Plural Double Bonds Between Ring Members Of The Oxazole Ring Patents (Class 548/247)
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Publication number: 20080125470Abstract: The present invention is directed to N-hydroxyamidino compounds which are modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.Type: ApplicationFiled: September 18, 2007Publication date: May 29, 2008Applicant: INCYTE CORPORATIONInventors: Andrew P. Combs, Brian M. Glass, Richard B. Sparks, Eddy Wai Tsun Yue
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Patent number: 7371777Abstract: The present invention provides a novel compound having an excellent PPAR agonist action. More specifically, it provides a compound represented by the following formula, a salt thereof, an ester thereof or a hydrate of them. Wherein a, b and c are the same as or different from one another and each represents 0 to 4; R1 to R6 are the same as or different from one another and each represents a hydrogen atom, a hydroxyl group, a cyano group, a halogen atom, etc.; A1 and A2 are the same as or different from each other and each represents a single bond, an oxygen atom, etc.; L, M and T each represent a single bond, an alkylene group having one to six carbon atoms, etc.; W represents a carboxyl group; the partial structure represented by the formula: represents a single bond or a double bond; X represents a single bond, an oxygen atom, —NRx1CQ1O—, etc.; Y represents Y1—Y2— (wherein Y1 represents a 5 to 14-membered aromatic ring having one to four substituents, etc.Type: GrantFiled: August 16, 2002Date of Patent: May 13, 2008Assignee: Eisai Co., Ltd.Inventors: Richard Clark, Fumiyoshi Matsuura, Eita Emori, Masanobu Shinoda, Shunji Kasai, Hideki Yoshitomi, Kazuto Yamazaki, Takashi Inoue, Sadakazu Miyashita, Taro Hihara
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Patent number: 7368578Abstract: The present invention provides a compound represented by the formula: wherein R1 is an optionally substituted 5-membered heterocyclic group; X, Y and V are the same or different and each is a bond, an oxygen atom, a sulfur atom and the like; Q is a divalent hydrocarbon group having 1 to 20 carbon atoms; ring A is an aromatic ring optionally further having 1 to 3 substituents; Z is —(CH2)n-Z1- or -Z1-(CH2)n— (n is an integer of 0 to 8, Z1 is a bond, an oxygen atom, a sulfur atom and the like); ring B is a nitrogen-containing heterocycle optionally further having 1 to 3 substituents; W is a bond or a divalent hydrocarbon group having 1 to 20 carbon atoms; R2 is a hydrogen atom, a cyano group, —PO(OR9)(OR10) (R9 and R10 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, and R9 and R10 are optionally bonded to form an optionally substituted ring) and the like, or a salt thereof, which has a superior adipose tissue weight decreasing action, a hypoglycemic actiType: GrantFiled: September 9, 2003Date of Patent: May 6, 2008Assignee: Takeda Pharmaceutical Company LimitedInventors: Yu Momose, Nobuyuki Takakura, Tsuyoshi Maekawa, Hiroyuki Odaka, Hiroyuki Kimura
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Patent number: 7368224Abstract: The invention provides a photopolymerizable composition having a high photosensitivity, which comprises a metal complex of a squarylium compound, a radical generator, and a compound having at least one ethylenically unsaturated double bond. The photopolymerizable composition of the present invention is advantageously used for a visible laser recording material such as a PS (Presensitized Plate) for laser direct plate-making, a dry film resist, a digital proof, a hologram, or the like, a panchromatic sensitive material (e.g., a sensitive material for a color hologram and a sensitive material used for full-color display and containing a photopolymerizable composition in a microcapsule), paints, adhesives, and so on.Type: GrantFiled: April 3, 2003Date of Patent: May 6, 2008Assignee: Kyowa Hakko Chemical Co., Ltd.Inventors: Tsuguo Yamaoka, Ikuo Shimizu, Hiroshi Toyoda, Motoharu Kinugasa, Masanori Ikuta, Kyoko Katagi
