Chalcogen Bonded Directly To Ring Carbon Of The Oxadiazole Ring Patents (Class 548/132)
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Patent number: 8173674Abstract: The invention relates to sulfonyl-phenyl-oxadiazolones and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta or PPARdelta and PPARgamma agonist activity. What are described are compounds of the formula I, in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.Type: GrantFiled: June 9, 2009Date of Patent: May 8, 2012Assignee: Sanofi-AventisInventors: Stefanie Keil, Matthias Urmann, Karl Schoenafinger, Wolfgang Wendler, Maike Glien, Hans-Ludwig Schaefer, Eugen Falk
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Publication number: 20120065196Abstract: The present invention provides compounds represented by the formula (Ie): and the formula (If): wherein each symbol is as defined in the specification. According to the present invention, these compounds have a DGAT inhibitory activity and are useful for the prophylaxis, treatment or improvement of diseases or pathologies caused by high expression or high activation of DGAT.Type: ApplicationFiled: July 20, 2007Publication date: March 15, 2012Inventors: Shuji Kitamura, Thomas Daniel Aicher, Steve Gonzales, Yvan Le Huerou, Scott Alan Pratt, Yoshihisa Nakada
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Publication number: 20120015991Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.Type: ApplicationFiled: September 27, 2011Publication date: January 19, 2012Applicant: AMIRA PHARMACEUTICALS, INC.Inventors: John Howard HUTCHINSON, Thomas Jon Seiders, Bowei Wang, Jeannie M. Arruda, Jeffrey Roger Roppe, Timothy Parr
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Patent number: 8088802Abstract: An N-phenylarylsulfonylamide compound of formula (I) (R1 is COOH etc.; R2 is hydrogen, methyl, etc.; R3 and R4 are a combination of methyl and methyl, etc.; R5 is isopropyl etc.; Ar is thiazolyl, pyridyl, 5-methyl-2-furyl each optionally substituted with methyl; n is zero or 1), a synthetic intermediate for the compound and a process for its preparation. The compound of formula (I) binds to a prostaglandin E2 receptor, especially an EP1 subtype receptor, and antagonizes it. It is less affected by protein binding, so it has a satisfactory in vivo activity. Therefore, it is considered to be useful as an analgesic, an antipyretic agent, an agent for the treatment of pollakiuria (frequent urination) and/or lower urinary tract disease syndrome or an antineoplastic agent.Type: GrantFiled: October 21, 2009Date of Patent: January 3, 2012Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Atsushi Naganawa, Tetsuji Saito, Kaoru Kobayashi, Takayuki Maruyama, Yoshihiko Nakai, Shinsuke Hashimoto
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Patent number: 8084618Abstract: Heterocyclic compounds derived from benzotriazine, triazines, triazoles and oxadiazoles are disclosed. The methods of synthesis and of use of such heterocyclic compounds are also provided.Type: GrantFiled: January 8, 2010Date of Patent: December 27, 2011Assignee: TargeGen, Inc.Inventors: Wolfgang Wrasidlo, Elena Dneprovskaia
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Patent number: 8063044Abstract: This invention relates to pyrazole derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivative thereofs, wherein R1 to R4 are defined in the description, and to processes for the preparation thereof, intermediates used in their preparation of, compositions containing them and the uses of such derivatives. The compounds of the present invention bind to the enzyme reverse transcriptase and are modulators, especially inhibitors thereof. As such the compounds of the present invention are useful in the treatment of a variety of disorders including those in which the inhibition of reverse transcriptase is implicated. Disorders of interest include those caused by Human Immunodeficiency Virus (HIV) and genetically related retroviruses, such as Acquired Immune Deficiency Syndrome (AIDS).Type: GrantFiled: August 25, 2008Date of Patent: November 22, 2011Assignee: Pfizer Inc.Inventors: Lyn Howard Jones, Charles Eric Mowbray, David Anthony Price, Matthew Duncan Selby, Paul Anthony Stupple
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Publication number: 20110230477Abstract: The present invention is directed to novel compounds of formula (I) and their use in treating metabolic diseases.Type: ApplicationFiled: December 7, 2009Publication date: September 22, 2011Applicant: Euroscreen S.A.Inventors: Hamid Hoveyda, Cyrille Evangelos Brantis, Guillaume Dutheuil, Ludivine Zoute, Didier Schils, Jerome Bernard
