Polycyclo Ring System Having The 1,3-thiazole Ring As One Of The Cyclos Patents (Class 546/270.1)
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Publication number: 20090163535Abstract: Disclosed are substituted heteroarylalkanoic acids of the following formula D-A-C(O)R?, where D, A, and R? are defined herein. These compounds are useful in the treatment of chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds and methods of treatment employing the compounds, as well as methods for their synthesis.Type: ApplicationFiled: April 22, 2008Publication date: June 25, 2009Applicant: The Institues for Pharmaceutical Discovery, Inc.Inventors: Michael C. Van Zandt, Leo Geraci
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Publication number: 20090130077Abstract: The invention relates to substituted benzothiazoles, benzoxazoles—and their counterparts having pyridine and pyrimidine rings replacing the benzene ring—that are PDE4 inhibitors useful for treating stroke, myocardial infarct, and cardiovascular inflammatory conditions, to pharmaceutical compositions comprising these compounds, and to methods for the treatment of stroke, myocardial infarct, and cardiovascular inflammatory conditions in a mammal. The compounds have general formula I: in which A and B are carbocycles or heterocycles.Type: ApplicationFiled: November 20, 2008Publication date: May 21, 2009Applicant: deCODE genetics ehfInventors: Jasbir Singh, Mark E. Gurney, Alex Burgin, Vincent Sandanayaka, Alexander Kiselyov, Munagala Rao
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Publication number: 20090130076Abstract: The invention relates to substituted benzothiazoles, benzoxazoles—and their counterparts having pyridine and pyrimidine rings replacing the benzene ring—that are PDE4 inhibitors useful for treating stroke, myocardial infarct, and cardiovascular inflammatory conditions, to pharmaceutical compositions comprising these compounds, and to methods for the treatment of stroke, myocardial infarct, and cardiovascular inflammatory conditions in a mammal. The compounds have general formula I: in which A and B are carbocycles or heterocycles.Type: ApplicationFiled: November 20, 2008Publication date: May 21, 2009Applicant: DECODE GENETICS EHFInventors: Jasbir Singh, Mark E. Gurney, Alex Burgin, Alexander Kiselyov, Munagala Rao
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Patent number: 7531558Abstract: Compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein P, W, X, Y, R2, R3, r and s are as defined in the specification, processes for preparing such compounds, pharmaceutical compositions comprising such compounds and their use in therapy.Type: GrantFiled: February 12, 2004Date of Patent: May 12, 2009Assignee: Glaxo Group LimitedInventors: Gregor James Macdonald, Darren Jason Mitchell, Harshad Kantilal Rami, Mervyn Thompson, Leontine Saskia Trouw, Susan Marie Westaway
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Publication number: 20090111794Abstract: Aryl-substituted bridged or fused diamine compounds, pharmaceutical compositions containing them, and methods of using the compounds and the pharmaceutical compositions for leukotriene A4 hydrolase (LTA4H or LTA4H) modulation and for the treatment of disease states, disorders, and conditions mediated by LTA4H activity, such as allergy, asthma, autoimmune diseases, pruritis, inflammatory bowel disease, ulcerative colitis, and cardiovascular disease, including atherosclerosis and prevention of myocardial infarction.Type: ApplicationFiled: October 30, 2008Publication date: April 30, 2009Inventors: Genesis M. Bacani, Scott D. Bembenek, Wendy Eccles, James P. Edwards, Matthew T. Epperson, Laurent Gomez, Cheryl A. Grice, Aaron M. Kearney, Adrienne M. Landry-Bayle, Alice Lee-Dutra, Kelly J. McClure, Taraneh Mirzadegan, Alejandro Santillan, JR.