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Patent number: 7365088Abstract: The present invention relates to a compound of the formula I wherein J1, J2, R0, R1, R2, Q, V, G and M are as defined herein. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.Type: GrantFiled: May 19, 2004Date of Patent: April 29, 2008Assignee: Sanofi-Aventis Deutschland GmbHInventors: Marc Nazare, Volkmar Wehner, Volker Laux, Matthias Urmann, Armin Bauer, Hans Matter
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Patent number: 7358268Abstract: This invention is directed to the compound of formula (I) which is useful for inhibiting the activity of Factor Xa. The present invention is also directed to compositions containing said compounds, processes for their preparation, their use, such as in inhibiting the formation of thrombin or for therapeutically or prophylactically treating a patient suffering from, or subject to, or associated with a disease state associated with a cardiovascular disorder.Type: GrantFiled: December 4, 2003Date of Patent: April 15, 2008Assignee: Sanofi-Aventis Deutschland GmbHInventors: Marc Nazare, Armin Bauer, Volkmar Wehner, David W. Will, Hans Matter, Michael Wagner, Herman Schreuder
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Patent number: 7358377Abstract: Methods and intermediates for preparing enantiomerically enriched Schweinfurthin analogs which are useful for the treatment of cancer, as well as novel Schweinfurthin analogs having anti-cancer activity, compositions comprising such analogs and therapeutic methods comprising administering such analogs.Type: GrantFiled: March 29, 2005Date of Patent: April 15, 2008Assignees: University of Iowa Research Foundation, The United States of AmericaInventors: David F. Wiemer, Jeffrey D. Neighbors, John A. Beutler
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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
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Patent number: 7348440Abstract: The present invention relates to dihydropyrrole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: GrantFiled: June 12, 2003Date of Patent: March 25, 2008Assignee: Merck & Co., Inc.Inventors: Kenneth L. Arrington, Paul J. Coleman, Christopher D. Cox, Mark E. Fraley, Robert M. Garbaccio, George D. Hartman, William F. Hoffman, Edward S. Tasber
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Publication number: 20080070928Abstract: A glucokinase activator is provided; and a remedy and/or a preventive for diabetes, or a remedy and/or a preventive for diabetes such as retinopathy, nephropathy, neurosis, ischemic cardiopathy, arteriosclerosis, and further a remedy and/or a preventive for obesity are provided. A glucokinase activator characterized by containing a 2-heteroaryl-substituted benzimidazole derivative of a general formula (I-0) or its pharmaceutically-acceptable salt: [in the formula, X represents a carbon atom or a nitrogen atom; X1, X2, X3 and X4 each independently represent a carbon atom or a nitrogen atom; the ring A represents a 5- or 6-membered nitrogen-containing aromatic hetero ring of a formula (II): (in the formula, X represents a carbon atom or a nitrogen atom); R1 represents an aryl, etc.; R2 represents a hydroxy, etc.; R3 represents a —C1-6 alkyl, etc.; R4 represents a —C1-6 alkyl, etc.; X5 represents —O—, etc.Type: ApplicationFiled: December 28, 2004Publication date: March 20, 2008Inventors: Katsumasa Nonoshita, Makoto Ishikawa, Hiroshi Nakashima, Daisuke Tsukahara, Yoshio Ogino, Fumiko Sakai, Yoshikazu Nagae, Keisuke Arakawa, Teruyuki Nishimura, Jun-Ichi Eiki
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Publication number: 20080027096Abstract: The invention provides compounds of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt, for use in the treatment or prophylaxis of condition mediated by an androgen receptor.Type: ApplicationFiled: March 4, 2005Publication date: January 31, 2008Inventors: Neeraj Garg, Eva Kristina Kock, Henrik Per Hakan Jernstedt, Mikael Johan Gillner