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Publication number: 20110201640Abstract: Provided is a tricyclic compound having a PPAR ? agonist activity, which is represented by the general formula (I) wherein Z represents a single bond or the like, Y represents a hydrogen atom, lower alkyl optionally having substituent(s) or the like, X represents a hydrogen atom or the like, A represents aryl or the like, B and C are the same or different and each represents an aromatic carbocycle or the like, R4-R9 are the same or different and each represents hydrogen or the like, V represents a single bond or the like, R10 and R11 are the same or different and each represents hydrogen or the like, or a pharmaceutically acceptable salt thereof or the like:Type: ApplicationFiled: August 6, 2009Publication date: August 18, 2011Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Arata Yanagisawa, Keiji Uehara, Masahiro Matsubara, Kimihisa Ueno, Michihiko Suzuki, Takeshi Kuboyama, Keisuke Yamamoto, Tomohiro Tamura
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Patent number: 7998968Abstract: A compound represented by the formula (I): wherein R1 is an oxo group, ?N—R or the like; a group represented by the formula: is a group represented by the formula: R2 is a group represented by the formula: R3 and R4 are each H, or C1-C6 alkyl, C3-C6 cycloalkyl, C1-C6 alkoxy, C1-C6 alkylamino, di(C1-C6)alkylamino or C1-C6 alkylthio, each of which is optionally substituted; and R5 is H, or C1-C6 alkyl, C2-C6 alkenyl, cyclic group, each of which is optionally substituted, —CO—R8 or —O—R8?, or a salt thereof. For example, the compound may be substituted pyrimidines and pharmaceutical compositions of the formula (I) where X=—CR3; X1=—CR2 or —NR2; and X2=—CR5 or —NR5. The compound of the present invention is useful as a drug for the prophylaxis or treatment of cardiovascular diseases, metabolic diseases and/or central nervous system diseases.Type: GrantFiled: November 25, 2009Date of Patent: August 16, 2011Assignee: Takeda Pharmaceutical Company LimitedInventors: Takanobu Kuroita, Hiroki Sakamoto, Hideyuki Igawa, Minoru Sasaki, Kouhei Asano, Tsuyoshi Maekawa, Koji Fuji
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Patent number: 7998988Abstract: The invention relates to biphenyl compounds of formula (I): wherein U, V and W together form a group of the formula *—CH?CH—CH<, *—CH2—CH2—CH< or *—CH2—CH2—N<, in which * means the point of linkage to the phenyl ring; A is O or CH2; and D, E, X, Y, Z, R1, R2, o, n, and p are as defined in the specification. The invention also relates to pharmaceutical compositions of the compound of the compounds. The compounds and pharmaceutical compositions of the invention can be used in the treatment or prevention of cardiovascular disorders.Type: GrantFiled: October 9, 2006Date of Patent: August 16, 2011Assignee: Bayer Schering Pharma AktiengellschaftInventors: Stephan Bartel, Michael Hahn, Wahed Ahmed Moradi, Klaus Münter, Thomas Rölle, Johannes-Peter Stasch, Karl-Heinz Schlemmer, Frank Wunder
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Patent number: 7985761Abstract: The present invention relates to novel diphenylurea derivatives useful as chloride channel blockers or BKCa channel modulators. In other aspects the invention relates to the use of these compounds in a method for therapy, and to pharmaceutical compositions comprising the compounds of the invention.Type: GrantFiled: March 9, 2007Date of Patent: July 26, 2011Assignee: Neurosearch A/SInventors: Bjarne H. Dahl, Palle Christophersen, Lars Siim Madsen
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Patent number: 7982047Abstract: A description follows of 1,3-diones having general formula (I): together with their use as herbicides for the control of weeds in agricultural crops.Type: GrantFiled: September 21, 2004Date of Patent: July 19, 2011Assignee: Isagro Ricerca S.r.l.Inventors: Giovanni Meazza, Piero Paravidino, Franco Bettarini, Daniele Forgia, Luca Fornara
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Patent number: 7977671Abstract: The present invention relates to a compound having an oxadiazole ring structure having a substituted pyridyl group connected thereto, represented by the following general formula (1). According to the present invention, it becomes possible to provide an organic compound having excellent characteristic of high stability in a thin film state, and the emission efficiency and durability of conventional organic EL devices can be remarkably improved.Type: GrantFiled: November 19, 2009Date of Patent: July 12, 2011Assignee: Hodogaya Chemical Co., Ltd.Inventors: Tetsuzo Miki, Makoto Nagaoka, Shuichi Hayashi, Yoshio Taniguchi, Musubu Ichikawa
