The Additional Hetero Ring Contains Sulfur As The Only Ring Hetero Atom [e.g., 5-(2-thienyl) Hydantoin, Etc.] Patents (Class 548/315.1)
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Patent number: 7737293Abstract: An amide is formed by reacting an ?-ketoacid or salt thereof in a decarboxylative condensation reaction with an amine or salt thereof comprising a nitrogen covalently bound to an atom selected from oxygen, nitrogen, and sulfur. The amide bond is formed between the ?-carbon of the ketoacid and the nitrogen of the amine. The ?-ketoacid can be formed using a novel sulfur reagent.Type: GrantFiled: November 10, 2008Date of Patent: June 15, 2010Assignee: Regents of the University of CaliforniaInventors: Jeffrey W. Bode, Ryan M. Fox
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Publication number: 20100144813Abstract: Novel 4-heteroarylimidazole-2-thione tyrosinase inhibiting compounds corresponding to the following general formula (I): formulated into pharmaceutical or cosmetic compositions are useful for the treatment or prevention of pigmentary disorders, or for preventing and/or treating signs of skin aging, and/or for body or hair hygiene.Type: ApplicationFiled: December 4, 2009Publication date: June 10, 2010Applicant: GALDERMA RESEARCH & DEVELOPMENTInventors: Jean Guy BOITEAU, Corinne Millois Barbuis, Karine Bouquet
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Publication number: 20100144810Abstract: A compound having the structure wherein R is an angiotensin receptor antagonist active group, and Y is Y is selected from the group consisting of R1 is selected from the group consisting of —O—C1-6 alkyl, —O-aryl, —O-heteroaryl, —O—C3-8 cycloalkyl, —C1-6 alkyl, -aryl, -heteroaryl, and —C3-8 cycloalkyl; R2 and R3 are independently selected from the group consisting of hydrogen and C1-4 alkyl, or a pharmaceutically acceptable salt or hydrate thereof, which is useful for treating hypertension.Type: ApplicationFiled: December 2, 2009Publication date: June 10, 2010Inventors: Michael Man-Chu Lo, Amjad Ali, Ravi P. Nargund
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Publication number: 20100144812Abstract: Compounds useful for lowering beta amyloid levels are provided. The compounds have the structure of formula Ia: wherein, R1 is lower alkyl, substituted lower alkyl, phenyl, substituted phenyl, benzyl, substituted benzyl, benzyloxy, substituted benzyloxy, or SO2R5; R5 is phenyl, substituted phenyl, heterocycle, substituted heterocycle, alkyl, or substituted alkyl; R2 is lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, or cycloalkyl; R3 is hydrogen, lower alkyl, or substituted lower alkyl; R4 is phenyl, substituted phenyl, heterocycle, substituted heterocycle, thiophene, or substituted thiophene; R6 is hydrogen, lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, cycloalkyl, or substituted cycloalkyl; W, X and Y are independently CR7 or N; and R7 is hydrogen, halogen, lower alkyl, or substituted lower alkyl.Type: ApplicationFiled: February 19, 2010Publication date: June 10, 2010Applicant: Wyeth LLPInventors: Lynn Resnick, Donna M. Huryn, Joan E. Sabalski, Joshua D. Berkowitz, Anthony Frank Kreft, Dennis Martin Kubrak, Thomas Joseph Caggiano, Koi Michele Morris
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Publication number: 20100137613Abstract: The present invention provides an improved and commercially viable process for preparation of eprosartan and its pharmaceutically acceptable acid addition salts thereof in high purity and in high yield. Thus, for example, methyl 4-[[2-butyl-5-formyl-1 H-imidazol-1-yl]methyl]benzoate is reacted with ethyl 2-carboxy-3-(2-thienyl)propionate in the presence of a base, such as piperidine or piperidinium propionate in propionic acid, in cyclohexane solvent to give ethyl (?E)-?-[(2-n-butyl-1-[(4-(methoxy-carbonyl) phenyl]methyl]-1 H-imidazol-5-yl]methylene-2-thiophene propionate substantially free of decarboxylate impurity namely, ethyl 3-(2-thienyl)propionate, which is then subjected to base hydrolysis followed by treatment with methanesulfonic acid to obtain eprosartan mesylate in high purity and in high yield.Type: ApplicationFiled: December 27, 2006Publication date: June 3, 2010Applicant: HETERO DRUGS LIMITEDInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy, Medabalimi Peter Paul Raj
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Publication number: 20100105719Abstract: The present invention relates to imidazolidinecarboxamide derivatives of the general formula I, wherein R, R1, R2, X and Y are as defined herein, or pharmaceutically usable salts thereof and the use thereof as medicinal substances.Type: ApplicationFiled: October 2, 2009Publication date: April 29, 2010Applicant: SANOFI-AVENTISInventors: Gerhard ZOLLER, Stefan PETRY, Gunter MÜLLER, Norbert TENNAGELS