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Publication number: 20080015232Abstract: Methods and intermediates for preparing enantiomerically enriched Schweinfurthin analogs which are useful for the treatment of cancer, as well as novel Schweinfurthin analogs having anti-cancer activity, compositions comprising such analogs and therapeutic methods comprising administering such analogs.Type: ApplicationFiled: March 29, 2005Publication date: January 17, 2008Inventors: David F. Wiemer, Jeffrey D. Neighbors, John A. Beutler
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Patent number: 7319109Abstract: The invention relates to a compound of formula (I): wherein all variables are as defined herein and to pharmaceutical compositions, methods of using, and processes for preparing the same.Type: GrantFiled: November 12, 2003Date of Patent: January 15, 2008Assignee: Smith Kline Beecham CorporationInventors: Sharon D Boggs, Jon L Collins, Stephen M Hyatt, Patrick R Maloney
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Patent number: 7319096Abstract: This invention relates to novel compounds which are thyroid receptor ligands, preferably antagonists, and to methods for using such compounds in the treatment of cardiac and metabolic disorders, such as cardiac arrhythmias, thyrotoxicosis, subclinical hyperthyrodism and liver diseases.Type: GrantFiled: April 15, 2002Date of Patent: January 15, 2008Assignee: Karo Bio ABInventors: Johan Malm, Peter Brandt, Karin Edvinsson, Thomas Ericsson, Sandra Gordon
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Patent number: 7319152Abstract: Compounds of formula I or II are provided, wherein R1-R8 are defined herein, and pharmaceutical compositions and kits containing these compounds.Type: GrantFiled: September 18, 2006Date of Patent: January 15, 2008Assignee: WyethInventors: Puwen Zhang, Jeffrey Curtis Kern, Eugene Anthony Terefenko, Eugene John Trybulski
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Patent number: 7304081Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.Type: GrantFiled: May 4, 2005Date of Patent: December 4, 2007Assignee: Incyte CorporationInventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Brian W. Metcalf, Chunhong He, Ding-Quan Qian, Colin Zhang
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Patent number: 7301034Abstract: A process for preparing 4-thioalkylbromobenzene derivatives of the formula I where: R1 is C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy, C1-C6-haloalkoxy, C3-C8-cycloalkyl, halogen, R2 is C1-C6-alkyl, C1-C6-alkoxy, C3-C8-cycloalkyl, C2-C6-alkenyl, cyano or a heterocyclic radical, R3 is C1-C6-alkyl, which comprises reacting a compound of the formula II, in which R1 and R2 are as defined above, with a dialkyl disulfide of the formula III R3—S—S—R3III in the presence of a nitrite and a catalyst in a suitable solvent is described.Type: GrantFiled: July 17, 2001Date of Patent: November 27, 2007Assignee: BASF AktiengesellschaftInventors: Rene Lochtman, Michael Keil, Joachim Gebhardt, Michael Rack, Wolfgang von Deyn
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Patent number: 7294650Abstract: Compounds of formula (I): and salts, solvates, and physiologically functional derivatives thereof, useful for the prophylaxis or treatment of a clinical condition for which a selective ?2-adrenoreceptor agonist is indicated, for example asthma or chronic obstructive pulmonary disease (COPD).Type: GrantFiled: December 15, 2004Date of Patent: November 13, 2007Assignee: Glaxo Group LimitedInventor: Keith Biggadike
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Patent number: 7291647Abstract: The present invention relates to compounds having the formula: salts thereof; compositions comprising one or more of the compounds and/or salts thereof; methods of using; and methods of making.Type: GrantFiled: August 17, 2005Date of Patent: November 6, 2007Assignee: Cytokine Pharmasciences, Inc.Inventor: Thais Sielecki-Dzurdz