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Patent number: 7968552Abstract: A compound which can be used as a pharmaceutical, particularly a insulin secretion promoter or a agent for preventing/treating disease in which GPR40 is concerned such as diabetes or the like, is provided. It was found that an oxadiazolidinedione compound which is characterized by the possession of a benzyl or the like substituent binding to the cyclic group via a linker at the 2-position of the oxadiazolidinedione ring, or a pharmaceutically acceptable salt thereof, has excellent GPR40 agonist action. In addition, since the oxadiazolidinedione compound of the present invention showed excellent insulin secretion promoting action and blood glucose level-lowering action, it is useful as an insulin secretion promoter or an agent for preventing/treating diabetes.Type: GrantFiled: April 23, 2007Date of Patent: June 28, 2011Assignee: Astellas Pharma Inc.Inventors: Kenji Negoro, Fumiyoshi Iwasaki, Kei Ohnuki, Toshio Kurosaki, Yasuhiro Yonetoku, Norio Asai, Shigeru Yoshida, Takatoshi Soga
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Publication number: 20110112051Abstract: The present invention relates generally to pyrrolidine and thiazolidine DPP-IV inhibitor compounds. The present invention also provides synthetic methods for preparation of such compounds, methods of inhibiting DPP-IV using such compounds and pharmaceutical formulations containing them for treatment of DPP-IV mediated diseases, in particular, Type-2 diabetes.Type: ApplicationFiled: January 13, 2011Publication date: May 12, 2011Applicant: Alantos Pharmaceuticals Holding, Inc.Inventors: Heiko KROTH, Tim Feuerstein, Frank Richter, Jürgen Boer, Michael Essers, Bert Nolte, Matthias Schneider, Matthias Hochguertel, Fritz-Frieder Frickel, Arthur Taveras, Christoph Steeneck
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Patent number: 7910606Abstract: The present invention is directed to a compound of formula I, in which R0; R1; R2; R3; R4; Q; V, G and M have the meanings indicated below. The compound of formula I is a pharmacologically active compound. It exhibits a strong anti-thrombotic effect and is suitable, for example, for the therapy and prophylaxis of a cardio-vascular disorder like a thromboembolic disease or restenosis. It is a reversible inhibitor 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 is directed to a process for the preparation of the compound of formula I, and pharmaceutical preparation comprising it.Type: GrantFiled: September 18, 2009Date of Patent: March 22, 2011Assignee: Sanofi-Aventis Deutschland GmbHInventors: Marc Nazare, Volkmar Wehner, David William Will, Hans Matter
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Publication number: 20110028493Abstract: The present invention aims to provide a compound having superior pharmacological action, physicochemical properties and the like and useful as an sGC activation drug, or an agent for the prophylaxis and/or treatment of diseases such as hypertension, ischemic cardiac disease, cardiac failure, kidney disease, arteriosclerotic disease, atrial fibrillation, pulmonary hypertension, diabetes, diabetic complications, metabolic syndrome, peripheral arterial obstruction, erectile dysfunction and the like. An sGC activation drug containing a compound represented by the formula (II): wherein each symbol is as defined in the specification, or a salt thereof, as an active ingredient.Type: ApplicationFiled: April 3, 2009Publication date: February 3, 2011Inventors: Nobuyuki Matsunaga, Yoshihisa Nakada, Yusuke Ohba, Hideyuki Nakagawa
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Publication number: 20110028463Abstract: [Problems] To provide a compound that is useful as an agent for treating chronic renal insufficiency or an agent for treating diabetic nephropathy. [Means for Solving Problems] The present inventors have conducted extensive studies on a compound having an EP4 receptor antagonistic action, and as a result, they have found that various amide derivatives having a carboxylic group or an equivalent thereof exhibit an excellent EP4 receptor antagonistic action, thereby completing the present invention. Since the compound of the present invention has an excellent EP4 receptor antagonistic action, it is useful as an agent for preventing and/or treating chronic renal insufficiency or diabetic nephropathy.Type: ApplicationFiled: July 2, 2008Publication date: February 3, 2011Applicant: Astellas Pharma Inc.Inventors: Eisuke Nozawa, Ryotaro Ibuka, Kazuhiro Ikegai, Keisuke Matsuura, Tatsuya Zenkoh, Ryushi Seo