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Publication number: 20100075964Abstract: Compounds of the invention, such as compounds of Formulae IIa, IIb, IIc or IId, and pharmaceutically acceptable salts, isomers, and prodrugs thereof, are useful as modulators of the activity of liver X receptors, where R1, R2, R21, R3 and G are defined herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.Type: ApplicationFiled: June 26, 2006Publication date: March 25, 2010Applicant: EXELIXIS, INC.Inventors: Brett B. Busch, Brenton T. Flatt, Xiao-Hui Gu, Shao-Po Lu, Richard Martin, Raju Mohan, Michael Charles Nyman, Edwin Schweiger, William C. Stevens, Jr., Tie-Lin Wang, Yinong Xie
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Publication number: 20100063119Abstract: There is provided a novel LXR? agonist useful as a preventative and/or therapeutic agent for arteriosclerosis; arteriosclerosis such as those resulting from diabetes; hyperlipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases caused by inflammatory cytokines, skin diseases such as allergic skin diseases, diabetes or Alzheimer's disease. The agonist is a carbinol derivative represented by the following general formula (1) or salt thereof, or their solvate.Type: ApplicationFiled: November 29, 2007Publication date: March 11, 2010Applicant: KOWA COMPANY, LTD.Inventors: Takayuki Matsuda, Ayumu Okuda, Minoru Koura, Yuki Yamaguchi, Sayaka Kurobuchi, Yuuichirou Watanabe, Kimiyuki Shibuya
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Patent number: 7671141Abstract: Disclosed herein are second order nonlinear optic polyimide polymers comprising repeating units represented by the formula: wherein each of the substituents is given the definition as set forth in the Specification and Claims. Also disclosed are the preparation processes of these polymers, chromophore-forming compounds for synthesis of these polymers, and the intermediate polymers thereof. The second order nonlinear optic polyimide polymers of formula (I) may be used in the manufacture of electro-optic (EO) devices, such as electro-optic waveguide devices.Type: GrantFiled: June 28, 2006Date of Patent: March 2, 2010Assignee: National Sun Yat-Sen UniversityInventors: Tzu-Chien Hsu, Chien-Fan Chen, Shou-Shiun Wu
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Patent number: 7670512Abstract: Disclosed herein are second order nonlinear optic polyimide polymers comprising repeating units represented by the formula: wherein each of the substituents is given the definition as set forth in the Specification and Claims. Also disclosed are the preparation processes of these polymers, chromophore-forming compounds for synthesis of these polymers, and the intermediate polymers thereof. The second order nonlinear optic polyimide polymers of formula (I) may be used in the manufacture of electro-optic (EO) devices, such as electro-optic waveguide devices.Type: GrantFiled: June 28, 2006Date of Patent: March 2, 2010Assignee: National Sun Yat-Sen UniversityInventors: Tzu-Chien Hsu, Chien-Fan Chen, Shou-Shiun Wu
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Publication number: 20100010062Abstract: The disclosed invention relates to a method of treatment of a disorder modulated by blocking angiotensin II (AII) receptors, and particularly selected from the group consisting of hypertension, congestive heart failure, renal failure, and combinations thereof, by administering to a subject in need thereof an effective dose of an eprosartan compound. With reference to the Recommended Effective Daily Dose of 600 mg, calculated on the basis of eprosartan administered in the form of eprosartan mesylate, it has now been found that a lower dose of eprosartan can be administered when the eprosartan compound is eprosartan acid. This dose is in the range of from 410 to 490 mg, most preferably about 450 mg.Type: ApplicationFiled: July 9, 2009Publication date: January 14, 2010Applicant: Solvay Pharmaceuticals B.V.Inventors: Paulus A.J. Link, Marcellus M. van der Hulst, Gerhard-Wilhelm Bielenberg, Cornelis R. van den Akker
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Publication number: 20090298900Abstract: Compounds represented by Formula I and II, or pharmaceutically acceptable salts thereof: inhibit bacterial 2-epimerase and are useful anti-infective agents.Type: ApplicationFiled: May 11, 2009Publication date: December 3, 2009Inventors: David J. Bearss, Hariprasad Vankayalapati, Yong Xu, Charles Erec Stabbins, Vincent A. Fischetti
