Nitrogen Attached Indirectly To The Tetrazole Ring By Nonionic Bonding Patents (Class 548/254)
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Publication number: 20110077279Abstract: A compound having the structure wherein R is an angiotensin II receptor antagonist selected from the group consisting of (IIa)-(IIh); A is wherein R1 and R2 are independently selected from the group consisting of hydrogen and C1-4 alkyl. Y is X0—Z wherein X0 is selected from the group consisting of: —O—, —O—CO—, —OCOO—, —OCONH— and —OSO2—; Z is a nitric oxide releasing moiety, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: May 18, 2009Publication date: March 31, 2011Inventors: Nicoletta Almirante, Massimiliano Ferrario, Silvia Stefanini, Stefano Biondi, Ennio Ongini
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Publication number: 20110003690Abstract: The invention relates to novel arylpyrroline compounds of formula (I) which having excellent insecticidal activity and which can thus be used as an insecticide is provided.Type: ApplicationFiled: January 29, 2009Publication date: January 6, 2011Applicant: BAY CROPSCIENCE AGInventors: Ulrich Goergens, Yasushi Yoneta, Tetsuya Murata, Jun Mihara, Kei Domon, Eiichi Shimojo, Katsuhiko Shibuya, Teruyuki Ichihara
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Patent number: 7855308Abstract: The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.Type: GrantFiled: January 19, 2009Date of Patent: December 21, 2010Assignee: Abbott LaboratoriesInventors: Michael E. Brune, Peer B. Jacobson, James T. Link, Jyoti R. Patel, Jeffrey J. Rohde, Qi Shuai, Martin Winn, Vince S. Yeh, Hong Yong
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Publication number: 20100311789Abstract: Racemic or enantiomerically enriched 3-substituted propanamine compounds represented by the following structural formula (I): or a pharmaceutically acceptable salt thereof are disclosed. Pharmaceutical compositions containing the subject compounds are also disclosed. The subject compounds are useful for the treatment of diseases of the central nervous system, such as depression, anxiety and pain disorders.Type: ApplicationFiled: June 3, 2009Publication date: December 9, 2010Inventors: Chun-Eung Park, Kyung-Hyun Min, Yong-Je Shin, Yu-Jin Shin, Hae-Jeong Yoon, Won Kim, Eun-Ju Ryu, Coo-Min Chung, Hui-Ho Kim
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Publication number: 20100305166Abstract: A compound of formula (I) or salts thereof, wherein R1, R2, R3, R4, n and X are as defined in the specification; a process for preparing such compounds, a pharmaceutical composition comprising such compounds; and the use of such compounds in medicine.Type: ApplicationFiled: October 30, 2008Publication date: December 2, 2010Inventors: Alessandra Gaiba, Susan Roomans, Martin Edward Swarbrick
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Patent number: 7834023Abstract: Compounds of formula I are provided: wherein Ar1 and Ar2 are substituted aromatic rings and L1 and L2 are independent divalent linking groups. The compounds are useful as platelet ADP receptor inhibitors, for treating thrombosis and for reducing the likelihood and/or severity of a secondary ischemic event in a patient.Type: GrantFiled: September 17, 2007Date of Patent: November 16, 2010Assignee: Portola Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Carroll Anna Crew, legal representative, Shawn M. Bauer, Anjali Pandey
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Publication number: 20100267698Abstract: This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula I The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABAA receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Novel processes for preparing compounds of Formula I are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABAA receptors in tissue sections.Type: ApplicationFiled: January 5, 2010Publication date: October 21, 2010Inventors: Guiying Li, Pamela Albaugh, Kevin S. Currie, Guolin Cai, Linda M. Gustavson, Kyungae Lee, Alan Hutchison, George D. Maynard, Jun Yuan, Ling Hong Xie, Manuka Ghosh, Nian Liu, George P. Luke, Scott Mitchell, Martin Patrick Allen, Spiros Liras