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Publication number: 20110021527Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: July 14, 2010Publication date: January 27, 2011Inventors: Paul R. FATHEREE, Ryan HUDSON, Robert Murray MCKINNELL
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Patent number: 7875637Abstract: The present invention relates to a compound represented by the formula (I) wherein R1 is a group represented by the formula wherein R2, R3, R4, R5, R6, R7 and R8 are each independently a hydrogen atom or a C1-6 alkyl, or a salt thereof. The compound of the present invention is useful as an agent for the prophylaxis or treatment of circulatory diseases such as hypertension and the like and metabolic diseases such as diabetes and the like.Type: GrantFiled: June 30, 2009Date of Patent: January 25, 2011Assignee: Takeda Pharmaceutical Company LimitedInventors: Takanobu Kuroita, Hiroki Sakamoto, Mami Ojima
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Publication number: 20110015234Abstract: The invention is concerned with novel indazole derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used in the prevention or treatment of diseases which are modulated by L-CPT1 inhibitors.Type: ApplicationFiled: September 8, 2010Publication date: January 20, 2011Inventors: Jean Ackermann, Konrad Bleicher, Simona M. Ceccarelli, Odile Chomienne, Patrizio Mattei
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Publication number: 20110009384Abstract: The present invention provides an agent for the prophylaxis or treatment of diabetes, which has a superior hypoglycemic action, and is associated with a fewer side effects such as body weight gain and the like. The resent invention relates an agent for the prophylaxis or treatment of diabetes, which comprises a compound represented by wherein each symbol is as defined in the description, or a salt thereof or a prodrug thereof.Type: ApplicationFiled: February 5, 2008Publication date: January 13, 2011Inventors: Taisuke Tawaraishi, Hiroshi Imoto, Nobuo Cho
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Publication number: 20100292283Abstract: This invention relates to novel phenyl-acetamide and phenyl-propionamide derivatives that are found to be potent modulators of potassium channels and, as such, are valuable candidates for the treatment of diseases or disorders as diverse as those which are responsive to the modulation of potassium channels.Type: ApplicationFiled: November 26, 2008Publication date: November 18, 2010Inventors: Antonio Nardi, Jeppe Kejser Christensen
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Publication number: 20100292273Abstract: Compounds of formula (I) are modulators of cannabinoid receptor CB1, useful inter alia for treatment of obesity: Formula (I). Wherein: X is a bond, or a divalent radical selected from —C(R10)(R11)—*, —C(R10)(R11)—O—*, —C(R10)(R11)CH2—*, —C(R10)(R11)CH2—O—*, —CH2C(R10)(R11)—*, —CH2C(R10)(R11)—O—*.Type: ApplicationFiled: December 8, 2008Publication date: November 18, 2010Applicant: 7TM PHARMA A/SInventors: Jean Marie Receveur, Emelie Bjurling, Anthony Murray, Thomas Hoegberg, Peter Aadal Nielsen, Jean-Michel Linget, Pia Karina Noerregaard, Dorthe Almholt
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Publication number: 20100286149Abstract: This invention relates to novel benzamide derivatives that are found to be potent modulators of potassium channels and, as such, are valuable candidates for the treatment of diseases or disorders as diverse as those which are responsive to the modulation of potassium channels.Type: ApplicationFiled: November 25, 2008Publication date: November 11, 2010Inventors: Antonio Nardi, Jeppe Kejser Christensen
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Publication number: 20100267688Abstract: 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, Chaozhong Cai, James C. Lanter, Thomas P. Markotan, Zhihua Sui