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Patent number: 7279494Abstract: The present invention provides certain [3.1.0] bicyclic oxazolidinone derivatives of formula I or pharmaceutically acceptable salts or prodrugs thereof that are antibacterial agents, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.Type: GrantFiled: April 1, 2004Date of Patent: October 9, 2007Assignee: Pfizer Inc.Inventors: Adam Renslo, Mikhail Fedor Gordeev, Dinesh Vinoobhai Patel, Hongwu Gao, Vara Prasad Venkata Nagendra Josyula
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Publication number: 20070219261Abstract: Compounds of formula I processes for their preparation, their use as pharmaceuticals and to pharmaceutical compositions comprising them.Type: ApplicationFiled: January 19, 2007Publication date: September 20, 2007Inventors: Aurelia Conte, Holger Kuehne, Thomas Luebbers, Patrizio Mattei, Cyrille Maugeais, Werner Mueller, Philippe Pflieger
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Patent number: 7256206Abstract: The present invention relates to bicyclic derivatives, process for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG/S1P receptor mediated signal transduction.Type: GrantFiled: February 11, 2004Date of Patent: August 14, 2007Assignee: IRM LLCInventors: Shifeng Pan, Nathanael S. Gray, Yuan Mi, Wenqi Gao, Yi Fan, Sophie Lefebvre
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Patent number: 7250432Abstract: The present invention relates to a pharmaceutical composition for the prevention and the treatment of cancers containing diaryl-isoxazole derivatives as an effective ingredient. Diaryl-isoxazole derivatives of the present invention inhibit metastasis of breast cancer cell lines and angiogenesis, so that they can be produced as a metastasis inhibitor and further as a pharmaceutical composition for the prevention and the treatment of angiogenesis related diseases including cancers, rheumatoid arthritis, psoriasis, or angiogenesis diseases caused in eyeball, etc.Type: GrantFiled: October 20, 2004Date of Patent: July 31, 2007Assignee: Korea Research Institute of Bioscience and BiotechnologyInventors: Byoung-Mog Kwon, Kwang-Hee Son, Dong-Cho Han, Sang-Ku Lee, Ki-Deok Shin, Sun-Bok Jeon, Jung-Hoon Oh
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Patent number: 7244763Abstract: This invention relates to compounds that alter PPAR activity. The invention also relates to pharmaceutically acceptable salts of the compounds, pharmaceutically acceptable compositions comprising the compounds or their salts, and methods of using them as therapeutic agents for treating or preventing dyslipidemia, hypercholesterolemia, obesity, hyperglycemia, atherosclerosis, hypertriglyceridemia and hyperinsulinemia in a mammal. The present invention also relates to methods for making the disclosed compounds.Type: GrantFiled: February 6, 2004Date of Patent: July 17, 2007Assignee: Warner Lambert Company LLCInventors: Larry D. Bratton, Xue-Min Cheng, Noe Erasga, Gary F. Filzen, Andrew G. Geyer, Chitase Lee, Bharat K. Trivedi, Paul C. Unangst
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Publication number: 20070155799Abstract: Novel fenicol compounds having useful properties as antibiotic prodrugs, are provided, together with methods of making and using these new compounds.Type: ApplicationFiled: December 18, 2006Publication date: July 5, 2007Inventors: Tomasz W. Glinka, Dale Edward Shuster, Chander Shekher Celly, Robert D. Simmons, Jason Zhang
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Patent number: 7229987Abstract: The present invention relates to a melanin concentrating hormone antagonist compound of formula I: (I); or a pharmaceutically acceptable salt, solvate, enantiomer or prodrug thereof useful in the treatment, prevention or amelioration of symptoms associated with obesity and related diseases.Type: GrantFiled: May 6, 2003Date of Patent: June 12, 2007Assignee: Eli Lilly and CompanyInventors: Jochen Ammenn, James Ronald Gillig, Lawrence Joseph Heinz, Philip Arthur Hipskind, Michael Dean Kinnick, Yen-Shi Lai, John Michael Morin, Jr., James Arthur Nixon, Carsten Ott, Kenneth Allen Savin, Theo Schotten, Lawrence John Slieker, Nancy June Snyder, Michael Alan Robertson
