Chalcogen Bonded Directly At The 2-position Of The Oxazole Ring Patents (Class 548/221)
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Publication number: 20110306614Abstract: The invention relates to N-hydroxysulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxysulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxysulfonamide derivatives.Type: ApplicationFiled: August 19, 2011Publication date: December 15, 2011Applicants: THE JOHNS HOPKINS UNIVERSITY, CARDIOXYL PHARMACEUTICALS, INC.Inventors: John P. Toscano, Frederick Arthur Brookfield, Andrew D. Cohen, Stephen Martin Courtney, Lisa Marie Frost, Vincent Jacob Kalish
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Publication number: 20110301156Abstract: Vanilloid receptor ligand compounds corresponding to formula I: pharmaceutical compositions containing such compounds, a process for producing such compounds, and methods of using such compounds for treating or inhibiting pain and various other disorders or conditions.Type: ApplicationFiled: August 16, 2011Publication date: December 8, 2011Applicant: Gruenenthal GmbHInventors: Robert Frank, Gregor Bahrenberg, Thomas Christoph, Klaus Schiene, Jean De Vry, Derek Saunders, Bernd Sundermann, Jeewoo Lee
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Patent number: 8071593Abstract: Described are compounds which inhibit, regulate and/or modulate kinase signal transduction, for example of Met kinase. The compounds are of the formulae A1 to A148 and B1 described herein, including 2-oxobenzoxazol-3-ylmethyl]phenyl}carbamate and 2-oxooxazolo[4,5-b]pyridin-3-ylmethyl)phenyl]carbamate compounds, and pharmaceutically usable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. Also described are compositions containing these compounds. Also described are methods for the treatment of diseases in which the inhibition, regulation and/or modulation of kinase signal transduction plays a role by administering these compounds.Type: GrantFiled: May 8, 2008Date of Patent: December 6, 2011Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Oliver Schadt, Dieter Dorsch, Frank Stieber, Andree Blaukat
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Patent number: 8063067Abstract: Compounds of the formula (I): in which R, R1, R2 and R3 are as defined in the description, the use thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes, pharmaceutical compositions comprising them, and processes for the preparation of these compounds.Type: GrantFiled: July 23, 2009Date of Patent: November 22, 2011Assignee: Merck Patent GmbHInventors: Jean Jacques Zeiller, Hervè Dumas, Valérie Guyard-Dangremont, Isabelle Berard, Francis Contard, Daniel Guerrier, Gérard Ferrand, Yves Bonhomme
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Publication number: 20110251212Abstract: A compound which specifically binds to a receptor of NR1/NR2B, and is used as a NR2B receptor antagonist is provided. It has been found out that a piperazine derivative represented by the formula (I) binds specifically to a receptor of NR1/NR2B, and is used as a NR2B receptor antagonist. A compound represented by: wherein R1 is each independently C1-C3 alkyl or the like, m is an integer of 0 to 4, X is —N(R4)—C(?O)—C(?O)—, —N(R4)—(CR5R6)p—C(?O)—, —N(R4)—C(?O)—(CR7R8)q— or —C(?O)—N(R4)—(CR7R8)q—, p and q are each independently an integer of 1 to 3, R4, R5, R6, R7 and R8 are each independently a hydrogen atom or lower alkyl, A1 is benzoxazolinone or the like, and A2 is optionally substituted phenyl or the like, or a pharmaceutically acceptable salt or a solvate thereof.Type: ApplicationFiled: August 19, 2008Publication date: October 13, 2011Applicant: SHIONOGI & CO., LTD.Inventors: Moriyasu Masui, Minoru Tomida, Naotake Kobayashi, Kousuke Anan, Aya Tazawa, Kayoko Hata
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Publication number: 20110251200Abstract: The invention provides to a family of aryl guanidine-based F1F0-ATPase inhibitors, e.g., mitochondrial F1F0-ATPase inhibitors, methods for their discovery, and their use as therapeutic agents for treating certain disorders.Type: ApplicationFiled: September 11, 2009Publication date: October 13, 2011Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Gary D. Glick, Peter Toogood, Gina Ney