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Publication number: 20100267775Abstract: A pharmaceutical agent having GPR40 receptor agonistic action, particularly a compound which is useful as an insulin secretagogue or an agent for preventing and/or treating diabetes mellitus. The present inventors have examined a compound having GPR40 receptor agonistic action, confirmed that an oxadiazolidinedione compound which has a substituent such as a benzyl group, etc. linked with a substituent such as a phenyl group, etc. through a linker at the 2-position of an oxadiazolidinedione ring, or a pharmaceutically acceptable salt thereof has an excellent GPR40 agonistic activity, and thus completed the invention. The oxadiazolidinedione compound has excellent insulin secretagogue action and anti-hyperglycemic action, and therefore can be used as an insulin secretagogue or an agent for preventing and/or treating diabetes mellitus.Type: ApplicationFiled: October 22, 2008Publication date: October 21, 2010Inventors: Kenji Negoro, Fumiyoshi Iwasaki, Kei Ohnuki, Toshio Kurosaki, Kazuyuki Tsuchiya, Kazuyuki Kuramoto, Shigeru Yoshida, Takatoshi Soga
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Patent number: 7812341Abstract: The present invention relates to a compound having an oxadiazole ring structure having a substituted pyridyl group connected thereto, represented by the following general formula (1). According to the present invention, it becomes possible to provide an organic compound having excellent characteristic of high stability in a thin film state, and the emission efficiency and durability of conventional organic EL devices can be remarkably improved.Type: GrantFiled: March 25, 2005Date of Patent: October 12, 2010Assignee: Hodogaya Chemical Co., Ltd.Inventors: Tetsuzo Miki, Makoto Nagaoka, Shuichi Hayashi, Yoshio Taniguchi, Musubu Ichikawa
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Patent number: 7803940Abstract: A compound represented by the formula (I): wherein R1 is an oxo group, ?N—R or the like; a group represented by the formula: is a group represented by the formula: R2 is a group represented by the formula: R3 and R4 are each H, or C1-C6 alkyl, C3-C6 cycloalkyl, C1-C6 alkoxy, C1-C6 alkylamino, di(C1-C6)alkylamino or C1-C6 alkylthio, each of which is optionally substituted; and R5 is H, or C1-C6 alkyl, C2-C6 alkenyl, cyclic group, each of which is optionally substituted, —CO—R8 or —O—R8?, or a salt thereof. The compound of the present invention is useful as a drug for the prophylaxis or treatment of cardiovascular diseases, metabolic diseases and/or central nervous system diseases.Type: GrantFiled: May 2, 2008Date of Patent: September 28, 2010Assignee: Takeda Pharmaceutical Company LimitedInventors: Takanobu Kuroita, Hiroki Sakamoto, Hideyuki Igawa, Minoru Sasaki, Kouhei Asano, Tsuyoshi Maekawa, Koji Fuji
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Publication number: 20100210849Abstract: Compositions and processes for controlling nematodes are described herein, e.g., nematodes that infest plants or animals. The compounds include oxazoles, oxadiazoles and thiadiazoles.Type: ApplicationFiled: February 10, 2010Publication date: August 19, 2010Applicant: DIVERGENCE, INC.Inventors: Urszula Slomczynska, Matt W. Dimmic, William P. Haakenson, JR., Al Wideman
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Patent number: 7759493Abstract: Bicyclic compounds containing a phenyl or pyridyl ring fused to a cycloalkyl or heterocyclic ring, to which is attached a 5-membered heterocyclic ring, including pharmaceutically acceptable salts and prodrugs thereof, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.Type: GrantFiled: January 30, 2006Date of Patent: July 20, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Min Ge, Lihu Yang, Changyou Zhou, Songnian Lin, Haifeng Tang, Eric Dean Cline, Sunita Malkani
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Publication number: 20100121071Abstract: The present invention provides a solid pharmaceutical composition containing compound (I) having an angiotensin II receptor antagonistic action and defined in the specification and a pH control agent, which composition is superior in the stability and dissolution property of compound (I).Type: ApplicationFiled: March 26, 2008Publication date: May 13, 2010Inventors: Shuji Yoneyama, Yutaka Tanoue
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Patent number: 7709481Abstract: The inventive compounds of the present invention are comprised of phenyl and pyridinyl-1,2,4-oxadiazolone derivatives and their physiologically acceptable salts and functional derivatives that are shown to provide peroxisome proliferator activator receptor (PPARdelta) agonist activity. The compounds of the present invention are comprised of the formula: wherein the substituents R1-R5 and R7-R10 are defined herein. The compounds are therapeutically effective in the regulation and modulation of lipid and carbohydrate metabolism in mammals and are thus suitable for the treatment of diseases such as type-2 diabetes, atherosclerosis, cardiovascular disorders and the like.Type: GrantFiled: March 26, 2008Date of Patent: May 4, 2010Assignee: Sanofi-AventisInventors: Stefanie Keil, Matthias Urmann, Patrick Bernardelli, Maike Glien, Wolfgang Wendler, Karen Chandross, Lan Lee