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Patent number: 7799820Abstract: Disclosed is a compound represented by the formula (I) below, which has a glucokinase-activating effect and is thus useful for treatment of diabetes or obesity, or a pharmaceutically acceptable salt thereof. In the formula, R1 represents an aryl or the like; R11 represents an aryl or the like; R2 represents a formyl or the like, R3 represents a C1-6 alkyl or the like; R3 represents a hydrogen atom or the like; Z1 represents —O— or the like; Z2 represents —O— or the like; Y1-Y4 respectively represent a carbon atom or a nitrogen atom; ring A represents a heteroaryl group; X represents a carbon atom or the like; m represents an integer of 0-2; and q represents an integer of 0-2.Type: GrantFiled: September 29, 2006Date of Patent: September 21, 2010Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Keiji Takahashi, Yoshio Ogino, Teruyuki Nishimura
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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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Publication number: 20100216854Abstract: The present invention provides novel 1,5 and 1,3,5-substituted imidazole compounds of formulas (I), (IIa), (IIIb) in hydrophilic or lipophilic form, which are useful as angiotensin II AT1 receptor antagonists with sympathetic suppressant properties. In particular, the invention provides pharmaceutical compositions containing the pharmacophoric groups of Losartan and Clonidine as well compounds, processes and intermediates for preparing compounds and their use in methods of treating hypertension and cardiovascular diseases through Renin Angiotensin System (RAS) and Sympathetic System (SS). Alkylated histamine based double action Saltans are lipophilic and can act transdermally.Type: ApplicationFiled: July 25, 2008Publication date: August 26, 2010Applicant: Eldrug S.A.Inventors: John Matsoukas, Charalambos Gavras, Dimitrios Vlaxakos, Michael Maragoudakis
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Publication number: 20100204199Abstract: Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-Beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: enantiomers, diastereomers, solvates, or salts thereof, wherein A, W, X and Z are defined herein.Type: ApplicationFiled: April 14, 2010Publication date: August 12, 2010Inventors: Xiang-Yang Ye, Jeffrey A. Robl, Ronald L. Hanson, Zhiwei Guo, Ramesh N. Patel
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Publication number: 20100184991Abstract: The invention relates to a process for the preparation of (S)-pyrrolidine-1H-tetrazole derivatives of formula wherein R1, R2 and R3, independently of one another, represent hydrogen, halogen or an organic radical, in racemic form or as an enantiomer, a tautomer, an analog thereof or a salt thereof.Type: ApplicationFiled: March 29, 2010Publication date: July 22, 2010Inventors: Gottfried Sedelmeier, Valentina Aureggi
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Publication number: 20100184975Abstract: The invention provides novel compounds useful for the treatment of neurodegenerative disorders including Alzheimer's disease and dementia. The compounds have a substituents chosen from -L-C(?O)OH, -L-CH?CHC(?O)OH, -L-C(?O)NH2, -L-C(?0)NH(C1-3alkyl), -L-C(?O)N(C1-3alkyl)2, -L-S(?O)2(C1-3alkyl), -L-S(?O)2NH2, -L-S(?O)2N(C1-3alkyl)2, -L-S(?O)2NH(C1-3alkyl), -L-C(?O)NHOH, -L-C(?O)CH2NH2, -L-C(?O)CH2OH, -L-C(?O)CH2SH, -L-C(?O)NHCN, -L-NHC(?O)ORo, -L-C(?O)NHRo, -L-NH(C?O)NHRo, -L-C(?O)N(Ro)2, -L-NH(C?O)N(Ro)2, -L-sulfo, -L-(2,6 difluorophenol), -L-phosphono, and -L-tetrazolyl, where L is a linker.Type: ApplicationFiled: March 8, 2010Publication date: July 22, 2010Applicant: Myriad Pharmaceuticals, Inc.Inventors: Rachel Slade, Yevgeniya Klimova, Robert J. Halter, Ashantai J. Yungai, Warren S. Weiner, Ruth J. Walton, Jon Adam Willardsen, Mark B. Anderson, Kenton Zavitz
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Publication number: 20100174091Abstract: A process for the preparation of a compound of formula (I), or a salt, hydrate or solvate thereof; wherein R1 and R2 are each independently hydrogen, or C1-6 alkyl groups or R1 and R2 are linked and, together with the cyclopentane carbon atoms to which they are attached, form a cyclopropyl ring.Type: ApplicationFiled: April 20, 2006Publication date: July 8, 2010Inventors: Michael Stewart Ashwood, Matthew Bio, Edward Cleator, David Hands, Faye Julia Sheen, Robert Darrin Wilson