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Patent number: 7524951Abstract: The present invention relates to compounds represented by formula (1) and a process for producing the same. The use of these compounds can realize the production of carbapenem derivatives having potent antimicrobial activity and a wide antimicrobial spectrum in a safe and cost-effective manner.Type: GrantFiled: December 15, 2003Date of Patent: April 28, 2009Assignee: Meiji Seika Kaisha, Ltd.Inventors: Toshiro Sasaki, Takashi Ando, Yasuo Yamamoto, Takahiro Imai, Dai Kubota, Katsuhiko Noguchi, Nobuyuki Hori, Eiki Shitara, Kunio Atsumi, Shohei Yasuda
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Publication number: 20090082571Abstract: The present invention relates to compounds represented by formula (1) and a process for producing the same. The use of these compounds can realize the production of carbapenem derivatives having potent antimicrobial activity and a wide antimicrobial spectrum in a safe and cost-effective manner.Type: ApplicationFiled: November 3, 2008Publication date: March 26, 2009Inventors: Toshiro Sasaki, Takashi Ando, Takahiro Imai, Dai Kubota, Eiki Shitara, Kunio Atsumi
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Publication number: 20090062259Abstract: The present invention relates to compounds according to formula (I), a process for preparing them, the intermediate compounds of the process and the use of the compounds in the manufacture of a medicament for use in treating diseases such as ARDS, pulmonary emphysema, bronchitis, bronchiectasis, COPD, asthma and rhinitis. The compounds are beta adrenoreceptor agonists.Type: ApplicationFiled: March 12, 2007Publication date: March 5, 2009Applicant: ASTRAZENECA ABInventors: Lilian Alcaraz, Andrew Lister, Garry Pairaudeau
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Publication number: 20090054463Abstract: The present invention relates generally to compounds represented in Formula I, pharmaceutical compositions comprising them and methods of treating of diseases or disorders related to the function of the calcium sensing receptor. The invention also relates to processes for making such compounds and to intermediates useful in these processes.Type: ApplicationFiled: July 10, 2008Publication date: February 26, 2009Inventors: Pierre Deprez, Christopher Fotsch, Paul Harrington, Sarah Lively, Kanaka Pattabiraman, David St. Jean, Taoues Temal-Laib
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Publication number: 20090029863Abstract: The invention disclosed in this document is related to field of pesticides and their use in controlling pests. In particular compounds having the following formula are disclosed.Type: ApplicationFiled: July 11, 2008Publication date: January 29, 2009Applicant: Dow AgroSciences LLCInventors: Benjamin M. Nugent, Ann M. Buysse, Jonathan M. Babcock, Matthias S. Ober, Timothy P. Martin
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Publication number: 20090028787Abstract: The present invention relates to novel heteroaryl substituted benzothiazole derivatives, precursors thereof, and therapeutic uses for such compounds, having the structural formula (I) below: [Chemical formula should be inserted here. Please see paper copy] and to their pharmaceutically acceptable salt, compositions and methods of use. Furthermore, the invention relates to novel heteroaryl substituted benzothiazole derivatives that are suitable for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. More specifically, the present invention relates to a method of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease as well as measuring clinical efficacy of Alzheimer's disease therapeutic agents.Type: ApplicationFiled: January 25, 2007Publication date: January 29, 2009Inventors: Ylva Gravenfors, Catrin Jonasson, Jonas Malmstrom, Gunnar Nordvall, David Pyring, Can Slivo, Daniel Sohn, Peter Strom, David Wensbo
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Publication number: 20090012082Abstract: The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting the cell with a hedgehog antagonist, such as a small molecule, in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity.Type: ApplicationFiled: November 3, 2005Publication date: January 8, 2009Applicant: CURIS, INC.Inventors: Olivin M. Guicherit, Edward Andrew Boyd, Judith Boyd, Shirley Ann Brunton, Stephen Price, John Harry Alexander Stibbard, Colin H. MacKinnon
