain, Simona Cotesta
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Patent number: 7491723Abstract: The present invention is directed to alkanoyl and cycloalkanoyl-amine 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: February 17, 2009Assignee: WyethInventors: Eugene John Trybulski, Paige Erin Mahaney, Lori Krim Gavrin, William Jay Moore, Joseph Peter Sabatucci
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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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Patent number: 7479559Abstract: The present invention relates to novel benzyl(idene)-lactam derivatives, compounds of the formula I wherein R1 is a group of the formula G1 or G2 depicted below, wherein R1, R3, R6, R13 X, a, n and m are as defined herein, their pharmaceutically acceptable salts, and pharmaceutical compositions which include selective antagonists, inverse agonists and partial agonists of serotonin 1 (5-HT1) receptors, specifically, of one or both of the 5-HT1A and 5-HT1B receptors. The compounds of the invention are useful in treating or preventing depression, anxiety, obsessive compulsive disorder (OCD) and other disorders for which a 5-HT1 agonist or antagonist is indicated and have reduced potential for cardiac side effects, in particular QTc prolongation.Type: GrantFiled: March 17, 2005Date of Patent: January 20, 2009Assignee: Pfizer Inc.Inventors: Michael Aaron Brodney, Stephane Caron, Christopher John Helal, Jeffrey W. Raggon, Yong Tao, Nga M. Do
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Patent number: 7476669Abstract: A cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for killing selected cell populations comprising: (A) a cytotoxic amount of one or more taxanes covalently bonded to a cell binding agent through a linking group, and (B) a pharmaceutically acceptable carrier, diluent or excipient. A method for killing selected cell populations comprising contacting target cells or tissue containing target cells with an effective amount of a cytotoxic agent comprising one or more taxanes linked to a cell binding agent. Novel sulfur-containing taxanes.Type: GrantFiled: April 18, 2007Date of Patent: January 13, 2009Assignee: Immunogen Inc.Inventors: Ravi V. J. Chari, Walter A. Blättler
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Patent number: 7465741Abstract: The invention concerns substituted tricyclic isoxazoline derivatives according to Formula (I), the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N-oxide form thereof, more in particular tricyclic dihydrobenzopyranoisoxazoline, dihydroquinolinoisoxazoline, dihydronaphthalenoisoxazoline and dihydrobenzothiopyranoisoxazoline derivatives substituted on the phenylpart of the tricyclic moiety with at least one radical that is attached to the phenyl radical by a carbon-carbon bond as well as processes for their preparation, pharmaceutical compositions comprising them and their use as a medicine, in particular for treating depression, anxiety, movement disorders, psychosis, Parkinson's disease and body weight disorders including anorexia nervosa and bulimia, wherin all variables are defined in claim 1.Type: GrantFiled: August 12, 2003Date of Patent: December 16, 2008Assignee: Janssen Pharmaceutica N.V.Inventors: José Ignacio Andrés-Gil, José Manuel Bartolomé-Nebreda, Rosa Maria Alvarez-Escobar, Margaretha Henrica Maria Bakker, Antonius Adrianus Hendrikus Petrus Megens
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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: 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: 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