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Patent number: 7999115Abstract: The invention relates to compounds of formula (I) wherein R1 represents H, alkyl, alkoxy, cyano or halogen; one of U and X represents CH or N and the other represents CH, or, in the case of U, may also represent CRa and, in the case of X, may also represent CRb; Ra represents halogen; Rb represents halogen or alkoxy; B represents N, D represents CH2 and A represents CH(OH)CH2 or CH2CH2, or B represents CH, D represents CH2 or O and A represents OCH2, CH2CH(OH), CH(OH)CH2, CH(OH)CH(OH), CH?CH, CH2CH2 or NHCO, or also B represents C(OH), D represents CH2 and A represents OCH2, CH2CH(OH), CH(OH)CH2, CH(OH)CH(OH), CH?CH, CH2CH2 Or NHCO; R2 represents H, alkyl, alkenyl, hydroxyalkyl or alkoxycarbonylalkyl; and E represents naphthyl or a binuclear heterocyclic group; and to salts of such compounds. These compounds are useful as antimicrobial agents.Type: GrantFiled: August 29, 2007Date of Patent: August 16, 2011Assignee: Actelion Pharmaceutical Ltd.Inventors: Christian Hubschwerlen, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
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Patent number: 7999086Abstract: The invention provides a method of conditioning azo pigments containing carboxylic ester groups, using glycol monoalkyl ethers or mixtures of glycols and glycol dialkyl ether.Type: GrantFiled: January 30, 2009Date of Patent: August 16, 2011Assignee: Clariant Finance (BVI) LimitedInventors: Jens Paetzold, Carsten Plueg, Frank Alfter
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Publication number: 20110195932Abstract: Combinations comprising (or consisting essentially of) one or more compounds of formula (1) with one or more ancillary agents, to processes for preparing the combinations, and to various therapeutic uses of the combinations. Also provided are pharmaceutical compositions containing the combinations as well as a method of treatment of Duchenne muscular dystrophy, Becker muscular dystrophy or cachexia using the combinations.Type: ApplicationFiled: August 1, 2008Publication date: August 11, 2011Inventors: Graham Michael Wynne, Stephen Paul Wren, Peter David Johnson, Paul Damien Price, Olivier De Moor, Gary Nugent, Richard Storer, Richard Joseph Pye, Colin Richard Dorgan
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Publication number: 20110182828Abstract: The present invention provides compounds of Formula (I), and pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, or isomers of said compounds), having the general structure: wherein L, R1, R2, R3, R4, R5, and R6 are selected independently of each other and as defined herein. The present invention also provides compounds (and salts, solvates, esters, prodrugs, tautomers, and isomers) of Formulas II, III, IV, V, and VI, as defined herein. Also provided are pharmaceutical compositions, methods of preparing, and methods of using such compounds in the treatment and prophylaxis of a wide range of immune, autoimmune, and inflammatory diseases and conditions.Type: ApplicationFiled: December 18, 2008Publication date: July 28, 2011Applicant: Schering CorporationInventors: John C. Anthes, Kevin D. Mccormick, John A. Hey, Robert G. Aslanian, Purakkattle J. Biju, Michael Y. Berlin, Daniel M. Solomon, Phillippa H. Solomon, Hongwu Yang, Yeon-Hee Lim, Yoon Joo Lee, Rema Danielle Bitar
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Patent number: 7982067Abstract: Compounds of the formula (II) and (IV) are provided, which may be employed as intermediates for making compounds useful in treating respiratory diseases.Type: GrantFiled: July 14, 2010Date of Patent: July 19, 2011Assignee: Glaxo Group LimitedInventors: Philip Charles Box, Diane Mary Coe, Brian Edgar Looker, Inderjit Singh Mann, Panayiotis Alexandrou Procopiou
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Patent number: 7951955Abstract: This invention relates to compounds of formula I their salts, and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions comprising these compounds and their use in the treatment of picornavirus infections in mammals, as well as novel intermediates useful in the preparation of the compounds of formula I.Type: GrantFiled: May 1, 2008Date of Patent: May 31, 2011Assignee: Biota Scientific Management Pty LtdInventors: Keith Watson, Guy Krippner, Pauline Stanislawski, Darryl McConnell
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Patent number: 7939670Abstract: A compound of the formula (I), (II), (III) or (IV) wherein Z, A, B, C, R, R1, R2, Q, and n are as described herein.Type: GrantFiled: February 23, 2009Date of Patent: May 10, 2011Assignee: Purdue Pharma L.P.Inventors: Qun Sun, R. Richard Goehring, Donald Kyle, Zhengming Chen, Sam Victory, John Whitehead