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Patent number: 7709509Abstract: The invention relates to oxadiazolones and to their physiologically acceptable salts and physiologically functional derivatives showing peroxisome proliferator activator receptor (PPAR) delta agonist activity comprising compounds of formula I, in which the R1-R7 substituents as well as the U, V, W, X Y and z radicals are as defined herein, and their physiologically acceptable salts and processes for their preparation. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved; neurodegenerative diseases and/or demyelinating disorders of the central and peripheral nervous systems and/or neurological diseases involving neuro-inflammatory processes and/or other peripheral neuropathies.Type: GrantFiled: June 5, 2008Date of Patent: May 4, 2010Assignee: Sanofi-Aventis Deutschland GmbHInventors: Stefanie Keil, Wolfgang Wendler, Maike Glien, Jochen Goerlitzer, Karen Chandross, Daniel G. McGarry, Jean Merrill, Patrick Bernardelli, Baptiste Ronan, Corinne Terrier
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Publication number: 20100105689Abstract: This invention relates to novel 1,4- and 1,5-diarylsubstituted 1,2,3-triazole derivatives that are found to be potent modulators of potassium channels and, as such, they are valuable candidates for the treatment of diseases or disorders as diverse as those which are responsive to modulation of potassium channels.Type: ApplicationFiled: January 17, 2008Publication date: April 29, 2010Inventors: Antonio Nardi, Morten Grunnet, Joachim Demnitz, Palle Christophersen, David Spencer Jones, Elsebet Østergaard Nielsen, Dorte Strøbæk, Lars Siim Madsen
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Publication number: 20100056526Abstract: A compound represented by the formula (I): wherein R1 is an oxo group, ?N—R or the like; a group represented by the formula: is a group represented by the formula: R2 is a group represented by the formula: or a salt thereof. The compound of the present invention is useful as a drug for the prophylaxis or treatment of circulatory diseases, metabolic diseases and/or central nervous system diseases.Type: ApplicationFiled: November 21, 2007Publication date: March 4, 2010Inventors: Takanobu Kuroita, Hiroki Sakamoto, Hideyuki Igawa, Minoru Sasaki, Kouhei Asano, Tsuyoshi Maekawa
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Publication number: 20100029685Abstract: This invention relates to oxadiazolyl and thiadiazolyl derivatives, which are found to be modulators of the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: ApplicationFiled: October 24, 2007Publication date: February 4, 2010Applicant: NeuroSearch A/SInventors: Bjarne H. Dahl, Dan Peters, Gunnar M. Olsen, Daniel B. Timmermann, Susanne Jorgensen
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Publication number: 20100016383Abstract: Compounds of formula wherein A0 is a bond or a C1-C6alkylene bridge; A1, A2 and A3 are a C1-C6alkylene bridge; D is CH or N; W is, for example, O, S, SO, SO2, —C(?O)—O— or —O—C(?O)—; T is a bond or, for example, O, NH, S, SO or SR2; Q is, for example, O, S, SO or SO2; Y is, for example, O, S, SO or SO2; X1 and X2 are each independently of the other fluorine, chlorine or bromine; R1, R2 and R3 are, for example, H, halogen, OH, SH, CN or nitro; R4 is, for example, H, halogen, OH, SH, CN, nitro or C1-C6alkyl; R5 is, for example, H, CN, OH, C1-C6alkyl or C3-C8cycloalkyl; k is 1, 2 or 3 when D is nitrogen; or is 1, 2, 3 or 4 when D is CH; m is 1 or 2; E is heteroaryl which is unsubstituted or substituted—depending upon the substitutions possible on the ring—by from one to four identical or different substituents selected from R10; and R10 is, for example, halogen, CN, NO2, OH, SH or C1-C6alkyl; and, where applicable, their possible E/Z isomers, E/Z isomeric mixtures and/or tautomers, in each case in free formType: ApplicationFiled: September 23, 2009Publication date: January 21, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Werner Zambach, Arthur Steiger, Peter Renold, Stephan Trah, Roger Graham Hall