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Publication number: 20090012080Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: June 20, 2008Publication date: January 8, 2009Applicant: Sirtris Pharmaceuticals, Inc.Inventors: Jean Bemis, Jeremy S. Disch, Michael Jirousek, Walter Joseph Lunsmann, Pui Yee Ng, Chi B. Vu
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Publication number: 20090005399Abstract: Substituted imidazo[2,1-b]thiazole compounds corresponding to formula I, a method for producing them, pharmaceutical compositions containing them, and the use thereof for regularing mGluR5 receptors, or for treating or inhibiting disorders or disease states at least partially mediated by mGluR5 receptor such as pain, anxiety attacks, drug or alcohol dependency, and others.Type: ApplicationFiled: September 9, 2008Publication date: January 1, 2009Applicant: Gruenenthal GmbHInventors: Sven KUEHNERT, Saskia ZEMOLKA, Michael HAURAND, Klaus SCHIENE
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Publication number: 20080300275Abstract: The present invention provides compounds of formula (I) wherein e, R1, R2, R3, R4, R5, R4, R5, R6, R7, R7a, R7b, A, D, m and n are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: August 3, 2006Publication date: December 4, 2008Applicant: ASTRAZENECA ABInventors: Roger Bonnert, Alice Flaherty, Garry Pairaudeau, Michael Stocks
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Publication number: 20080275090Abstract: The present invention provides novel amino-benzazoles and analogues thereof, which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases responsive to modulation of P2Y1 receptor activity.Type: ApplicationFiled: April 17, 2008Publication date: November 6, 2008Inventors: Timothy F. Herpin, George C. Morton, Robert P. Rehfuss, R. Michael Lawrence, Michael A. Poss, Jacques Y. Roberge, Timur Gungor
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Publication number: 20080267883Abstract: This invention relates to new fluorescent chemical entities, including fluorescent molecules that comprise a carboxyl or carbonyl functionalized pyridine moiety. This invention also relates to the corresponding reactive versions of such molecules. This invention also relates to the corresponding conjugates with moieties such as peptides, proteins, various biomolecules, carbocyclic and heterocyclic compounds, sugars, and their uses thereof.Type: ApplicationFiled: September 1, 2006Publication date: October 30, 2008Inventors: Milind Rajopadhye, Nara Narayanan, Jeffrey D. Peterson
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Publication number: 20080261953Abstract: Compounds and compositions are provided for treatment or amelioration of one or more symptoms of ?-synuclein toxicity, ?-synuclein mediated diseases or diseases in which ?-synuclein fibrils are a symptom or cause of the disease. In one embodiment, the compounds for use in the compositions and methods are heteroaryl acylguanidines, heteroarylhydrazones, dihy-dropyridones, heteroaryl and aryl styryl ketones, and heteroarylpyrazoles.Type: ApplicationFiled: September 16, 2005Publication date: October 23, 2008Applicants: WHITEHEAD INSTITUTE FOR BIOMEDICAL RESEARCH, FOLDRX PHARMACEUTICALS, INC.Inventors: Susan L. Lindquist, Tiago Outeiro, Richard Labaudiniere
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Publication number: 20080207698Abstract: The present invention provides compounds of formula (I) wherein Ra, Rb, R1, R2, R3, R4, R5, R6 and R29 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: December 19, 2007Publication date: August 28, 2008Inventors: Stephen Connolly, Alexander Humphries, Premji Meghani
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Publication number: 20080193700Abstract: The invention relates to novel optical recording media, which comprise particular novel metal chelates and have an excellent recording and playback quality, especially at a wavelength of from 300 to 500 nm.Type: ApplicationFiled: April 25, 2005Publication date: August 14, 2008Applicant: CIBA SPECIALTY CHEMICALS HOLDING INC.Inventors: Heinz Wolleb, Annemarie Wolleb, Frank Bienewald, Beat Schmidhalter, Jean-Luc Budry