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Publication number: 20100144809Abstract: This invention relates to novel benzamidine derivatives of formula (I) 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. A stereoisomer or a mixture of its stereoisomers, or an N-oxide thereof, or a pharmaceutically-acceptable addition salt thereof, wherein B may be absent (i.e. no heterocyclic ring is formed); and when absent, the nitrogen next to B holds a hydrogen (i.e. “NH”), and A represents NH2 or OH; or B may be present (i.e. forms part of a heterocyclic ring); and when present, B represents C?O or C?S; and A represents NH or O; and wherein the rest of variables are as specified in claim 1.Type: ApplicationFiled: May 7, 2008Publication date: June 10, 2010Applicant: Neuro Search A/SInventors: Antonio Nardi, Joachim Demnitz, Morten Grunnet, Palle Christophersen, David Spencer Jones, Elsebet Østergaard Nielsen, Dorte Strøbæk, Lars Siim Madsen
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Publication number: 20100137387Abstract: This invention relates to novel ?-keto-amide derivatives that are found to be potent modulators of ion channels, and in particular potassium channels and chloride 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: April 29, 2008Publication date: June 3, 2010Applicant: NeuroSearch A/SInventors: Antonio Nardi, Jeppe Kejser Christensen, Morten Grunnet, Palle Christophersen, David Spencer Jones, Elsebet Østergaard Nielsen, Dorte Strøbæk, Lars Siim Madsen
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Patent number: 7728023Abstract: The present invention relates to a compound represented by the formula (I), wherein all symbols are as defined in the description, a salt thereof, a solvate thereof, or a prodrug thereof, which has a leukotriene receptor antagonistic activity which is expected to be more effective than those of the leukotriene receptor antagonists currently used in clinical trials. Therefore, it is useful as an agent for the prevention and/or treatment of a leukotriene-mediated disease such as a respiratory diseases such as bronchial asthma, chronic obstructive pulmonary disease, pulmonary emphysema, chronic bronchitis, pneumonia (e.g. interstitial pneumonia etc.), severe acute respiratory syndrome (SARS), acute respiratory distress syndrome (ARDS), allergic rhinitis, sinusitis (e.g. acute sinusitis, chronic sinusitis, etc.), or the like, or as an expectorant or an antiitussive.Type: GrantFiled: February 24, 2006Date of Patent: June 1, 2010Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Jun Takeuchi, Yoshisuke Nakayama, Manabu Fujita
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Publication number: 20100120784Abstract: Heteroaromatic compounds of structural formula (I) or a pharmaceutically acceptable salt thereof, wherein W is a substituted heteroaryl, X and Y are each independently a bond, —O—, —S—, —S(O)—, —S(O)2—, —NR6—, —C(O)—, —C(CH3)(OH)— or —C(CH3)?CH—, u (I) is an integer from 1 to 4, and Ar is an optionally substituted phenyl or naphtyl, are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD) The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis, obesity, Type 2 diabetes, insulin resistance, hyperglycemia, Metabolic Syndrome, neurological disease, cancer, and liver steatosisType: ApplicationFiled: April 17, 2008Publication date: May 13, 2010Inventors: Nicolas Lachance, Chun Sing Li, Jean-Philppe Leclerc, Yeeman K. Ramtohul
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Patent number: 7714143Abstract: A method of forming monoammonium salt of 5,5?-bis-1H-tetrazole (BTA-1NH3) is presented comprising the steps of charging a mixing vessel with a solution of free BTA acid and distilled water, adding ammonium hydroxide in excess to obtain a pH of at least 9.5 and mixing the solution, and adding sulfuric acid cooled to 10-20 degrees Celsius to obtain a pH of at least 4.5 and mixing the solution. A gas generator 10 containing a gas generant 12 containing the BTA-1NH3 formed in accordance with the present invention is also presented. Gas generating systems 180 such as vehicle occupant protection systems 180, containing the gas generator 10, are also provided.Type: GrantFiled: March 31, 2008Date of Patent: May 11, 2010Assignee: TK Holdings, Inc.Inventors: Deborah L. Hordos, Sean P. Burns
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Publication number: 20100113777Abstract: A compound, or its salt, or a solvate thereof having a cPLA2 inhibiting activity having the formula (I): or a pharmaceutical composition, cPLA2 inhibitor and inhibitors of various lipid mediator production containing the same as active ingredients.Type: ApplicationFiled: March 28, 2008Publication date: May 6, 2010Applicant: Asubio Pharma Co., Ltd.Inventors: Toshiyuki Tomoo, Takashi Nakatsuka, Yasuhiro Hayashi, Toyoko Katayama