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Publication number: 20100010045Abstract: The present invention is directed to a compound of formula I, in which R0; R1; R2; R3; R4; Q; V, G and M have the meanings indicated below. The compound of formula I is a pharmacologically active compound. It exhibits a strong anti-thrombotic effect and is suitable, for example, for the therapy and prophylaxis of a cardio-vascular disorder like a thromboembolic disease or restenosis. It is a reversible inhibitor 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 is directed to a process for the preparation of the compound of formula I, and pharmaceutical preparation comprising it.Type: ApplicationFiled: September 18, 2009Publication date: January 14, 2010Applicant: sanofi-aventis Deutschland GmbHInventors: Marc NAZARE, Volkmar WEHNER, David W. WILL, Hans MATTER
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Patent number: 7638514Abstract: There are described compounds of formula (I) wherein X1 and X2 are each independently of the other fluorine, chlorine or bromine; A1 and A2 are, for example, a bond or a C1-C6alkylene bridge; A3 is a C1-C6alkylene bridge; R1 and R2 are, for example, halogen, OH, SH, CN, nitro, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkyl-carbonyl, C2-C6alkenyl, C2-C6haloalkenyl or C3-C6alkynyl; R,3 is, for example, H, halogen, OH, SH, CN, nitro, C1-C6alkyl or C1-C6haloalkyl; R4 and R5 are, for example, H, halogen, cyano, nitro, C1-C6alkyl or C1-C3haloalkyl; m is 1 or 2; Y is, for example, O, S, SO or SO2; Q is, for example, O, S, SO or SO2; W is, for example, a bond, O, S, SO, S02, —C(?O)—O— or —O—C(?O)—; T is, for example, a bond, O, S, SO, SO2, —C(?O)—O— or —O—C(?O)—; and E is aryl unsubstituted or substituted from one to five times or heterocyclyl unsubstituted or, depending upon the possibilities of substitution on the ring, substituted from one to four times; and, where applicable, their possible E/Z isomers, E/Z isomeric mixtType: GrantFiled: August 25, 2004Date of Patent: December 29, 2009Assignee: Syngenta Crop Protection, Inc.Inventors: Werner Zambach, Stephan Trah, Roger Graham Hall, William Lutz
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Publication number: 20090318481Abstract: This application relates to a substituted hydroxyphenyl ketone compound of formula I, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof and its use in treating migraine. This application also relates to processes for preparing a compound of formula I, and intermediate compounds useful therein.Type: ApplicationFiled: August 28, 2009Publication date: December 24, 2009Inventors: Thomas Daniel AICHER, Guillermo S. CORTEZ, Todd Michael GROENDYKE, Albert KHILEVICH, James Allen KNOBELSDORF, Fredrik Pehr MARMSATER, Jeffrey Michael SCHKERYANTZ, Tony Pisal TANG
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Patent number: 7629369Abstract: An N-phenylarylsulfonylamide compound of formula (I) (R1 is COOH etc.; R2 is hydrogen, methyl, etc.; R3 and R4 are a combination of methyl and methyl, etc.; R5 is isopropyl etc.; Ar is thiazolyl, pyridyl, 5-methyl-2-furyl each optionally substituted with methyl; n is zero or 1), a synthetic intermediate for the compound and a process for its preparation. The compound of formula (I) binds to a prostaglandin E2 receptor, especially an EP1 subtype receptor, and antagonizes it. It is less affected by protein binding, so it has a satisfactory in vivo activity. Therefore, it is considered to be useful as an analgesic, an antipyretic agent, an agent for the treatment of pollakiuria (frequent urination) and/or lower urinary tract disease syndrome or an antineoplastic agent.Type: GrantFiled: September 30, 2005Date of Patent: December 8, 2009Assignee: Ono Pharmaceuticals Co., Ltd.Inventors: Atsushi Naganawa, Tetsuji Saito, Kaoru Kobayashi, Takayuki Maruyama, Yoshihiko Nakai, Shinsuke Hashimoto
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Publication number: 20090298871Abstract: The invention relates to sulfonyl-phenyl-oxadiazolones and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta or PPARdelta and PPARgamma agonist activity. What are described are compounds of the formula I, in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.Type: ApplicationFiled: June 9, 2009Publication date: December 3, 2009Applicant: SANOFI-AVENTISInventors: Stefanie KEIL, Matthias URMANN, Karl SCHOENAFINGER, Wolfgang WENDLER, Maike GLIEN, Hans-Ludwig SCHAEFER, Eugen FALK