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Patent number: 7223780Abstract: The present invention is directed to the compound of formula I which is useful for inhibiting the activity of blood clotting enzyme Factor Xa. The present invention is also directed to compositions containing said compounds, processes for their preparation, their use, such as for inhibiting the formation of thrombin or for therapeutically treating a patient suffering from, or subject to, a disease state associated with a cardiovascular disorder.Type: GrantFiled: May 19, 2004Date of Patent: May 29, 2007Assignee: Sanofi-Aventis Deutschland GmbHInventors: Marc Nazare, Volker Laux, Armin Bauer, Michael Wagner
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Patent number: 7205325Abstract: The present invention 1 includes compounds of formula (I), and their pharmaceutically acceptable salts. These compounds are useful in the control or prevention of cancer.Type: GrantFiled: March 25, 2004Date of Patent: April 17, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Birgit Bossenmaier, Walter-Gunar Friebe, Thomas Friess, Bernhard Goller, Matthias Rueth, Edgar Voss
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Patent number: 7199248Abstract: The present invention relates to a process for preparing a pharmaceutical starting compound compound by hydrolyzing a compound of the general formula (II): Wherein R1 is protected carboxy, R2 is lower alkoxy or higher alkoxy, A1 is an aromatic bivalent group, heterocyclic bivalent group or cyclo (lower) alkane bivalent group, and A2 is an aromatic bivalent group, heterocyclic bivalent group or cyclo (lower) alkane bivalent group, with aqueous potassium hydroxide and by treating with hydrochloric acid.Type: GrantFiled: August 4, 2003Date of Patent: April 3, 2007Assignee: Astellas Pharma Inc.Inventors: Hiroyuki Tsuboi, Atsushi Ohigashi, Yoshitaka Shimojo
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Patent number: 7186742Abstract: The present invention provides benzamide inhibitors of the P2X7 receptor of the formula: wherein R1–R3 are as defined herein. The compounds of the invention are useful in the treatment of IL-1 mediated disorders, including, without limitation, inflammatory diseases such as osteoarthritis and rheumatoid arthritis; allergies, asthma, COPD, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.Type: GrantFiled: May 12, 2004Date of Patent: March 6, 2007Assignee: Pfizer IncInventors: Mark A Dombroski, Allen J. Duplantier, Chakrapani Subramanyam
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Patent number: 7186738Abstract: Compounds of the formula (I), or a pharmaceutically-acceptable salts, or in-vivo-hydrolysable esters thereo Formula (I): wherein N-HeT is for example triazolyl; Q is for example phenyl or pyridyl, substituted with: T is for example selected from (TAa1 to TAa12) such as (TAa1) and (TAa5): R4h, R5h, R6h are for example selected from hydrogen, (1–4C)alkyl, (1–4C)alkoxy-carbonyl, (1–4C)alkanoyl and carbamoyl; processes for making them, compositions containing them and their use as antibacterial agents are described.Type: GrantFiled: March 16, 2004Date of Patent: March 6, 2007Assignee: AstraZeneca ABInventors: Michael Barry Gravestock, Neil James Hale, Sheila Irene Hauck
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Patent number: 7173129Abstract: The invention relates to compounds, pharmaceutical compositions and methods of using compounds of the general formula or its pharmaceutically acceptable salt or ester, wherein the substituents are defined in the application.Type: GrantFiled: June 7, 2004Date of Patent: February 6, 2007Assignee: Athero Genics, Inc.Inventors: Kimberly J. Worsencroft, Liming Ni, Zhihong Ye, Charles Q. Meng, M. David Weingarten, Jacob E. Simpson, James A. Sikorski
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Patent number: 7173052Abstract: The present invention relates to certain resorcinol derivatives and their use as skin lightening agents.Type: GrantFiled: December 2, 2004Date of Patent: February 6, 2007Assignees: Pfizer Inc., Pfizer Products Inc.Inventors: Stuart E. Bradley, Eric W. Collington, Matthew C. Fyfe, Martin J. Procter, Colin P. Sambrook Smith