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Publication number: 20080161358Abstract: The present invention provides previous methods for the use of compounds as depicted by structure I, pharmaceutical compositions containing the same, and methods for the prophylaxis, management and treatment of metabolic diseases and diseases modulated by MCD inhibition. The compounds disclosed in this invention are useful for the prophylaxis, management and treatment of diseases involving in malonyl-CoA regulated glucose/fatty acid metabolism pathway. In particular, these compounds and pharmaceutical composition containing the same are indicated in the prophylaxis, management and treatment of cardiovascular diseases, diabetes, cancer and obesity.Type: ApplicationFiled: October 2, 2007Publication date: July 3, 2008Inventors: Mark D. Kafka, Mark E. Wilson, Anna Russell, Gary D. Lopaschuk, Jason R. Dyck
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Patent number: 7393866Abstract: The present invention provides to a novel compound having an ACAT inhibiting activity.Type: GrantFiled: November 9, 2004Date of Patent: July 1, 2008Assignee: Kowa Company, Ltd.Inventors: Kimiyuki Shibuya, Toru Miura, Katsumi Kawamine, Yukihiro Sato, Tadaaki Ohgiya, Takahiro Kitamura, Chiyoka Ozaki, Toshiyuki Edano, Mitsuteru Hirata
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Publication number: 20080153869Abstract: The invention relates to compounds having one of the below formulae that may be used to inhibit kinases as well as compositions of matter and kits comprising these compounds, and methods using the compounds.Type: ApplicationFiled: June 13, 2005Publication date: June 26, 2008Inventors: Jerome C. Bressi, Anthony R. Gangloff, David J. Hosfield, Andrew J. Jennings, Bheema R. Paraselli, Jeffrey A. Stafford
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Patent number: 7390907Abstract: Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, dType: GrantFiled: September 30, 2004Date of Patent: June 24, 2008Assignee: Amgen Inc.Inventors: Ning Chen, Thomas Nixey, Mark H. Norman
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Publication number: 20080132513Abstract: The invention relates to certain fused ring compounds, or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: ApplicationFiled: September 25, 2007Publication date: June 5, 2008Applicant: Synta Pharmaceuticals Corp.Inventors: Quinglin Che, Nha Huu Vo, Shoujun Chen
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Patent number: 7378240Abstract: The present invention relates to new cyanine dyes according to the formula (I), wherein A1 and A2 are each independently O, S, or N, and R is H or a carbohydrate that may contain a hetero atom, and m is 0 to 5, and n is 0 to 5.Type: GrantFiled: November 10, 2003Date of Patent: May 27, 2008Assignee: Light Up Technologies ABInventors: Gunnar Westman, Jonas Karlsson
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Patent number: 7371748Abstract: This invention relates to compounds of formula I wherein R1 and R2 are defined herein, or a pharmaceutically acceptable salt thereof. It has been found that the compounds of formula I are adenosine receptor ligands with good affinity to the A2A-receptor and a high selectivity to the A1- and A3 receptors. These compounds are useful, inter alia, in treatment of Alzheimer's disease, depression, Parkinson's disease and ADHD.Type: GrantFiled: May 17, 2004Date of Patent: May 13, 2008Assignee: Hoffman-La Roche Inc.Inventors: Alexander Flohr, Roland Jakob-Roetne, Roger David Norcross, Claus Riemer
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Publication number: 20080108799Abstract: The present invention relates to the use of thiazolyl-pyridinium based dyes in optical layers for optical data recording, preferably for optical data recording using a laser with a wavelength up to 450 mn. The invention further relates to a write only read many (WORM) type optical data recording medium capable of recording and reproducing information with radiation of blue laser, which employs a thiazolyl-pyridinium based type dye in the optical layer. The present invention further relates to new thiazolyl-pyridinium based dyes, of formula (V), (VI) or (VIII).Type: ApplicationFiled: August 31, 2005Publication date: May 8, 2008Inventor: Andre Weiss