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Publication number: 20090291967Abstract: Compounds, particularly compounds having activity as modulators of cadherin-mediated cell adhesion having the following structure: or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein R1, R2, R3, R4, R5, R6, A, X, Y, Z, m and n are as defined herein. Methods associated with preparation and use of the same, as well as pharmaceutical compositions containing the same, are also disclosed.Type: ApplicationFiled: March 5, 2009Publication date: November 26, 2009Applicant: ADHEREX TECHNOLOGIES, INC.Inventors: Mukur Gupta, Brian Huber, Orest W. Blaschuk
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Publication number: 20090281084Abstract: The invention relates to phenyl-1,2,4-oxadiazolone derivatives with phenyl group and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta agonist activity. What are described are compounds of the formula I, in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.Type: ApplicationFiled: May 29, 2009Publication date: November 12, 2009Applicant: SANOFI-AVENTISInventors: Patrick Bernardelli, Stefanie Keil, Matthias Urmann, Hans Matter, Wolfgang Wendler, Maike Glien, Karen Chandross, Lan Lee, Corinne Terrier, Herve Minoux
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Patent number: 7598423Abstract: This application relates to a substituted hydroxyphenyl ketone compound of formula I, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof and its use in treating migraine. This application also relates to processes for preparing a compound of formula I, and intermediate compounds useful therein.Type: GrantFiled: November 15, 2005Date of Patent: October 6, 2009Assignee: Eli Lilly and CompanyInventors: Thomas Daniel Aicher, Guillermo S. Cortez, Todd Michael Groendyke, Albert Khilevich, James Allen Knobelsdorf, Fredrik Pehr Marmsater, Jeffrey Michael Schkeryantz, Tony Pisal Tang, Nicholas Andrew Magnus
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Publication number: 20090239915Abstract: The present invention relates to derivatives of 2-phenyl-benzimidazoles of the formula I, in which X, R, R1 to R3 and n have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired.Type: ApplicationFiled: March 27, 2009Publication date: September 24, 2009Applicant: SANOFI-AVENTISInventors: Gerhard ZOLLER, Hartmut STROBEL, David William WILL, Paulus WOHLFART
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Publication number: 20090227640Abstract: The present application relates to novel heterocyclic compounds, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.Type: ApplicationFiled: October 9, 2006Publication date: September 10, 2009Applicant: BAYER HEALTHCARE AGInventors: Stephan Bartel, Michael Hahn, Wahed Ahmed Moradi, Klaus Münter, Thomas Rölle, Johannes-Peter Stasch, Karl-Heinz Schlemmer, Frank Wunder
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Patent number: 7572920Abstract: The present invention relates to a compound represented by the formula (I) wherein R1 is a group represented by the formula wherein R2, R3, R4, R5, R6, R7 and R8 are each independently a hydrogen atom or a C1-6 alkyl, or a salt thereof. The compound of the present invention is useful as an agent for the prophylaxis or treatment of circulatory diseases such as hypertension and the like and metabolic diseases such as diabetes and the like.Type: GrantFiled: August 23, 2006Date of Patent: August 11, 2009Assignee: Takeda Pharmaceutical Company LimitedInventors: Takanobu Kuroita, Hiroki Sakamoto, Mami Ojima
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Publication number: 20090186909Abstract: [Problem] A compound which can be used as a pharmaceutical, particularly a insulin secretion promoter or a agent for preventing/treating disease in which GPR40 is concerned such as diabetes or the like, is provided. [Means for resolution] It was found that an oxadiazolidinedione compound which is characterized by the possession of a benzyl or the like substituent binding to the cyclic group via a linker at the 2-position of the oxadiazolidinedione ring, or a pharmaceutically acceptable salt thereof, has excellent GPR40 agonist action. In addition, since the oxadiazolidinedione compound of the present invention showed excellent insulin secretion promoting action and blood glucose level-lowering action, it is useful as an insulin secretion promoter or an agent for preventing/treating diabetes.Type: ApplicationFiled: April 23, 2007Publication date: July 23, 2009Inventors: Kenji Negoro, Fumiyoshi Iwasaki, Kei Ohnuki, Toshio Kurosaki, Yasuhiro Yonetoku, Norio Asai, Shigeru Yoshida, Takatoshi Soga