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Publication number: 20090286840Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: ApplicationFiled: April 12, 2007Publication date: November 19, 2009Inventors: Guy Brenchley, Steven Durrant, Jean-Damien Charrier, Ronald Knegtel, Sharn Ramaya, Shazia Sadiq
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Publication number: 20090281101Abstract: Compounds comprising a structure or a pharmaceutically acceptable salt thereof, or a prodrug thereof; wherein a dashed line represents the presence or absence of a bond are disclosed, wherein Y, A, B, and J are as described. Methods, compositions, and medicaments related thereto are also disclosed.Type: ApplicationFiled: May 1, 2009Publication date: November 12, 2009Applicant: ALLERGAN, INC.Inventor: David W. Old
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Publication number: 20090274655Abstract: Anti-viral agents of compounds of Formula (I): wherein A, R1, R2 and R3 are as defined in the specification, processes for their preparation and their use in HCV treatment are provided.Type: ApplicationFiled: November 15, 2007Publication date: November 5, 2009Inventors: Richard Martin Grimes, Charles David Hartley, Jacqueline Elizabeth Mordaunt, Pritom Shah, Martin John Slater, Gemma Victoria White
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Publication number: 20090270473Abstract: The invention relates to compounds having the formula: wherein: Q, W, Y, Z, r, and Ar are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: April 28, 2009Publication date: October 29, 2009Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Robert Murray McKinnell
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Publication number: 20090253764Abstract: The invention relates to the use of imidazole derivatives of the formula (1): in which A, R?1, R?2 and R?3 are as defined in the description, as AMPK activators. The invention also relates to processes for the preparation of the said compounds, to their uses for the preparation of medicaments for the treatment of insulin resistance, diabetes and related pathologies, and also obesity, and to the pharmaceutical compositions comprising them. Certain compounds of the formula (1) are novel and, in this respect, also form part of the invention.Type: ApplicationFiled: June 12, 2007Publication date: October 8, 2009Inventors: Gerard Moinet, Dominique Marais, Sophie Hallakou-Bozec, Christine Charon
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Publication number: 20090215847Abstract: There is provided compounds of formula I, wherein the dotted line, X1, X2, X3, A, Y1, Y2, Y3, Y4, Z1, Z2, R2 and R3 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful as selective agonists of the AT2 receptor, and thus, in particular, in the treatment of inter alia gastrointestinal conditions, such as dyspepsia, IBS and MOF, and cardiovascular disorders.Type: ApplicationFiled: April 12, 2006Publication date: August 27, 2009Inventors: Mathias Alterman, Anders Hallberg, Xiongyu Wu
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Patent number: 7566734Abstract: The present invention is directed to imidazolyl derivatives of formula (I) where the substituents are defined in the specification, which are useful as agonists or antagonists of somatostatin receptors.Type: GrantFiled: July 31, 2001Date of Patent: July 28, 2009Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques, S.A.S.Inventors: Christophe Alain Thurieau, Lydie Francine Poitout, Marie-Odile Galcera, Thomas D. Gordon, Barry A. Morgan, Christophe Philippe Moinet, Dennis C. H. Bigg
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Publication number: 20090176716Abstract: The invention relates to compounds of the general formula (I) and salts and physiologically functional derivatives thereof, wherein Y is —NRaRb, —NRcC?ONRaRb, —NRcC?SNRaRb, —NRcC?NRdNaRb, heterocycle, —C?ONRaRb, heterocycle, or aryl; n is 0 to 8; m is 0, or 1; r is 0 to 3; t is 0 to 3; X is O or N; Z is CH2, C?O, C?S or a single bond; Z1 is CO—R2, CS—R2, (CH2)t—R2 or the side-chain of a naturally occurring amino acid; Z2 is CO—R2, CS—R2 or (CH2)t—R3 or the side-chain of a naturally occurring amino acid; Z3 is CO—R2, CS—R2 or (CH2)t—R4 or the side-chain of a naturally occurring amino acid; Z4 is H, alkyl, alkoxy, or cycloalkyl; R1, R2, R3, and R4 are independently from each other H, OH, SH, NH2, CN, NO2, alkyl, cycloalkyl, heterocycloalkyl, haloalkyl, alkylthio, haloalkyloxy, hydroxyalkyl, hydroxyalkylamino, alkylamino, alkylaryl, alkylsulfinyl, alkylsulfonyl, alkylthioalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, alkoxyalkyl, alkoxy, aryloxy, heteroaryl, aryl, or halogen.Type: ApplicationFiled: March 9, 2009Publication date: July 9, 2009Inventors: Johann Leban, Martin Kralik