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Patent number: 7678796Abstract: The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.Type: GrantFiled: April 25, 2007Date of Patent: March 16, 2010Assignee: AstraZeneca ABInventors: Andreas Wallberg, Karolina Nilsson, Björn Holm, Mats Nagard, Kenneth Granberg, Abdelmalik Slassi, Louise Edwards, Methvin Isaac, Tao Xin, Tomislav Stefanac
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Publication number: 20100063299Abstract: Disclosed herein is an improved, commercially viable and industrially advantageous process for the preparation of Irbesartan, or a pharmaceutically acceptable salt thereof, in high yield and purity.Type: ApplicationFiled: March 6, 2008Publication date: March 11, 2010Inventors: Udhaya Kumar, Praveen Kumar Neela, Nitin Sharadchandra Pradhan, Jon Valgeirsson
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Patent number: 7649009Abstract: Pyrazole amides are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.Type: GrantFiled: July 1, 2005Date of Patent: January 19, 2010Assignee: Merck & Co., Inc.Inventors: Teresa Beeson, Linda Brockunier, Emma R. Parmee, Subharekha Raghavan
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Publication number: 20090306396Abstract: The present invention relates to novel compounds having a xanthine oxidase inhibitory effect and an uricosuric effect and pharmaceutical compositions comprising the same as an active ingredient. That is, the present invention relates nitrogen-containing heterocyclic compounds represented by the following general formula (I): wherein Y1 represents N or C(R4); Y2 represents N or C(R5); R4 and R5 independently represent an alkyl group, a hydrogen atom etc.; one of R1 and R2 represents an optionally substituted aryl group, an alkoxy group or an optionally substituted heterocyclic group; the other of R1 and R2 represents a haloalkyl group, a cyano group, a halogen atom etc.; and R3 represents a 5-tetrazolyl group or a carboxy group, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising the same as an active ingredient.Type: ApplicationFiled: October 3, 2006Publication date: December 10, 2009Applicant: KISSEI PHARMACEUTICAL CO., LTD.Inventors: Takahiro Toyoshima, Toshinobu Sasaki, Chikara Hoshino, Masakazu Takeda
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Publication number: 20090291993Abstract: The present application relates to novel difluorophenol derivatives, 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: November 26, 2009Inventors: Stephan Bartel, Michael Hahn, Wahed Ahmed Moradi, Eva-Maria Becker, Thomas Rölle, Johannes-Peter Stasch, Karl-Heinz Schlemmer, Frank Wunder, Andreas Knorr
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Publication number: 20090281327Abstract: The present invention provides a process for the preparation of Olmesartan medoxomil] by condensing the ethyl 4-(1-hydroxy-1-methylethyl)-2-propylimidazole-5-carboxylate with 4-[2-(trityl tetrazol-5-yl)phenyl]benzyl bromide to obtain ethyl 4-(1-hydroxy-1-methyl ethyl)-2-propyl-1-{4-[2-(trityl tetrazol-5-yl)phenyl]phenyl}methylimidazole-5-carboxylate and then hydrolyzing ethyl 4-(1-hydroxy-1-methyl ethyl)-2-propyl-1-{4-[2-(trityl tetrazol-5-yl)phenyl]phenyl}methyl imidazole-5-carboxylate to obtain trityl Olmesartan dihydrate followed by reacting trityl Olmesartan dihydrate with 4-chloromethyl-5-methyl-2-oxo-1,3-dioxolene to obtain trityl Olmesartan medoxomil and then deprotecting trityl Olmesartan medoxomil to obtain Olmesartan medoxomil.Type: ApplicationFiled: June 15, 2007Publication date: November 12, 2009Inventors: Gorantla Seeta Ramanjaneyulu, Bandari Mohan, Purna Chandra Ray, Madhuresh Kumar Sethi, Vijendra Singh Rawat, Yerramalla Raja Krishna, Vemula Lakshminarayana, Mamidi Srinivas
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Publication number: 20090281328Abstract: A new class of phosphoinositide-dependent kinase-1 (PDK-1) inhibitors of formula I: wherein X is selected from the group consisting of alkyl and haloalkyl; Ar is an aryl radical selected from the group consisting of phenyl, biphenyl, naphthyl, anthryl, phenanthryl, and fluorenyl; and wherein Ar is optionally substituted with one or more radicals selected from the group consisting of halo, C1-C4 alkyl, C1-C4 haloalkyl, azido, C1-C4 azidoalkyl, aryl, alkylaryl, haloaryl, haloalkylaryl, and combinations thereof; and R is selected from the group consisting of nitrile, acetonitrile, ethylnitrile, propylnitrile, carboxamide, amidine, tetrazole, oxime, hydrazone, acetamidine, aminoacetamide, guanidine, and urea. Also provided are methods of using the compounds for the treatment and prevention of cancer in humans.Type: ApplicationFiled: June 2, 2009Publication date: November 12, 2009Applicant: THE OHIO STATE UNIVERSITY RESEARCH FOUNDATIONInventor: Ching-Shih Chen