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Patent number: 7361671Abstract: Disclosed are substituted heteroarylalkanoic acids acids of the following formula D-A-C(O)R?, where D, A, and R? are defined herein. These compounds are useful in the treatment of chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds and methods of treatment employing the compounds, as well as methods for their synthesis.Type: GrantFiled: November 14, 2002Date of Patent: April 22, 2008Assignee: The Institute for Pharmaceutical Discovery, Inc.Inventors: Michael C. Van Zandt, Leo Geraci
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Patent number: 7358263Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands and methods for using such compounds and compositions.Type: GrantFiled: February 16, 2006Date of Patent: April 15, 2008Assignee: Abbott LaboratoriesInventors: Marlon D. Cowart, Yi-Yin Ku, Sou-Jen Chang, Dilinie P. Fernando
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Patent number: 7351807Abstract: Dye-sulfenate derivatives and their bioconjugates for dual phototherapy of tumors and other lesions.Type: GrantFiled: July 3, 2001Date of Patent: April 1, 2008Assignee: Mallinckrodt Inc.Inventors: Raghavan Rajagopalan, Samuel I. Achilefu, Joseph E. Bugaj, Richard B. Dorshow
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Patent number: 7338956Abstract: The present invention relates to acylamino-substituted heteroaromatic compounds of formula I, wherein R1, R2, R3, R4 and R5 and X are as defined herein, to pharmaceutical compositions comprising such compounds, to methods for the stimulation of the expression of endothelial NO synthase, and methods of treatment comprising administering such compounds.Type: GrantFiled: August 5, 2003Date of Patent: March 4, 2008Assignee: Sanofi-Aventis Deutschland GmbHInventors: Hartmut Strobel, Paulus Wohlfart, Peter Below
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Patent number: 7326403Abstract: A radioactive iodine-labeled compound represented by the following formula (I): wherein X represents a radioactive iodine atom which may substitute at an arbitrary position on the benzene ring (preferably 123I, 125I and the like.), n represents an integer of 1 to 3, R1 and R2 each independently represent a substituted or unsubstituted alkyl group, Y represents an alkylene group having 1 to 6 carbon atoms (preferably methylene group), M represents a counter ion, and m represents the number of ions required to neutralize the charge of the molecule. A radioactive iodine-labeled compound that can selectively accumulate in tumor cells or tumor tissue and a scintillation imaging agent containing the compound are provided.Type: GrantFiled: May 26, 2005Date of Patent: February 5, 2008Assignee: FUJIFILM CorporationInventors: Yasuhiro Magata, Hideo Saji
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Publication number: 20070299113Abstract: The invention relates to imidazothiazole derivatives as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are group I mGluR modulators and are therefore useful for the control and prevention of various disorders, including acute and/or chronic neurological disorders.Type: ApplicationFiled: June 22, 2007Publication date: December 27, 2007Applicant: MERZ PHARMA GMBH & CO. KGAAInventors: Ivars Kalvinsh, Larisa Kaulina, Valerjans Kauss, Ronalds Zemribo, Wojciech Danysz, Markus Henrich, Christopher Graham Raphael Parsons, Tanja Weil, Elina Erdmane
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Patent number: 7226740Abstract: Unsymmetrical cyanine dyes that incorporate an aza-benzazolium ring moiety are described, including cyanine dyes substituted by a cationic side chain, monomeric and dimeric cyanine dyes, chemically reactive cyanine dyes, and conjugates of cyanine dyes. The subject dyes are virtually non-fluorescent when diluted in aqueous solution, but exhibit bright fluorescence when associated with nucleic acid polymers such as DNA or RNA, or when associated with detergent-complexed proteins. A variety of applications are described for detection and quantitation of nucleic acids and detergent-complexed proteins in a variety of samples, including solutions, electrophoretic gels, cells, and microorganisms.Type: GrantFiled: October 13, 2003Date of Patent: June 5, 2007Assignee: Invitrogen CorporationInventors: Richard P. Haugland, Stephen T. Yue
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Patent number: 7189854Abstract: Novel cyclic compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders.Type: GrantFiled: May 26, 2005Date of Patent: March 13, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Jagabandhu Das, Ping Chen, Derek J. Norris