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Publication number: 20090156585Abstract: A specific combination, linked pro-drug or a compound of an angiotensin receptor antagonist and a NEPi are used in the treatment of hypertension.Type: ApplicationFiled: November 8, 2006Publication date: June 18, 2009Inventors: Lili Feng, Sven Erik Godtfredsen, Bin Hu, Yugang Liu, Piotr Karpinski, Paul Allen Sutton, Mahavir Prashad, Michael J. Girgis, Thomas J. Blacklock
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Publication number: 20090149474Abstract: The present invention relates to novel imidazole derivatives having a positive allosteric GABAB receptor (GBR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABAB agonist, for the inhibition of transient lower esophageal sphincter relaxations, for the treatment of gastroesophageal reflux disease, as well as for the treatment of functional gastrointestinal disorders and irritable bowel syndrome (IBS). The compounds are represented by the general formula (I) wherein R1, R2, R3 and R4 are as defined in the description. For example, R1 may be phenyl, R2 may be dimethylamino pyrrolidin-1-yl, R3 may be alkoxy and R4 may be alkyl, ai arylalkyl, aryloxyalkyl, aryloxy or heterocyclylalkyl.Type: ApplicationFiled: December 21, 2006Publication date: June 11, 2009Inventors: Udo Bauer, Wayne Brailsford, Linda Gustafsson, Tor Svensson
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Publication number: 20090118335Abstract: The present invention provides a compound having a superior acid secretion inhibitory action, an antiulcer activity and the like.Type: ApplicationFiled: March 30, 2007Publication date: May 7, 2009Applicant: Takeda Pharmaceutical Company LimitedInventors: Atsushi Hasuoka, Terufumi Takagi, Masahiro Kajino, Haruyuki Nishida
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Publication number: 20090062361Abstract: Disclosed herein is a compound represented by a formula Therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: ApplicationFiled: August 15, 2008Publication date: March 5, 2009Applicant: ALLERGAN, INC.Inventor: David W. Old
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Publication number: 20090042931Abstract: There is provided compounds of formula I, wherein A, X1, X2, X3, X4, Y1, Y2, Y3, Y4, Z1, Z2, R4 and R5 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful as selective agonists of the AT2 receptor, and thus, in particular, in the treatment of inter alia gastrointestinal conditions, such as dyspepsia, IBS and MOF, and cardiovascular disorders.Type: ApplicationFiled: April 12, 2006Publication date: February 12, 2009Applicant: Vicore Pharma ABInventors: Mathias Alterman, Anders Hallberg, Xiongyu Wu
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Publication number: 20090032106Abstract: There is provided novel n-type conjugated compounds based on 2-vinyl-4,5-dicyanoimidazole moieties conjugated via the vinyl group to an aromatic moiety. Also provided are thin films and photovoltaics comprising the novel compounds, as well as methods of synthesizing the compounds.Type: ApplicationFiled: July 31, 2007Publication date: February 5, 2009Inventors: Alan Sellinger, Richard Yee Cheong Shin, Thomas Kietzke, Zhikuan Chen, Sundarraj Sudhakar
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Patent number: 7482374Abstract: The invention relates to compounds of formula (I): wherein substituents are as defined.Type: GrantFiled: July 17, 2004Date of Patent: January 27, 2009Assignee: Glaxo Group LimitedInventors: Alan David Borthwick, Henry Anderson Kelly, Nigel Stephen Watson, Robert John Young
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Publication number: 20090012057Abstract: The invention describes compositions and kits comprising at least one cardiovascular compound comprising at least one nitric oxide enhancing group, or pharmaceutically acceptable salts thereof, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; Q) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension; (n) treating ophthalmic disorders; (o) treating metabolic syndrome; and (p) treating hyperlipidemia.Type: ApplicationFiled: February 28, 2006Publication date: January 8, 2009Applicant: NitroMed, Inc.Inventor: David S. Garvey