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Publication number: 20090264653Abstract: Indoles that have activity as inhibitors of FAAH are described as are indoles and indole derivatives that have activity as inhibitors of DAO.Type: ApplicationFiled: December 18, 2006Publication date: October 22, 2009Inventors: Wilmin Bartolini, Brian M Cali, Barbara Chen, Yueh-Tyng Chien, Mark G. Currie, G. Todd Milne, James Philip Pearson, John Jeffrey Talley, Jane Yang, Craig Zimmerman, Charles Kim, Kevin Sprott, Timothy Barden, Regina Lundigran, Ara Mermerian
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Publication number: 20090258918Abstract: This invention relates to potent selective agonists of the EP4 subtype of prostaglandin E2 receptors, their use or a formulation thereof in the treatment of glaucoma and other conditions which are related to elevated intraocular pressure in the eye of a patient.Type: ApplicationFiled: June 10, 2009Publication date: October 15, 2009Inventors: Xavier Billot, Robert N. Young, Yongxin Han
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Patent number: 7595405Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted tetrazolyl, R2 is optionally substituted phenyl, optionally substituted pyridinyl or optionally substituted thienyl, and R3, R4, R5 and R6 are as defined herein. Also provided are methods of using the compounds for treating diseases associated with the P2X3 and/or a P2X2/3 receptor antagonist and methods of making the compounds.Type: GrantFiled: June 28, 2007Date of Patent: September 29, 2009Assignee: Roche Palo Alto LLCInventors: Michael Patrick Dillon, Ronald Charles Hawley, Li Chen, Lichun Feng, Minmin Yang
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Patent number: 7576098Abstract: The present invention relates generally to compounds that inhibit serine proteases. In particular it is directed to novel heterocyclic compounds, or a stereoisomer or pharmaceutically acceptable salt, solvate, or prodrug form thereof, which are useful as selective inhibitors of serine protease enzymes of the coagulation cascade; for example thrombin, factor VIIa, factor Xa, factor XIa, factor IXa, and/or plasma kallikrein. In particular, it relates to compounds that are factor VIIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of using the same.Type: GrantFiled: December 7, 2005Date of Patent: August 18, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Peter W. Glunz, Nicolas Wurtz, Xuhong Cheng
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Patent number: 7572753Abstract: The use of certain tetrazole compounds as fungicides is disclosed wherein said compounds are of the structural formula: wherein: R is selected from the group consisting of phenyl groups of the structural formula: and thienyl groups of the structural formula: and X and Y are each selected from the group consisting of hydrogen, haloalkyl, halogen, and nitro. Novel compounds wherein X is selected from the group consisting of haloalkyl, halogen, and nitro and Y is selected from the group consisting of hydrogen, haloalkyl, halogen, and nitro are also disclosed.Type: GrantFiled: September 15, 2005Date of Patent: August 11, 2009Assignee: Chemtura CorporationInventors: Mark A. Dekeyser, Ahmad Ghavami, Robert G. Davis, Sheldon B. Park, Steven J. Hobbs, Clifford Pratt, Gaik-Lean Chee, Daniel Walther
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Patent number: 7557220Abstract: A linear isocyanate polymer produced by utilizing an effective amount of tetrazole diol or tetrazole polyol, reacting with an effective amount isocyanate resin, and cooling to room temperature producing a linear polyisocyanate polymer.Type: GrantFiled: May 27, 2005Date of Patent: July 7, 2009Assignee: The United States of America as represented by the Secretary of the NavyInventors: David J. Irvin, Mark H. Mason