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Publication number: 20110105477Abstract: The present invention relates to HIV protease, and methods for inhibiting the function of HIV protease. In particular, present invention provides compounds that inhibit or block the biological activity of HIVp, thereby causing the replication of the HIV virus to be inhibited or to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS. The compounds and formulations also find use in diagnostic and research settings.Type: ApplicationFiled: September 12, 2008Publication date: May 5, 2011Applicant: The Regents of the University of MichiganInventors: Heather A. Carlson, Kelly L. Damm, Kristen L. Meagher
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Publication number: 20110098302Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the antagonists of PGD2 receptors described herein, as well as methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.Type: ApplicationFiled: February 12, 2009Publication date: April 28, 2011Applicant: AMIRA PHARMACEUTICALS, INC.Inventors: John Howard Hutchinson, Thomas Jon Seiders, Brian Andrew Stearns, Bowei Wang, Yen Pham Truong, Jeannie M. Arruda
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Publication number: 20110021762Abstract: A process is provided for the synthesis of 4,5-diamino cyclohexene carboxylate ester (1): or a pharmaceutically acceptable salt thereof. R1-R3 are a silyl-, an aliphatic, alicyclic, aromatic, arylaliphatic, or an arylalicyclic group. R4, R11 and R12 are H, a silyl-group, an aliphatic, alicyclic, aromatic, arylaliphatic, or an arylalicyclic group. 3,4-Dihydropyran compound (9): with R5 and R6 being suitable protecting groups, is reacted to form aldehyde (4): which is oxidized and converted to N-substituted carbamate (3): with R7 being a suitable protecting group. (3) is, via oxazolinidone (13): converted to azido carboxylate ester (2): and then to 4,5-diamino cyclohexene carboxylate ester (1).Type: ApplicationFiled: December 10, 2008Publication date: January 27, 2011Applicant: NANYANG TECHNOLOGICAL UNIVERSITYInventors: Xuewei Liu, Jimei Ma
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Publication number: 20110021573Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the antagonists of PGD2 receptors described herein, as well as methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.Type: ApplicationFiled: February 25, 2009Publication date: January 27, 2011Applicant: AMIRA PHARMACEUTICALS, INC.Inventors: John Howard Hutchinson, Brian Andrew Stearns, Thomas Jonathan Seiders, Jill Melissa Scott, Jeannie M. Arruda, Bowei Wang
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Patent number: 7868204Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.Type: GrantFiled: March 25, 2005Date of Patent: January 11, 2011Assignee: MethylGene Inc.Inventors: Daniel Delorme, Soon Hyung Woo, Arkadii Vaisburg, Oscar Moradei, Silvana Leit, Stephane Raeppel, Sylvie Frechette, Giliane Bouchain
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Publication number: 20100331298Abstract: Chemokine receptor antagonists, in particular, compounds of Formula (I) that act as antagonists of the chemokine CCR2 receptor, including pharmaceutical compositions and uses thereof to treat or prevent diseases associated with monocyte accumulation, lymphocyte accumulation or leukocyte accumulation are described herein.Type: ApplicationFiled: December 10, 2008Publication date: December 30, 2010Applicant: CytoPathfinder, Inc.Inventors: Efrat Ben-Zeev, Dongli Chen, Merav Fichman, Shomir Ghosh, Steffi Koerner, Jian Lin, Yael Marantz, Rosa E. Melendez, Pradyumna Mohanty, Sharon Shacham, Zhaoda Zhang
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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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Publication number: 20100267945Abstract: A compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof, where R1 is optionally substituted lower alkyl, Y is —S(O)2—, R2 is hydrogen or optionally substituted lower alkyl, R7 is hydrogen or optionally substituted lower alkyl, X is a group of the formula: where R5 and R6 are each independently hydrogen, a group of the formula: is optionally substituted cycloalkylene, p is 0, and q is 1 or 2, Z is optionally substituted carbocyclyl or optionally substituted heterocyclyl, and provided that a compound wherein Z is fused heterocyclyl consisting of three rings or optionally substituted pyrimidinyl is excluded.Type: ApplicationFiled: June 25, 2010Publication date: October 21, 2010Applicant: Shionogi & Co., Ltd.Inventors: Takayuki Okuno, Naoki Kouyama, Masahiro Sakagami