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Publication number: 20080312299Abstract: Imidazole derivatives of formula (I) wherein R1, R2a, R2b, A, V and W are as defined in the description, as inhibitors of fructose-1,6-bisphosphatase, their preparation process and their use in the prevention or treatment of diabetes, and other diseases where the inhibition of gluconeogenesis, control of blood glucose levels, reduction in glycogen stores, or reduction in insulin levels is beneficial and diseases related to the insulin resistance syndrome.Type: ApplicationFiled: July 19, 2006Publication date: December 18, 2008Inventors: Denis Carniato, Gerard Moinet, Gerard Botton, Annick Arbellot De Vacqueur, Annick Audet
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Publication number: 20080306091Abstract: The present invention provides a 2-amino-5-heteroaryl-5-phenylimidazolone compound of formula I The present invention also provides methods for the use thereof to inhibit ?-secretase (BACE) and treat ?-amyloid deposits and neurofibrillary tanglesType: ApplicationFiled: July 28, 2008Publication date: December 11, 2008Applicant: WyethInventors: Michael Sotirios Malamas, Ping Zhou, William Floyd Fobare, William Ronald Solvibile, Iwan Suwandi Gunawan, James Joseph Erdei, Yinfa Yan, Patrick Michael Andrae, Dominick Anthony Quagliato
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Publication number: 20080306121Abstract: The present invention provides small molecule compounds of bisheterocycle in tandem having the structural formula of P1-P2, and the use thereof as well as a composition containing the compounds, each of P1 and P2 is an unsaturated 5-member heterocyclic ring having one or two heteroatoms. This compound may effectively inhibit the replication of influenza virus, the DNA replication of hepatitis B virus (HBV), and the formation of HBsAg and HBeAg. These compounds can be used for the preparation of a medicament for viral diseases, and may overcome the limitations of the known nucleosides drugs, including cytotoxicity, the requirement of other drugs having different structures for against the drug-resistant virus variants induced by long-term therapy. The structure of the compounds according to the invention is relatively simple and easy to be prepared.Type: ApplicationFiled: January 24, 2006Publication date: December 11, 2008Applicant: Shanghai Institute of Materia Medica, Chinese Academy of SciencesInventors: Fajun Nan, Jianping Zuo, Wenlong Wang, Haijun Chen, Peilan He
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Patent number: 7446213Abstract: Novel methods allowing for the simple optical detection and electrochemical detection of doubled-straded oligonucleotides are disclosed. The methods are rapid, selective and versatile. Advantageously, they do not require any chemical reaction on the probes or on the analytes since they are based on different electrostatic interactions between cationic poly(3-alkoxy-4-methylthiophene) derivatives and single-stranded or doubled-stranded (hybridized) oligonucleotides.Type: GrantFiled: March 7, 2006Date of Patent: November 4, 2008Assignee: Geneohm Sciences Canada, Inc.Inventors: Mario Leclerc, Hoang Anh Ho, Maurice Boissinot
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Publication number: 20080262064Abstract: The present invention relates to novel imidazole compounds having a positive allosteric GABAB receptor (CUR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABAB agonist, for the inhibition of transient lower esophageal sphincter relaxations, for the treatment of gastroesophageal reflux disease, as well as for the treatment of functional gastrointestinal disorders and irritable bowel syndrome (IBS).Type: ApplicationFiled: April 17, 2008Publication date: October 23, 2008Applicant: ASTRAZENECA ABInventors: Udo Bauer, Wayne Brailsford, Leifeng Cheng, Maria Jonforsen, Florian Raubacher, Peter Schell, Tor Svensson
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Patent number: 7425639Abstract: An improved process for preparing arylethanoldiamines is described. Compounds of this type are known to be useful as agonists at a typical beta-adrenoceptors (also known as beta-3-adrenoceptors).Type: GrantFiled: December 17, 2001Date of Patent: September 16, 2008Assignee: SmithKline Beecham CorporationInventors: Jason William Beames Cooke, Bobby Neal Glover, Ronnie Maxwell Lawrence, Matthew Jude Sharp, Maria Fumiko Tymoschenko