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Patent number: 7189743Abstract: The present invention relates to new compounds of general formula having thrombin-inhibiting activity. Exemplary are: 1-Methyl-2-[4-(N-hydroxyamidino)-phenylaminomethyl]-benzimidazol-5-yl-carboxylic acid-(N-2-pyridyl-N-2-ethoxycarbonylethyl)-amide, and 1-Methyl-2-[4-(N-methoxycarbonylamidino)-phenylaminomethyl]-benzimidazol-5-yl-carboxylic acid-(N-2-pyridyl-N-2-hydroxycarbonylethyl)-amide.Type: GrantFiled: February 11, 2005Date of Patent: March 13, 2007Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Norbert Hauel, Florian Colbatzky, Ulrich Busch
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Patent number: 7183293Abstract: This application is directed to compounds of the formula wherein j is 1; k is 0 or 1; m is 1, 2 or 3; n is 1 or 2; W1 and W2 are independently —O— or —S(?O)t—, where t is 0, 1, or 2; Y is ?C(R1a)—, where R1a is a member selected from the group consisting of H; F; Cl; CN; NO2; —(C1–C4)alkyl; —(C2–C4)alkynyl; fluorinated-(C1–C3)alkyl; fluorinated-(C1–C3)alkoxy; —OR16; and —C(?O)NR22aR22b; R22a and R22b are defined as set forth in the specification; —RA and RB are each a member independently selected from the group consisting of H; F; CF3; —(C1–C4)alkyl; —(C3–C7)cycloalkyl; phenyl; and benzyl; wherein said cycloalkyl, phenyl, and benzyl moieties are each independently substituted with 0 to 3 substituents R10, which is defined as set forth in the specification; R16 and R17 are defined as set forth in the specification; —RC and RD have the same meaning as defined above for RA and RB except that one of them must be —H, and they are selected independently of each other and of RA and RB; R1 and R2 are each a membType: GrantFiled: August 13, 2004Date of Patent: February 27, 2007Assignees: Pfizer Inc., Pfizer Products Inc.Inventors: Anthony Marfat, Robert J. Chambers, Thomas V. Magee
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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: 7153873Abstract: Salts of a bicyclic, N-acylated imidazo-3-amine or an imidazo-5-amine of the formula: addition products thereof with acids, and methods for preparing the salts and addition products. Also disclosed are pharmaceutical compositions comprising the same and methods using the pharmaceutical compositions for the treatment or prophylaxis of pain, drug or alcohol abuse, diarrhoea, gastritis, ulcers, urinary incontinence, depression, narcolepsy, overweight, asthma, glaucoma, tinnitus, itching, hyperkinetic syndrome, epilepsy, or schizophrenia, for inducing anesthesia, and for anxiolysis.Type: GrantFiled: June 6, 2006Date of Patent: December 26, 2006Assignee: Gruenenthal GmbHInventors: Matthias Gerlach, Corinna Sundermann
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Patent number: 7112413Abstract: Chemiluminescent heteroaryl substituted benzothiazole 1,2-dioxetane compounds capable of producing light energy when decomposed are provided. These chemiluminescent compounds are represented by the general formula: The heteroaryl substituent Y can be, for example, a pyridyl group or a benzothiazolyl group. The heteroaryl substituted benzothiazole compounds are substantially stable at room temperature. Kits including the heteroaryl substituted dioxetane compounds as well as methods for using these compounds for detecting the presence of one or more analytes in a sample are also provided.Type: GrantFiled: October 7, 2003Date of Patent: September 26, 2006
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Patent number: 7105533Abstract: Phenyl compounds substituted with a fused-heterobicyclo moiety, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, and panic, as well as in the treatment of pain and other diseases.Type: GrantFiled: September 9, 2003Date of Patent: September 12, 2006Assignee: Merck & Co., Inc.Inventors: Brian Thomas Campbell, Janet Lorraine Gunzer, Benito Munoz, Brian Andrew Stearns, Jean-Michel Andre Vernier, Bowei Wang
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Patent number: 7094790Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands and methods for using such compounds and compositions.Type: GrantFiled: April 30, 2004Date of Patent: August 22, 2006Assignee: Abbott LaboratoriesInventors: Marlon D. Cowart, Yi-Yin Ku, Sou-Jen Chang, Dilinie P. Fernando, Timothy A. Grieme, Robert J. Altenbach