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Patent number: 7514438Abstract: Novel compounds, or pharmaceutically-acceptable salts, tautomers or prodrugs thereof, of Formula I wherein A, W, X, Z, R1-R3, and R8 are as defined in the specification, are provided. Also provided are methods of treating or preventing a melanin concentrating hormone-mediated disorder in a subject, comprising administering to a subject in need of such treatment or prevention a compound of Formula I.Type: GrantFiled: August 11, 2004Date of Patent: April 7, 2009Assignee: Amgen, Inc.Inventors: Christopher Hulme, Paul A. Tempest, Vu Van Ma, Thomas Nixey, Guity Balow
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Publication number: 20090076281Abstract: The invention relates to the preparation of losartan and losartan potassium. More particularly, the invention relates to the preparation of losartan and losartan potassium in a simplified process that provides higher purity losartan potassium and losartan potassium having larger crystal sizes. The invention further includes formulating into readily usable dosage units for the therapeutic treatment (including prophylactic treatment) of mammals, including humans.Type: ApplicationFiled: May 5, 2005Publication date: March 19, 2009Applicant: MEDICHEM, S.A.Inventor: Carme Arnalot Aguilar
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Publication number: 20090042960Abstract: The compounds of the formula (I) in which R1 represents cycloalkyl, and its stereoisomers and any mixtures thereof are highly suitable as microbicides for protecting plants and materials.Type: ApplicationFiled: June 27, 2006Publication date: February 12, 2009Inventors: Rainer Bruns, Martin Kugler, Erasmus Vogl, Hermann Uhr, Oliver Kretschik
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Publication number: 20090012087Abstract: This invention relates to novel pharmaceutically useful compounds of formula (I), in particular compounds that are competitive inhibitors of trypsin-like serine proteases, especially thrombin, their use as medicaments, pharmaceutical compositions containing them and synthetic routes to their production.Type: ApplicationFiled: July 2, 2008Publication date: January 8, 2009Applicant: ASTRAZENECA ABInventors: Jonas Branalt, Ingemar Nilsson, Magnus Polla
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Publication number: 20080281097Abstract: Process for preparing angiotensin II receptor antagonists, in particular irbesartan, protected forms for the preparation thereof, or a pharmaceutically acceptable salt thereof, that comprises the reaction between a biphenylamino derivative and an oxazolone derivative. New intermediates are useful for the preparation of angiotensin II receptor antagonists.Type: ApplicationFiled: August 3, 2006Publication date: November 13, 2008Applicant: FARMAPROJECTS, S. A.Inventor: Jordi Bessa Belmunt
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Publication number: 20080207715Abstract: The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, wherein: R1 represents heteroaryl, -carbocyclyl-heteroaryl, -alkenylheteroaryl or -alkylheteroaryl; R2 represents alkyl, which may optionally be substituted by one or more groups selected from amino, halogen, hydroxyl, -alkoxy, -thioalkyl, —C(O)O-alkyl and —C(O)OH; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl, haloalkyl, amino, halogen, hydroxyl, alkoxy-, -thioalkyl, —C(O)O-alkyl and —C(O)OH; alkenyl; alkynyl; -alkyl-aryl; -alkyl-heteroaryl; -alkyl-heterocyclyl; -alkyl-carbocyclyl; -aryl-heteroaryl; -heteroaryl-aryl; -heteroaryl-heteroaryl; -aryl-aryl; -aryl (monocyclic or bicyclic); heteroaryl (monocyclic or bicyclic); heterocyclyl; or R2 together with R4 may form a carbocyclyl group optionally substituted by one or more alkyl groups; R3 represents alkyl, which may optionally be substituted by one or more groups selected from amino, halogen, hydroxType: ApplicationFiled: November 8, 2007Publication date: August 28, 2008Applicant: PROBIODRUG AGInventors: Michael Thormann, Michael Altmstetter, Andreas Treml, Ulrich Heiser, Mirko Buchholz
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Patent number: 7414068Abstract: The present invention relates to benzopyran derivatives substituted with secondary amines including tetrazole, method for preparing thereof and pharmaceutical compositions containing them. The compounds of the present invention can be used for protecting neuronal cells and brain damage; antioxidation; inhibiting NO generation; protecting heart; suppressing angiogenesis; protecting preserving organs such as kidney, heart and tissue, and protecting organs in major cardiovascular surgery.Type: GrantFiled: April 10, 2003Date of Patent: August 19, 2008Assignee: Dongbu Hannong Chemical Co., Ltd.Inventors: Hong Lim, Dong-Ha Lee, Sun-Ok Kim, In-Young Choi, Sung-Eun Yoo, Kyu-Yang Yi, Sun-Kyung Lee, Jee-Hee Suh, Nak-Jeong Kim, Byung-Ho Lee, Ho-Won Seo, Hwa-Sup Shin