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Patent number: 7365196Abstract: A class of compounds is disclosed, comprising sulphonamido-substituted bridged bicycloalkyl structures. The compounds are inhibitors of gamma-secretase, and hence are useful in the treatment of and/or prevention of Alzheimer's disease.Type: GrantFiled: March 15, 2001Date of Patent: April 29, 2008Assignees: Merck Sharp & Dohme Ltd., Merck Frosst Canada & Co.Inventors: Patrice Charles Belanger, Ian James Collins, Joanne Claire Hannam, Timothy Harrison, Stephen John Lewis, Andrew Madin, Edward Giles McIver, Alan John Nadin, Joseph George Neduvelil, Mark Steven Shearman, Adrian Leonard Smith, Timothy Jason Sparey, Graeme Irvine Stevenson, Martin Richard Teall
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Publication number: 20080058397Abstract: A compound having a structure is disclosed herein. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: ApplicationFiled: August 30, 2007Publication date: March 6, 2008Inventor: David W. Old
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Patent number: 7320995Abstract: The present invention provides kinase inhibitors of Formula I: wherein W represents inter alia imidazol, oxazol, pyrazol, thiazol as triazol, which are substituted by phenyl or thienyl.Type: GrantFiled: July 31, 2003Date of Patent: January 22, 2008Assignee: Eli Lilly and CompanyInventors: Rosanne Bonjouklian, Jose Eugenio De Diego Gomez, Alfonso De Dios, Chafiq Hamdouchi Hamdouchi, Tiecho Li, Beatriz Lopez De Uralde Garmendia, Michal Vieth, Jeremy Schulenberg York, Robert Dean Dally, Miriam Filadelfa Del Prado Catalina, Carlos Jaramillo Aguado, Luisa Maria Martin-Cabrejas, Carlos Montero Salgado, Sheila Pleite Selgas, Concepcion Sanchez-Martinez, Timothy Alan Shepherd, James Howard Wikel
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Patent number: 7291642Abstract: The present invention provides bradykinin-B1 antagonists of the formula in which A, Ar, G, Q, R1 and R4 are as defined in claim 1, their enantiomers, their diastereomers, their mixtures and their salts, in particular their physiologically acceptable salts with organic or inorganic acids or bases having useful properties, their preparation, medicaments comprising the pharmacologically effective compounds, their preparation and their use.Type: GrantFiled: October 21, 2005Date of Patent: November 6, 2007Assignee: Boehringer Ingelheim International GmbHInventors: Iris Kauffmann-Hefner, Norbert Hauel, Henri Doods, Angelo Ceci, Stefan Peters
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Publication number: 20070249680Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.Type: ApplicationFiled: April 18, 2007Publication date: October 25, 2007Inventors: Carl R. Illig, Shelley K. Ballentine, Jinsheng Chen, Renee Louise DesJarlais, Sanath K. Meegalla, Bruce E. Tomczuk, Mark Wall, Kenneth Wilson
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Patent number: 7271271Abstract: Compounds are provided having the formula: wherein variables R0, R1, R2, R3, R4, Q, L and subscript n are as described herein. The subject compounds are useful for treatment of infammatory and immune conditions and diseases. Compositions and methods of treatment using the subject compounds are also provided. For example, the subject methods are useful for treatment of inflammatory and immune disorders and disease such as multiple sclerosis, rheumatoid arthritis, psoriasis, and inflammatory bowel disease.Type: GrantFiled: June 27, 2005Date of Patent: September 18, 2007Assignee: Amgen SF, LLCInventors: Zice Fu, Michael G. Johnson, An-Rong Li, Andrew P. Marcus, Julio C. Medina, Philippe Bergeron, Xiaoqi Chen, Xiaohui Du, Jeffrey Deignan, Jason A. Duquette, Darin Gustin, Jeffrey T. Mihalic
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Publication number: 20070197569Abstract: The present invention relates to a method for treating depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders which comprises administering to an individual a therapeutically effective amount of a compound of formula I wherein R, X, A, and n are as defined in the specification and pharmaceutically active salts, racemic mixtures, enantiomers, optical isomers and tautomeric forms thereof.Type: ApplicationFiled: January 19, 2007Publication date: August 23, 2007Inventors: Marius Hoener, Sabine Kolczewski, Henri Stalder
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Publication number: 20070197621Abstract: The present invention relates a method for treating depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders which comprises administering to an individual a therapeutically effective amount of a compound of formula I wherein R, R1, R2, A and n are as defined in the specification and to their pharmaceutically active salts. The invention also relates to novel compounds of formula I, pharmaceutical compositions containing them, and methods for their preparation.Type: ApplicationFiled: January 19, 2007Publication date: August 23, 2007Inventors: Guido Galley, Katrin Groebke Zbinden, Marius Hoener, Sabine Kolczewski, Roger Norcross, Henri Stalder