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Patent number: 7091219Abstract: Bis-sulfonamido hydroxyethylamino compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to retroviral protease inhibiting compounds of the formula: or a pharmaceutically acceptable salt, prodrug or ester thereof, wherein the variables are as defined herein.Type: GrantFiled: April 17, 2003Date of Patent: August 15, 2006Assignee: G. D. Searle & Co.Inventors: John N. Freskos, Daniel P. Getman, John J. Talley, James A. Sikorski
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Patent number: 7067516Abstract: Compounds of formula (I) where R5, R6a, each X, L, Cy and Lp are as defined in the specification, are tryptase inhibitors useful as antiinflammatory agents.Type: GrantFiled: December 12, 2001Date of Patent: June 27, 2006Assignee: Tularik LimitedInventors: Sarah Elizabeth Lively, Martin James Harrison, Neil Jason Naylor, Christopher Neil Farthing, Bohdan Waszkowycz
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Patent number: 7057042Abstract: The present invention relates to the use of compounds of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction, wherein A, L, D and B1 are as described in the specification.Type: GrantFiled: May 23, 2003Date of Patent: June 6, 2006Assignee: Abbott LaboratoriesInventors: Marlon D. Cowart, Steven P. Latshaw, Sherry L. Nelson, Andrew O. Stewart
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Patent number: 7049271Abstract: The present invention relates to novel phenyl-substituted 2-enamino-ketonitriles of the formula (I): in which Ar, X, Z, Y and K are each as defined in the description, to a plurality of processes for their preparation and to their use as herbicides and pesticides.Type: GrantFiled: April 25, 2001Date of Patent: May 23, 2006Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Jutta Böhmer, Ralf Wischnat, Mark Wilhelm Drewes, Peter Dahmen, Rolf Pontzen, Peter Lösel, Christoph Erdelen, Dieter Feucht
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Patent number: 7034035Abstract: The present invention relates to compounds of Formula I: wherein: a) ?represents a 6-membered heterocyclic aromatic ring in which X1 is N and X2, X3 and X4 are each independently CR?; R? is independently H, halogen, cyano, hydroxy, C1-C3 alkyl, C1-C3 haloalkyl, cyclopropyl, C1-C3 alkoxy, C1-C3 haloalkoxy, C1-C3 alkylthio, aryl, C1-C3 NHC(O)alkyl, NHC(O)H, C1-C3 haloalkylthio, C2-C4 alkenyl, C2-C4 haloalkenyl, C2-C4 alkynyl, C2-C4 haloalkynyl or nitro wherein adjacent R? substituents may form a ring; b) Z is O, S or NORZ in which RZ is H or C1-C3 alkyl; and c) A represents (i) C3-C14 cycloalkyl, containing 1 or 3 heteroatoms and 0-2 unsaturations, which may be unsubstituted or substituted with halogen, hydroxy, C1-C6 alkyl, C1-C6 haloalkyl, cyano, nitro, aroyl, aryloxy, heteroaryloxy, C1-C6 alkylthio, arylthio, heteroarylthio, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C8 acyloxy, aryl, heteroaryl, C1-C6 acyl, C1-C6 carboalkoxy or amido unsubstituted or substituted with one or two C1 -C6 alkyl groups, oType: GrantFiled: December 2, 2002Date of Patent: April 25, 2006Assignee: Dow AgroSciences LLCInventors: Michael J. Ricks, William H. Dent, III, Richard B. Rogers, Chenglin Yao, Bassam S. Nader, John L. Miesel, Gina M. Fitzpatrick, Kevin G. Meyer, Noormohamed M. Niyaz, Irene M. Morrison, Robert P. Gajewski
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Patent number: 7026321Abstract: Disclosed are novel heterocyclic derivatives, useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, and myocardial infarction. The compounds are also useful in the treatment of diabetes.Type: GrantFiled: January 16, 2004Date of Patent: April 11, 2006Assignee: CV Therapeutics, Inc.Inventors: Robert Jiang, Tim Marquart, Jeff Zablocki, Elfatih Elzein, Venkata Palle, Prabha Ibrahim
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Patent number: RE39198Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amounts of one of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: November 15, 2000Date of Patent: July 18, 2006Assignee: Aventis Pharmaceuticals Inc.Inventors: Joseph T. Strupczewski, Grover C. Helsley, Yulin Chiang, Kenneth J. Bordeau, Edward J. Glamkowski