Chalcogen Attached Indirectly To The Diazole Ring By Acyclic Nonionic Bonding Patents (Class 548/310.1)
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Patent number: 7612211Abstract: The invention is directed to compounds of Formula (I): to pharmaceutical compositions containing such compounds and to methods of treatment using them.Type: GrantFiled: December 12, 2007Date of Patent: November 3, 2009Assignee: Janssen Pharmaceutica N.V.Inventors: Wing S. Cheung, Daniel J. Parks, William H. Parsons, Sharmila Patel, Mark R. Player
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Publication number: 20090264488Abstract: Novel solid forms of bendamustine hydrochloride are described, as well as methods of their preparation and use.Type: ApplicationFiled: March 26, 2009Publication date: October 22, 2009Applicant: Cephalon, Inc.Inventors: Martin Ian Cooper, Laurent D. Courvoisier, Mark Eddleston, Robert E. McKean
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Patent number: 7566733Abstract: The present invention is directed to novel benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.Type: GrantFiled: September 26, 2005Date of Patent: July 28, 2009Assignee: Janssen Pharmaceutica N.V.Inventors: Raymond Ng, Zhihua Sui, Jihua Guan, James C. Lanter, Vernon C. Alford, Jr.
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Publication number: 20090181964Abstract: It is intended to provide a compound useful as a GnRH receptor antagonist. The inventors further investigated propane-1,3-dione derivatives. As a result, they confirmed that a compound having a benzene ring or a thiophene ring substituted with a group represented by —SO2—R3 in a propane-1,3-dione derivative having 2-(1,3-dihydro-2H-benzimidazol-2-ylidene) has an excellent GnRH receptor antagonistic effect and accomplished the present invention. Because the compound of the present invention has a potent GnRH receptor antagonistic effect, it is useful for the treatment of sex hormone-dependent diseases, particularly GnRH-related diseases. Further, because the compound of the present invention has an excellent metabolic stability in human and few drug interactions, therefore it has preferable characteristics as a pharmaceutical used for the above-mentioned diseases.Type: ApplicationFiled: March 30, 2006Publication date: July 16, 2009Inventors: Masaaki Hirano, Isao Kinoyama, Shunichiro Matsumoto, Eiji Kawaminami, Kei Ohnuki, Hirofumi Yamamoto, Kazuhiko Osoda, Tatsuhisa Takahisa, Takashi Shin, Takanori Koike, Itsuro Shimada, Hiroyuki Hisamichi, Toshiyuki Kusayama
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Publication number: 20090170921Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof: wherein R1-R7 are as disclosed in the specification.Type: ApplicationFiled: January 13, 2005Publication date: July 2, 2009Inventors: Marc Gerspacher, Sven Weiler
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Publication number: 20090082416Abstract: The present application describes deuterium-enriched bendamustine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: August 22, 2008Publication date: March 26, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Publication number: 20090030018Abstract: This invention relates to novel benzimidazole derivatives, pharmaceutical compositions containing these compounds, and methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABAA receptor complex, and in particular for combating anxiety and related diseases.Type: ApplicationFiled: April 18, 2006Publication date: January 29, 2009Inventors: Lene Teuber, Janus S. Larsen, Philip K. Ahring, Elsebet Ostergaard Nielsen, Naheed Mirza
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Publication number: 20090023931Abstract: Disclosed is an alanine racemase chiral binaphthol derivative having the ability to recognize amino alcohols selectively on the basis of chirality and transform amino acids from an L-form into a D-form. Methods for the optical resolution of amino acid or amino alcohol and for the optical transformation of D- and L-forms of amino acids using the binaphthol derivative are also provided.Type: ApplicationFiled: February 8, 2008Publication date: January 22, 2009Applicant: Ewha University - Industry Collaboration FoundationInventors: Kim Kwan Mook, Tang Lijun
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Publication number: 20090005344Abstract: Imidazole and benzimidazole boronic acid compounds, analogs thereof, and pharmaceutical formulations are described, along with methods of use thereof for inhibiting inflammatory cytokines such as tumor necrosis factor alpha (TNF-?) in a subject in need thereof.Type: ApplicationFiled: October 27, 2005Publication date: January 1, 2009Applicant: NKUADA, LLCInventors: James F. Burns, Leonardo A. Cabana, Glenn C. Collupy, John R. Didsbury, Tatyana A. Dyakonov, Simon N. Haydar, Michael L. Jones, Francine F. Li, Christopher J. Markworth, Jessymol Mathew, Frank J. Schoenen, David S. Van Vliet, David Middlemiss
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Patent number: 7456293Abstract: The present invention is concerned with racemic or enantiomerically enriched substituted carboxylic acids and derivatives thereof represented by Formula 1; or pharmaceutically acceptable salts thereof. The present invention also includes pharmaceutical compositions comprising an effective amount of a compound of Formula 1 in admixture with a pharmaceutically acceptable carrier or excipient. The compositions may include additional therapeutic agents for combination therapy. The present invention provides a new class of pharmaceutically active compounds, which are useful in the treatment and control of diabetes and its related metabolic diseases.Type: GrantFiled: March 28, 2006Date of Patent: November 25, 2008Assignee: SK Holding Co., LtdInventors: Yong Moon Choi, Hunwoo Shin, Palanichamy Ilankumaran
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Publication number: 20080275097Abstract: Compounds of Formula I: are HIV reverse transcriptase inhibitors, wherein V, W, X, Y, Z, R1, R2, R4, R5, R6, ring A, ring B, j and k are defined herein. The compounds of Formula I, and the pharmaceutically acceptable salts and prodrugs thereof, are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: December 6, 2007Publication date: November 6, 2008Inventors: Neville J. Anthony, Robert Gomez, Samson M. Jolly, Dai-Shi Su, John Lim
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Publication number: 20080146637Abstract: The invention is directed to compounds of Formula (I): to pharmaceutical compositions containing such compounds and to methods of treatment using them.Type: ApplicationFiled: December 12, 2007Publication date: June 19, 2008Inventors: Wing S. Cheung, Daniel J. Parks, William H. Parsons, Sharmila Patel, Mark R. Player
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Publication number: 20080102405Abstract: A resist composition comprising as a quencher a nitrogen-containing organic compound bearing a nitrogen-containing heterocycle and having a molecular weight of at least 380 exhibits a high resolution and satisfactory mask coverage dependence and is useful in microfabrication using electron beam or deep-UV.Type: ApplicationFiled: October 24, 2007Publication date: May 1, 2008Inventors: Takeru Watanabe, Youichi Ohsawa, Masaki Ohashi, Wataru Kusaki, Tomohiro Kobayashi
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Patent number: 7348438Abstract: The present invention is directed to novel benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.Type: GrantFiled: September 26, 2005Date of Patent: March 25, 2008Assignee: Janssen Pharmaceutica N.V.Inventors: Raymond Ng, Zhihua Sui, Jihua Guan, James C. Lanter, Vernon C. Alford, Jr.