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Publication number: 20100267714Abstract: The invention provides novel heterocyclic compounds, pharmaceutical compositions and methods of treatment that modulate levels of MIF expression and treat disorders associated with high or low levels of MIF expression.Type: ApplicationFiled: May 4, 2010Publication date: October 21, 2010Inventors: William L. Jorgensen, Richard J. Bucala
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Publication number: 20100267689Abstract: The present invention comprises compounds of Formula (I): wherein: X, R1, R2, R3, and R4 are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).Type: ApplicationFiled: April 15, 2010Publication date: October 21, 2010Inventors: Xuqing Zhang, Heather Rae Hufnagel, Cuifen Hou, Dana L. Johnson, Zhihua Sui
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Patent number: 7812040Abstract: This invention is directed to a compound of the formula Ia or Ib, as defined herein, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing a compound of formula I, a method of treatment of a disorder or condition that may be treated by antagonizing histamine H3 receptors, the method comprising administering to a mammal in need of such treatment a compound of formula I as described above, and a method of treatment of a disorder or condition selected from the group consisting of depression, mood disorders, schizophrenia, anxiety disorders, Alzheimer's disease, attention-deficit disorder (ADD), attention-deficit hyperactivity disorder (ADHD), psychotic disorders, sleep disorders, obesity, dizziness, epilepsy, motion sickness, respiratory diseases, allergy, allergy-induced airway responses, allergic rhinitis, nasal congestion, allergic congestion, congestion, hypotension, cardiovascular disease, diseases of the GI tract, hyper and hypo motility and acidic secretion of the gastro-iType: GrantFiled: June 12, 2006Date of Patent: October 12, 2010Assignee: Pfizer Inc.Inventor: Travis T Wager
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Publication number: 20100256130Abstract: The present invention relates to morpholinyl, and pyrrolidinyl analogs, pharmaceutical compositions containing them, and their use as antagonists of urotensin II.Type: ApplicationFiled: May 19, 2010Publication date: October 7, 2010Inventors: Krista B. Goodman, Michael J. Neeb, Clark A. Sehon, Andrew Q. Viet, Gren Z. Wang
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Publication number: 20100249132Abstract: Compounds of the formula (I), in which R1, D, E, L, Q, X and q have the meanings indicated in Claim 1, can and be employed for the treatment of tumours.Type: ApplicationFiled: September 9, 2008Publication date: September 30, 2010Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Melanie Schultz, Kai Schiemann, Gerard Botton, Andree Blaukat, Ingo Kober
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Publication number: 20100249124Abstract: The present invention relates to compounds of formula I wherein R1a to R1c, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.Type: ApplicationFiled: March 19, 2010Publication date: September 30, 2010Inventors: Daniel Hunziker, Christian Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
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Patent number: 7795287Abstract: A compound having a structure is disclosed herein. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: GrantFiled: August 30, 2007Date of Patent: September 14, 2010Assignee: Allergan, Inc.Inventor: David W. Old
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Patent number: 7759492Abstract: An enantioselective route to compounds of formula I is disclosed: The compounds of formula I are key intermediates in the synthesis of compounds useful in treatment of Alzheimer's disease.Type: GrantFiled: August 17, 2005Date of Patent: July 20, 2010Assignee: Merck Sharp & Dohme LimitedInventors: Stephen Philip Keen, Steven Fraser Oliver, Gavin William Stewart
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Publication number: 20100173961Abstract: The invention relates to benzooxazol-2-one derivatives of general formula (I) with the meanings indicated in the description, the pharmaceutically usable salts thereof, and the use thereof as medicinal substances.Type: ApplicationFiled: March 18, 2010Publication date: July 8, 2010Applicant: SANOFI-AVENTISInventors: Gerhard ZOLLER, Stefan PETRY, Gunter MÜLLER, Hubert HEUER, Norbert TENNAGELS