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Patent number: 7407974Abstract: The present invention provides compounds of Formula (I): wherein A, B, C, G, and W1 have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful to treat thrombotic disorders. Also disclosed are pharmaceutical compositions comprising one or more compounds of Formula I, processes for preparing compounds of Formula I, and intermediates useful for preparing compounds of Formula I.Type: GrantFiled: April 18, 2005Date of Patent: August 5, 2008Assignee: Pfizer Inc.Inventors: Christopher Franklin Bigge, Agustin Casimiro-Garcia, Danette Andrea Dudley, Jeremy John Edmunds, Kevin James Filipski, Jeffrey Thomas Kohrt, Chad Alan Van Huis
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Publication number: 20080153812Abstract: There is provided a compound of formula (I): or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.Type: ApplicationFiled: December 18, 2007Publication date: June 26, 2008Applicant: ASTRAZENECA ABInventors: David Buttar, Kevin Micheal Foote, Maria-Elena Theoclitou, Andrew Peter Thomas
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Publication number: 20080139628Abstract: The invention provides a method of reducing flushing induced by niacin or a niacin analog in a subject, comprising administering to said subject an effective flush reducing amount of a niacin receptor partial agonist. In addition, the invention provides a method of reducing flushing induced by niacin or a niacin analog in a subject, comprising administering to said subject an effective flush reducing amount of a niacin receptor partial agonist and an effective lipid altering amount of niacin or a niacin analog. The invention further provides a method of reducing flushing induced by niacin or a niacin analog in a subject, comprising administering to said subject an effective flush reducing amount of a niacin receptor partial agonist and subsequently administering to said subject an effective lipid altering amount of niacin or a niacin analog.Type: ApplicationFiled: November 1, 2005Publication date: June 12, 2008Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Dominic P. Behan, Daniel T. Connolly, Jeremy G. Richman
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Publication number: 20080132555Abstract: Disclosed herein are substituted phenyltetrazoles of Formula I, processes of preparation thereof, pharmaceutical compositions thereof, and the methods of their use thereof.Type: ApplicationFiled: November 28, 2007Publication date: June 5, 2008Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
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Patent number: 7378433Abstract: The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R1 is hydrogen, hydroxy, C1-6alkyl or aryl; R2 is hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl, optionally substituted pyrrolidinyl or aryl; R3 is hydrogen, optionally substituted C1-6alkyl or aryl; Het is an optionally substituted unsaturated heterocycle selected from imidazolyl, triazolyl, tetrazolyl and pyridinyl; is an optionally substituted unsaturated mono- or bicyclic heterocycle; and aryl is optionally substituted phenyl. The present invention also relates to processes for their preparation and compositions comprising said new compounds, as well as their use as a medicine.Type: GrantFiled: December 13, 2006Date of Patent: May 27, 2008Assignee: Janssen Pharmaceutica, N.V.Inventors: Marc Gaston Venet, Dominique Jean-Pierre Mabire, Jean Fernand Armand Lacrampe, Gerard Charles Sanz