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Patent number: 7169800Abstract: The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides processes for preparing the compounds of this invention, pharmaceutically acceptable compositions comprising the compounds of the invention, and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: September 24, 2004Date of Patent: January 30, 2007Assignee: Vertex Pharmaceuticals IncorporatedInventors: Alex Aronov, David J. Lauffer, Pan Li, Ronald C. Tomlinson
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Patent number: 7160903Abstract: Compounds of formula (I) are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved.Type: GrantFiled: June 13, 2002Date of Patent: January 9, 2007Assignee: Sanofi-Aventis Deutschland GmbHInventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase
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Patent number: 7157482Abstract: Compounds of the formula (I), or a pharmaceutically-acceptable salts, or in-vivo-hydrolysable esters thereof, wherein: N—HET is for example triazolyl substituted with R1; R1 is for example optionally substituted (1-4C)alkyl; Q is for example phenyl or pyridyl, substituted with T; T is for example selected from (TAa1 to TAa12) such as (TAa1 and TAa5); formula (II): R4h, R5h, R6h are for example selected from hydrogen, (1-4C)alkyl, (1-4C)alkoxycarbonyl, (1-4C)alkanoyl and carbamoyl; processes for making them, compositions containing them and their use as antibacterial agents are described.Type: GrantFiled: March 16, 2004Date of Patent: January 2, 2007Assignee: AstraZeneca ABInventors: Michael Barry Gravestock, Neil James Hale, Sheila Irene Hauck
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Patent number: 7157454Abstract: The invention relates to compounds of formula: These compounds show affinity for the bradykinin receptors with selectivity towards the B1 receptors; they may be used for the preparation of medicinal products intended for treating or preventing inflammation pathologies and persistent or chronic inflammatory diseases.Type: GrantFiled: March 27, 2002Date of Patent: January 2, 2007Assignee: Sanofi-AventisInventors: Bernard Ferrari, Jean Gougat, Yvette Muneaux, Pierre Perreaut, Lionel Sarran
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Patent number: 7153815Abstract: A insecticide characterized by containing as active ingredient a hydrazone derivative of formula (I) wherein A and Q are an aryl or a heterocyclic group, W is oxygen atom, an aminylene, an alkylene group, an oxyalkylene group or an alkyleneoxy, X1 and X2 are hydrogen atom, an alkyl, an alkenyl, an alkynyl, an aryl, a heterocyclic group, formyl, an acyl, an alkoxycarbonyl, an aryloxycarbonyl, a heterocyclic oxycarbonyl, an alkylsulfinyl, an arylsulfinyl, a heterocyclic sulfinyl, an alkylsulfonyl, an arylsulfonyl or a heterocyclic sulfonyl, Y is oxygen atom or sulfur atom, Z is hydrogen atom, a halogen atom, cyano, an alkyl, an alkenyl, an alkynyl, an amino, an alkoxy or an alkylthio, the substituents may be substituted; and novel hydrazon derivatives.Type: GrantFiled: January 10, 2003Date of Patent: December 26, 2006Assignee: Nihon Nohyaku Co., Ltd.Inventors: Shinji Kawata, Shuko Okui, Shigeru Suzuki, Toshiki Fukuchi, Akiyuki Suwa
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Patent number: 7135489Abstract: A stable crystalline form of 4-[5-methyl-3-phenylisoxazol-4-yl]benzenesulfonamide is described. This crystal structure, designated Form B, is more stable, has favorable handling properties and is characterized by its melting point, x-ray and other physical characterizations.Type: GrantFiled: July 26, 2002Date of Patent: November 14, 2006Assignee: G. D. Searle & Co.Inventors: John J Talley, John R Medich, Kathleen T McLaughlin, Henry T Gaud, Edward E Yonan