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Publication number: 20100158996Abstract: A novel therapeutic agent for hyperlipidemia, which is an ester compound represented by the formula (1?) (wherein R1 and R2 are each hydrogen atom or optionally substituted aryl, etc.; X is —COO— or —CON(R10)—; R3 and R4 are each hydrogen atom, C1-C6 alkyl or C1-C6 alkoxy, etc.; R5, R6 and R7 are each hydrogen atom, C1-C6 alkyl or C1-C6 alkoxy, etc.; R9 and R9 are each independently hydrogen atom, C1-C6 alkyl, —CON(R18) (R19) or —COO(R20), etc.; ring A, ring B and ring C are each independently aryl or heterocycle residue, etc.; Alk1 and Alk2 are each independently alkanediyl, etc.; l and m are each an integer of 0 or 1 to 3) or a prodrug thereof, or a pharmaceutically acceptable salt of either. The therapeutic agent selectively inhibits MTP in the small intestine, thus causes no such side effect as a fatty liver.Type: ApplicationFiled: February 12, 2010Publication date: June 24, 2010Inventors: Atsushi Hagiwara, Yasuhiro Ohe, Naoya Odani, Shizue Watanabe, Taku Ikenogami, Takashi Kawai, Kenya Madono, Toshio Taniguchi
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Publication number: 20100137274Abstract: The invention relates to the field of blood coagulation. Novel oxazolidinone derivatives of the general formula (I) processes for their preparation and their use as medicinally active compounds for the prophylaxis and/or treatment of disorders are described.Type: ApplicationFiled: June 30, 2009Publication date: June 3, 2010Applicant: Bayer Schering Pharma AGInventors: Alexander Straub, Thomas Lampe, Jens Pohlmann, Susanne Rohrig, Elisabeth Perzborn, Karl-Heinz Schlemmer, Joseph Pernerstorfer
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Patent number: 7728020Abstract: The present invention relates to new amino acid derivatives, process for the production, their use, in particular in transplantation, and pharmaceutical compositions containing them.Type: GrantFiled: March 8, 2005Date of Patent: June 1, 2010Assignee: Novartis AGInventors: Klaus Hinterding, Klemens Högenauer
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Patent number: 7709513Abstract: The invention relates to benzooxazol-2-one derivatives of general formula (I) with the meanings indicated in the description, the pharmaceutically usable salts thereof, and the use thereof as medicinal substances.Type: GrantFiled: December 5, 2007Date of Patent: May 4, 2010Assignee: Sanofi-AventisInventors: Gerhard Zoller, Stefan Petry, Gunter Müller, Hubert Heuer, Norbert Tennagels
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Patent number: 7683182Abstract: The present invention is directed to monohydrate and anhydrate crystal forms of 2-(3-fluoro-4-hydroxyphenyl)-7-vinyl-1,3-benzoxazol-5-ol, an estrogenic receptor modulator useful in the treatment of, for example, diseases related to abnormal levels of estrogen.Type: GrantFiled: March 6, 2006Date of Patent: March 23, 2010Assignee: Wyeth LLCInventors: Abdolsamad Tadayon, Silvio Iera, Hong Wen, Marc S. Tesconi, Mannching Sherry Ku
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Publication number: 20100063298Abstract: A method of preparing novel [11C]-labeled benzophenone/bezoxazole analogues is provided. The present invention also provides novel [11C]-labeled benzophenone/bezoxazole analogues prepared from the GMP synthesis method. Kit claims for preparing novel [11C]-labeled benzophenone/bezoxazole analogues and a method of use thereof are also provided.Type: ApplicationFiled: May 21, 2007Publication date: March 11, 2010Inventors: Farhad Karimi, Bengt Langstrom
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Patent number: 7652125Abstract: A resin composition having high heat resistance and low dielectric constant after heat treatment, a varnish thereof and a semiconductor device using the same are provided by a resin composition including a compound having a structure represented by the general formula (1): wherein, “Ar” is an aromatic group; “a” is 0 or 1; R11 is an organic group having one or more carbon atoms and at least one is a group having an alicyclic structure; when “q” is an integer of 2 or more, R11s may be the same or different from each other; at least one of R1 to R5 and at least one of R6 to R10 on respective benzene rings are Ar-binding sites or R11-binding sites and the others of R1 to R5 and R6 to R10 are each hydrogen, a group having an alicyclic structure, an organic group having 1 to 10 carbon atoms, a hydroxyl group or a carboxyl group; when “a” is 0, at least one of R1 to R5 and R6 to R10 is a group having an alicyclic structure; “q” is an integer of 1 or more; and “X” is any of —O—, —NHCO—, —COHN—, —COO— and —OCO—.Type: GrantFiled: September 29, 2005Date of Patent: January 26, 2010Assignee: Sumitomo Bakelite Company, Ltd.Inventors: Takashi Enoki, Atsushi Izumi, Yumiko Yamamoto, Takahiro Harada