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Patent number: 7259172Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.Type: GrantFiled: July 2, 2004Date of Patent: August 21, 2007Assignee: MethylGene Inc.Inventors: Jeffrey M. Besterman, Jubrail Rahil, Arkadii Vaisburg
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Patent number: 7192975Abstract: Compounds of the formula wherein the substituents are as defined in the specification which are useful for the treatment of pain.Type: GrantFiled: July 24, 2003Date of Patent: March 20, 2007Assignee: Societe de Conseils de Recherches Et d''Applications Scientifiques (S.C.R.A.S.)Inventors: Dennis Bigg, Anne-Marie Liberatore, Pierre-Etienne Chabrier De Lassauniere
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Patent number: 7183277Abstract: Novel compounds of the formula I in which D, W, X, Y, T and R1 are as defined in Patent Claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumours.Type: GrantFiled: March 31, 2003Date of Patent: February 27, 2007Assignee: Merck Patent GmbHInventors: Dieter Dorsch, Werner Mederski, Johannes Gleitz, Bertram Cezanne, Christos Tsaklakidis, Christopher Barnes
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Patent number: 7173129Abstract: The invention relates to compounds, pharmaceutical compositions and methods of using compounds of the general formula or its pharmaceutically acceptable salt or ester, wherein the substituents are defined in the application.Type: GrantFiled: June 7, 2004Date of Patent: February 6, 2007Assignee: Athero Genics, Inc.Inventors: Kimberly J. Worsencroft, Liming Ni, Zhihong Ye, Charles Q. Meng, M. David Weingarten, Jacob E. Simpson, James A. Sikorski
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Patent number: 7109227Abstract: The invention relates to novel imidazolamino compounds. Also disclosed are methods of treating cancer by using one of these compounds and pharmaceutical compositions containing one of these compounds.Type: GrantFiled: August 26, 2003Date of Patent: September 19, 2006Assignee: National Health Research InstitutesInventors: Chiung-Tong Chen, Wen-Tai Li, Der-Ren Hwang, Chu-Chung Lin
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Patent number: 7105564Abstract: The present invention provides novel compounds having a dual antagonistic activity against thromboxane A2 receptor and prostaglandin D2 receptor and pharmaceutical compositions comprising them. A compound of the formula (I): wherein R1 is —CH2—CH?CH—CH2—CH2—CH2—COOR2 or —CH?CH—CH2—CH2—CH2—COOR2; R2 is hydrogen or alkyl; m is 0 or 1; p is 0 or 1; X1 and X3 each is independently optionally substituted aryl or optionally substituted heteroaryl; X2 is a bond, —CH2—, —S—, —SO2—, —CH2—O—, —O—CH2—, —CH2—S—, —S—CH2—, or the like; X4 is —CH2—, —CH2—CH2—, —C(?O)—, or the like, have a dual antagonistic activity against both a thromboxane A2 receptor and a prostaglandin D2 receptor.Type: GrantFiled: March 2, 2000Date of Patent: September 12, 2006Assignee: Shionogi & Co., Ltd.Inventors: Tsunetoshi Honma, Yoshiharu Hiramatsu, Akinori Arimura
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Patent number: 7083928Abstract: Novel methods allowing for the simple optical and electrochemical detection of double-stranded oligonucleotides are disclosed. The methods are rapid, selective and versatile. Advantageously, they do not require any chemical reaction on the probes or on the analytes since they are based on different electrostatic interactions between cationic poly (3-alkoxy-4-methylthiophene) derivatives and single-stranded or double-stranded (hibridized) oligonucleotides.Type: GrantFiled: April 5, 2002Date of Patent: August 1, 2006Assignees: Infectio Diagnostic (I.D.I.), Inc., Universite' LavalInventors: Mario Leclerc, Hoang Anh Ho, Maurice Boissinot
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Patent number: 7041693Abstract: The present application describes novel hydantoin derivatives of formula (I): or pharmaceutically acceptable salt or prodrug forms thereof, wherein L, Z0, R1, R4, R5, and R11 are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-? converting enzyme (TACE), aggrecanase, or a combination thereof.Type: GrantFiled: October 2, 2003Date of Patent: May 9, 2006Assignee: Bristol-Myers Squibb CompanyInventor: James Sheppeck