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Publication number: 20080087549Abstract: An additive for copper plating comprising, as an effective ingredient, a nitrogen-containing biphenyl derivative represented by the following formula (I): [wherein X represents a group selected from the following groups (II)-(VII): and Y represents a lower alkyl group, lower alkoxy group, nitro group, amino group, sulfonyl group, cyano group, carbonyl group, 1-pyridyl group, or the formula (VIII): (wherein R? represents a lower alkyl group)], a copper plating solution formed by adding the additive for copper plating to a copper plating solution containing a copper ion ingredient and an anion ingredient, and a method of manufacturing on an electronic circuit substrate having a fine copper wiring circuit, which comprises electroplating in the copper plating solution using as the cathode an electronic circuit substrate in which fine microholes or microgrooves in the shape of an electronic circuit are formed on the surface.Type: ApplicationFiled: August 18, 2004Publication date: April 17, 2008Applicant: EBARA-UDYLITE CO.,LTD.Inventors: Hiroshi Ishizuka, Nobuo Sakagawa, Ryoichi Kimizuka, Wei-ping Dow
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Patent number: 7326732Abstract: A compound of formula (I): or a salt, solvate and chemically protected form thereof, wherein: R5 is an optionally substituted C5-20 aryl or C4-20 alkyl group; A is selected from the group consisting of: wherein X and Y are selected from the group consisting of: O and CR3; S and CR3; NH and CR3; NH and N; O and N; S and N; N and S; and N and O, and where the dotted lines indicate a double bond in the appropriate location, and where Q is either N or CH; R3 is selected from H, F, Cl and optionally substituted C1-4 alkyl, C1-4 alkoxy, C5-7 aryl and C5-7 aryl-C1-4 alkyl groups; R4 is selected from H, F, Cl and optionally substituted C1-4 alkyl, C1-4 alkoxy, C5-7 aryl and C5-7 aryl-C1-4 alkyl groups; R6 is selected from H, F, Cl and optionally substituted C1-4 alkyl, C1-4 alkoxy, C5-7 aryl and C5-7 aryl-C1-4 alkyl groups; D is selected from: B is selected from the group consisting of: where RN? is selected from H and C1-4 alkyl; where one of RP3 and RP4 is —Cm alkylene-R2 and tType: GrantFiled: February 11, 2005Date of Patent: February 5, 2008Assignee: Pharmagene Laboratories LimitedInventors: Alexander William Oxford, Richard Jon Davis, Robert Alexander Coleman, Kenneth Lyle Clark, David Edward Clark, Neil Victor Harris, Garry Fenton, George Hynd, Keith Alfred James Stuttle, Jonathan Mark Sutton, Mark Richard Ashton, Edward Andrew Boyd, Shirley Ann Brunton
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Patent number: 7323483Abstract: The present invention provides processes for the preparation of substituted naphthylindole derivatives that can be used as inhibitors of plasminogen activator inhibitor-1(PAI-1). In certain embodiments of the invention, the processes involve reactions that include one or more of an Oppenauer oxidation, a Fischer indole synthesis, a methyl ether cleavage, or coupling a substituted methyltetrazole with a substituted naphthol.Type: GrantFiled: January 25, 2006Date of Patent: January 29, 2008Assignee: WyethInventors: Vladimir A. Dragan, John Richard Potoski, Wayne G. McMahon, Jean Louise Helom, Xinxu Shi
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Patent number: 7323480Abstract: The present invention is directed to certain novel triazole compounds represented by Formula I and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof. The present invention is also directed to methods of making and using such compounds and pharmaceutical compositions containing such compounds to treat or control a number of diseases mediated by PPAR such as glucose metabolism, lipid metabolism and insulin secretion, specifically Type 2 diabetes, hyperinsulemia, hyperlipidemia, hyperuricemia, hypercholesteremia, atherosclerosis, one or more risk factors for cardiovascular disease, Syndrome X, hypertriglyceridemia, hyperglycemia, obesity, and eating disorders.Type: GrantFiled: May 24, 2005Date of Patent: January 29, 2008Assignee: Metabolex, Inc.Inventors: Yan Zhu, Jingyuan Ma, Peng Cheng, Zuchun Zhao, Francine M. Gregoire, Vera A. Rakhmanova
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Patent number: RE41226Abstract: Compounds of formula (I) wherein the groups are as defined in the description are disclosed. The compounds of formula (I) are endowed with reversible inhibiting activity of carnitine palmitoyl-transferase and are useful in the preparation of medicaments useful in the pathologies related to a hyperactivity of carnitine polymitoyl-transferase, such as hyperglycemia, diabetes and pathologies related thereto, heart failure, ischemia.Type: GrantFiled: December 1, 2006Date of Patent: April 13, 2010Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Fabio Giannessi, Mauro Marzi, Patrizia Minetti, Francesco De Angelis, Maria Ornella Tinti, Piero Chiodi, Arduino Arduini