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Patent number: 7642275Abstract: Compounds, pharmaceutical compositions, kits and methods are provided for use with histone deacetylases (HDACs) that comprise a compound of the formulae: wherein the variables are as defined herein.Type: GrantFiled: December 16, 2005Date of Patent: January 5, 2010Assignee: Takeda San Diego, Inc.Inventors: Jerome C. Bressi, Jason W. Brown, Robert J. Skene, Jeffrey A. Stafford, Phong H. Vu, Anthony R. Gangloff, Andrew J. Jennings, Stephen W. Kaldor
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Publication number: 20090325944Abstract: The invention relates to methods and products for modulating glycosylation of proteins. The invention is useful for treating glycosylation-associated disorders such as neurodegeneration, diabetes, including complications of diabetes such as insulin resistance, nephropathy, microvascular damage, and endothelial dysfunction. The invention also relates in part to assays that are useful for identifying and testing candidate compounds for modulating glycosylation of proteins.Type: ApplicationFiled: April 11, 2007Publication date: December 31, 2009Inventors: Suzanne Walker Kahne, Benjamin Gross
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Publication number: 20090325962Abstract: The compounds of the invention are inhibitors of alpha4 containing integrin-mediated binding to ligands such as VCAM-1 and MAdCAM.Type: ApplicationFiled: August 21, 2009Publication date: December 31, 2009Applicant: Genentech, Inc.Inventors: David Y. Jackson, Frederick C. Sailes, Daniel P. Sutherlin
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Publication number: 20090299063Abstract: Provided herein are compounds and methods of using compounds that selectively inhibit binding to one or more docking domain regions of an extracellular signal-recognition kinase to inhibit in a cell having an extracellular signal-regulated kinase activity. Such methods may be used to inhibit cell proliferation of a neoplastic cell, to treat a cancer and further may be used in conjunction with administration of an anticancer drug at a reduced dosage to treat a cancer with a concomitant reduction in toxicity to an individual receiving the treatment. Also provided is a method to design and screen for compounds to inhibit binding within the extracellular signal-regulated kinase docking domain region, using at least in part computer-aided drug design modeling.Type: ApplicationFiled: March 29, 2006Publication date: December 3, 2009Inventors: Paul Shapiro, Alexander D. MacKerell, JR.
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Patent number: 7625889Abstract: The present invention relates to a series of substituted bis aryl and heteroaryl compounds of formula (I): Wherein X, Y, Z, A, B, D, Ar, R1 and R2 are as defined herein. The compounds of this invention are selective 5HT2A antagonists, and are therefore, useful in treating a variety of diseases including but not limited to a wide variety of sleep disorders as disclosed and claimed herein.Type: GrantFiled: July 25, 2007Date of Patent: December 1, 2009Assignee: Aventis Pharmaceuticals Inc.Inventors: Paul Robert Eastwood, Hazel Hunt, David Mark Fink, Helen Katherine Smith, Richard Simon Todd
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Publication number: 20090203712Abstract: Disclosed is a novel compound having an NPY Y5 receptor antagonistic activity. A compound represented by the formula: its pharmaceutically acceptable salt or solvate thereof, wherein X is hydrogen or the like, Y is a group of the formula: Z is —NR7— or the like, R1 is hydrogen or the like, R2 and R3 are each independently hydrogen or the like, n is 0 or 1, p is 0 to 6.Type: ApplicationFiled: August 28, 2007Publication date: August 13, 2009Inventor: Toshisada Yano
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Publication number: 20090204336Abstract: The invention relates to compounds which bind to the PDZ domains of proteins with PDZ domains, the uses of such compounds and screening methods for identification of such compounds.Type: ApplicationFiled: April 28, 2006Publication date: August 13, 2009Applicant: Forschungsverbund Berlin e. V.Inventors: Mangesh Joshi, Hartmut Oschkinat, Markus Schade, Carolyn Vargas
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Publication number: 20090091234Abstract: A salt molten at room temperature that does not contain any organic solvent, excelling in stability; and a display device that is improved in the durability in high-temperature environment by virtue of the use thereof. There is provided a salt molten at room temperature characterized by being composed of a silver salt and any of compounds of the following general formula (I) or general formula (II).Type: ApplicationFiled: April 6, 2006Publication date: April 9, 2009Applicant: KONICA MINOLTA HOLDINGS, INC.Inventor: Noriyuki Kokeguchi