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Patent number: 7135472Abstract: The present invention provides novel 3-heterocyclic benzylamides and related derivatives having the general Formula I wherein R1, R2, R3, R4, R5, R6, A and Het are as defined in the specification, or a nontoxic pharmaceutically acceptable salt, solvate or hydrate thereof which are openers or activators of KCNQ potassium channels. The present invention also provides pharmaceutical compositions comprising said novel 3-heterocyclic benzylamides and to the method of treatment of disorders sensitive to KCNQ potassium channel opening activity such as migraine or a migraine attack, bipolar disorders, epilepsy, acute and chronic pain and anxiety.Type: GrantFiled: November 21, 2003Date of Patent: November 14, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Yong-Jin Wu, Alexandre L'Heureux, Huan He
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Patent number: 7125863Abstract: Compounds according to formula (1), wherein R1 is H or CN, X1 is S, O, SO2 or CH2, X2 is CO, CH2 or a covalent bond, Het is a nitrogen-containing heterocycle and n is 1–5 are new. The compounds of the invention are inhibitors of dipeptidyl peptidase IV.Type: GrantFiled: April 26, 2001Date of Patent: October 24, 2006Assignee: Ferring BVInventors: David Michael Evans, Gary Robert William Pitt
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Patent number: 7112679Abstract: The present invention relates to processes for the production of ?-aryl-?-ketonitriles, which serve as synthetic intermediates in the preparation of a series of biologically important molecules such as corticotropin releasing factor (CRF) receptor antagonists.Type: GrantFiled: February 25, 2004Date of Patent: September 26, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Jiacheng Zhou, Lynette May Oh, Philip Ma
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Patent number: 7105564Abstract: The present invention provides novel compounds having a dual antagonistic activity against thromboxane A2 receptor and prostaglandin D2 receptor and pharmaceutical compositions comprising them. A compound of the formula (I): wherein R1 is —CH2—CH?CH—CH2—CH2—CH2—COOR2 or —CH?CH—CH2—CH2—CH2—COOR2; R2 is hydrogen or alkyl; m is 0 or 1; p is 0 or 1; X1 and X3 each is independently optionally substituted aryl or optionally substituted heteroaryl; X2 is a bond, —CH2—, —S—, —SO2—, —CH2—O—, —O—CH2—, —CH2—S—, —S—CH2—, or the like; X4 is —CH2—, —CH2—CH2—, —C(?O)—, or the like, have a dual antagonistic activity against both a thromboxane A2 receptor and a prostaglandin D2 receptor.Type: GrantFiled: March 2, 2000Date of Patent: September 12, 2006Assignee: Shionogi & Co., Ltd.Inventors: Tsunetoshi Honma, Yoshiharu Hiramatsu, Akinori Arimura
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Patent number: 7105556Abstract: Compounds are provided which have the structure wherein Q is C or N, X1 is C or N, and R1, R2, R2a, R2b, R2c, R3, Y, A, m, n, X2, X3 and X4 are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.Type: GrantFiled: May 22, 2002Date of Patent: September 12, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Peter T. Cheng, Yoon Jeon, Wei Wang
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Patent number: 7087630Abstract: The invention describes novel cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one COX-2 selective inhibitor, optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor, and/or, optionally, at least one therapeutic agent. The novel cyclooxygenase 2 selective inhibitors of the invention can be optionally nitrosated and/or nitrosylated.Type: GrantFiled: June 25, 2003Date of Patent: August 8, 2006Assignee: Nitromed, Inc.Inventors: Upul K. Bandarage, Richard A. Earl, Maiko Ezawa, Xinqin Fang, David S. Garvey, Subhash P. Khanapure, Ramani R. Ranatunga, Stewart K. Richardson, Joseph D. Schroeder, Cheri A. Stevenson, Shiow-Jyi Wey