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Publication number: 20090075938Abstract: There are disclosed compound of Formula (1): A1, A2, A3 and A4 which may be the same or different, represent N or CR1, X is a divalent group selected from O, S(O)n, C?W, NR4, NC(?O)R5 and CR6R7, W is O, S, NR20, Y is N or CR8, one of R4, R5, R6, R8, R9 and NR20 represents -L-R3, in which L is a single bond or a linker group, additionally, R1, R3-R9, which may be the same or different, independently represent hydrogen or a substituent and R20 represents hydrogen, hydroxyl, alkyl optionally substituted by aryl, alkoxy optionally substituted by aryl, aryl, CN, optionally substituted alkoxy, optionally substituted aryloxy, optionally substitute alkanoyl, optionally substituted aroyl, NO2, NR30R31, in which R30 and R31, which may be the same or different, represent hydrogen, optionally substituted alkyl or optionally substituted aryl; additionally, one of R30 and R31 may represent optionally substituted alkanoyl or optionally substituted aroyl, n represents an integer from 0 to 2, in addition, when an adjacent paiType: ApplicationFiled: February 9, 2007Publication date: March 19, 2009Inventors: Graham Michael Wynne, Stephen Paul Wren, Peter David Johnson, Paul Damien Price, Olivier De Moor, Gary Nugent, Richard Storer, Richard Joseph Pye, Colin Richard Dorgan
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Publication number: 20090054448Abstract: The present invention relates to compounds of formula (I): or pharmaceutically acceptable salts or stereoisomers thereof. The compounds of the present invention are inhibitors of histone deacetylase (HDAC) and are useful for treating cellular proliferative diseases, including cancer. Further, the compounds of the present invention are useful for treating neurodegenerative diseases, schizophrenia and stroke among other diseases.Type: ApplicationFiled: September 5, 2006Publication date: February 26, 2009Inventor: Philip Jones
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Patent number: 7495020Abstract: A class of 2-aryloxy-2-arylalkanoic acids comprises compounds that are potent agonists of PPAR alpha and/or gamma, and are therefore useful in the treatment, control or prevention of non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, obesity, vascular restenosis, inflammation, and other PPAR alpha and/or gamma mediated diseases, disorders and conditions.Type: GrantFiled: January 18, 2006Date of Patent: February 24, 2009Assignee: Merck & Co., Inc.Inventors: Alan D. Adams, A. Brian Jones, Joel P. Berger, James F. Dropinski, Alexander Elbrecht, Kun Liu, Karen Lamb MacNaul, Guo-Qiang Shi, Derek J. Von Langen, Gaochao Zhou
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Publication number: 20090023916Abstract: Coupling reactions, suitable for use in organic or aqueous media, are performed by contacting a 1,2,4,5-tetrazine with a dienophile. The dienophile may be covalently bonded to a protein, and the coupling reaction may be performed in biological media such as those containing cells or cell lysates. The reactions may be performed in the presence of primary amines, thiols, acetylenes, azides, phosphines, and products of Staudinger and/or Sharpless-Huisgen reactions Novel 3-substituted cyclopropene compounds and trans-cyclooctenes are exemplary dienophiles for these reactions.Type: ApplicationFiled: July 17, 2008Publication date: January 22, 2009Applicant: University of DelawareInventors: Joseph Michael Fox, Melissa Blackman, Maksim Royzen, Ni Yan
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Publication number: 20080319032Abstract: This invention relates generally to tetrahydrobenzothiazole analogues and tetrahydrobenzooxyzole analogues, to pharmaceutical compositions which include these compounds and a pharmaceutically acceptable carrier, and to methods of treatment using these compounds. The invention also encompasses pharmaceutically acceptable esters, amides, and salts of such compounds. The invention further provides a method of reducing or delaying apoptosis in a population of cells, comprising contacting the population of cells with a tetrahydrobenzothiazole analogue or a tetrahydrobenzooxyzole analogue, thereby reducing or delaying apoptosis in the population of cells.Type: ApplicationFiled: November 13, 2007Publication date: December 25, 2008Inventors: Nigel H Greig, Mark Mattson, Xiaoxiang Zhu, Qian-Sheng Yu, Harold Wayne Holloway