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Patent number: 7060710Abstract: The present invention provides compounds of formula I: in which: one of X and Y is a nitrogen atom substituted by a group R6? and the other is a carbon atom substituted by an isoxazole group substituted on its carbon atoms by groups R3 and R4; one of R6 and R6? is hydrogen; either all of W1, W2, W3 and W4 are carbon or one of W1, W2, W3 and W4 is nitrogen and the rest are carbon; and R1 and R2 are, independently, a small group, heteroaromatic ring or a 4–7 membered cyclic amine ring; processes for making them; pharmaceutical composition containing them; their use in therapy, particularly for enhancing cognition in conditions such as Alzheimer's Disease; and methods of treatment using them.Type: GrantFiled: November 22, 2002Date of Patent: June 13, 2006Assignee: Merck Sharp & Dohme Ltd.Inventors: Tamara Ladduwahetty, Angus Murray MacLeod, Kevin John Merchant, Francine Sternfeld
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Patent number: 7052742Abstract: Fluorinated five-membered ring compounds of the formula (I) R1—X—(A1—M1)a—(A2—M2)b—A3—Y—E ??(I) where E is a radical T—Z—R2 containing a five-membered ring and, for example, T is undirected and is 4-fluorothiophene-2,5-diyl, 3-fluorothiophene-2,5-diyl, 3-fluorothiophene-2,4-diyl, 5-fluorothiophene-2,4-diyl, furan-2,5-diyl, furan-2,4-diyl, isoxazole-3,5-diyl, thiazole-2,5-diyl, thiazole-2,4-diyl, cyclopentane-1,3-diyl or cyclopentene-1,3-diyl, R1 and R2 are hydrogen, X is a single bond, —O—, OC(?O)—, —C(?O)O— or —OC(?O)O—, Y is —OC(?O)—, —OCH2—, —CH2CH2—, Z is a single bond or —O—, A1, A2, A3 are each, independently of one another, phenylene-1,4-diyl, M1, M2 are undirected and are each, independently of one another, —OC(?O)—, —OCH2—, —CH2CH2—, —OC(?O)CH2CH2—, —OCH2CH2CH2—, —C?C—, —CH2CH2CH2CH2— or a single bond, a, b are each, independently of one another, 0 or 1, are used in FLC mixtures.Type: GrantFiled: August 31, 2000Date of Patent: May 30, 2006Assignee: Clariant International Ltd.Inventors: Barbara Hornung, Toshiaki Nonaka, Ayako Ogawa, Wolfgang Schmidt, Rainer Wingen
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Patent number: 7045532Abstract: ACE-2 inhibitors for the treatment of body weight and related disorders are disclosed. ACE-2 inhibitors include peptides and small molecules. Examples of small molecule ACE-2 inhibitors include compounds of formula (I): Z-???(I) Wherein Z is a zinc coordinating moiety and ? is an amino-acid mimicking moiety, and pharmaceutically acceptabale salts thereof. Methods of using the inhibitors and pharmaceutical compositions containing the inhibitors to treat a body weight disorder, to decrease appetite, to increase muscle mass, to decrease body fat, to treat diabetes and to treat a state associated with altered lipid metabolism, are also described.Type: GrantFiled: October 31, 2001Date of Patent: May 16, 2006Assignee: Millennium Pharmaceuticals, Inc.Inventors: Susan L. Acton, Timothy D. Ocain, Alexandra E. Gould, Natalie A. Dales, Bing Guan, James A. Brown, Michael Patane, Vivek J. Kadambi, Michael Solomon, Alain Stricker-Krongrad
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Patent number: 7034046Abstract: The present invention relates to compounds according to the general formula (I) which bind to the nuclear receptor, NR1H4, and act as agonists and antagonists of the NR1H4 receptor. The invention further relates to the treatment of diseases and/or conditions through binding of the nuclear receptor by the compounds.Type: GrantFiled: July 1, 2002Date of Patent: April 25, 2006Assignee: Phenex Pharmaceuticals AGInventors: Ulrike Bauer, Zach Cheruvallath, Ulrich Deuschle, Elena Dneprovskaia, Tim Gahman, Kristina Giegrich, Ronnie Hanecak, Normand Hébert, John Kiely, Ingo Kober, Manfred Kögl, Harald Kranz, Claus Kremoser, Matthew Lee, Kerstin Otte, Carlton Sage, Manish Sud
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Patent number: RE39575Abstract: The present invention is directed to chemical compositions of substituted thioacetamides, processes for the preparation thereof and uses of the compositions in the treatment of diseases.Type: GrantFiled: November 23, 2004Date of Patent: April 17, 2007Assignee: Cephalon, Inc.Inventors: Edward R. Bacon, Sankar Chatterjee, Derek Dunn, John P. Mallamo, Jeffry L. Vaught, Matthew S. Miller