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Patent number: 7309716Abstract: The present invention relates to compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein the R1, Z, Y, RA, and W groups of formula I are as defined herein. The invention also provides pharmaceutically acceptable compositions and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: October 28, 2004Date of Patent: December 18, 2007Assignee: Vertex Pharmaceuticals IncorporatedInventors: Dean M. Wilson, Andreas P. Termin, Jesus E. Gonzalez, III, Nicole Zimmermann, Yulian Zhang, Lev T. D. Fanning
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Patent number: 7271261Abstract: 2-Aryl substituted benzimidazoles and imidazo[4,5]pyridines are disclosed as inhibitors of Cds1 and useful as adjuvants to chemotherapy or radiation therapy in the treatment of cancer.Type: GrantFiled: October 18, 2002Date of Patent: September 18, 2007Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Kristen L. Arienti, Frank U. Axe, J. Guy Breitenbucher, Liming Huang, Alice Lee, Kelly J. McClure
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Patent number: 7173053Abstract: Compounds of formula (I) are antibacterial or antiprotozoal agents for treatment of infections in humans and non-human mammals, wherein: Z represents a radical of formula —N(OH)CH(?O) or formula C(?O)NH(OH); R1 represents hydrogen, methyl or trifluromethyl, or except when Z is a radical of formula —N(OH)(?O), a hydroxy, halo or amino group; R2 represents a group R10—(X)n-(ALK)m— wherein R10, ALK, X, m and n are as defined in the specification; R3 represents hydrogen, (C1–C6) alkyl or phenyl(C1–C6)alkyl-; and R5 and R6 are as defined in the specification.Type: GrantFiled: November 8, 2001Date of Patent: February 6, 2007Assignee: British Biotech Pharmaceuticals LimitedInventors: Paul Raymond Beckett, Steven Launchbury, Gilles Pain, Lisa Marie Pratt
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Patent number: 7144909Abstract: This invention relates to novel compounds which are thyroid receptor ligands, preferably antagonists, and to methods for using such compounds in the treatment of cardiac and metabolic disorders, such as cardiac arrhythmias, thyrotoxicosis, subcllinical hyperthyrodism and liver diseases.Type: GrantFiled: January 30, 2002Date of Patent: December 5, 2006Assignee: Karo Bio ABInventors: Johan Malm, Erik Flöistrup, Spiros Grivas, Yi-Lin Li
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Patent number: 7129258Abstract: This invention provides estrogen receptor modulators of formula I, having the structure wherein R1, R2, R2a, R3, R3a, and R4, and X as defined in the specification, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: August 19, 2004Date of Patent: October 31, 2006Assignee: WyethInventors: Michael S. Malamas, Robert E. McDevitt, Iwan Gunawan, Eric S. Manas, Michael D. Collini
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Patent number: 7115645Abstract: Benzimidazoles of general formula I and the use of benzimidazole derivatives for the production of pharmaceutical agents for treatment and prophylaxis of diseases that are associated with a microglia activation are described.Type: GrantFiled: January 16, 2001Date of Patent: October 3, 2006Assignee: Schering AktiengesellschaftInventors: Wolfgang Halfbrodt, Joachim Kuhnke, Ursula Moenning
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Patent number: 7030139Abstract: Compounds of general formula (I), are disclosed and claimed in the present application, as well as salts and pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of painType: GrantFiled: April 18, 2002Date of Patent: April 18, 2006Assignee: AstraZeneca ABInventors: Yun-Xing Cheng, Miroslaw Tomaszewski, Christopher Walpole, Hua Yang
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Patent number: 6919366Abstract: This invention relates to a family of benzimidazole analogs, which are inhibitors of the IgE response to allergens. These compounds are useful in the treatment of allergy, asthma, or any diseases where IgE is pathogenic.Type: GrantFiled: October 16, 2001Date of Patent: July 19, 2005Assignee: Avanir PharmaceuticalsInventors: Jagadish C. Sircar, Mark L. Richards, Michael G. Campbell, Michael W. Major
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Patent number: 6919331Abstract: The present invention concerns antiviral compounds, their methods of preparation and their compositions, and use in the treatment of viral infections. More particularly, the invention provides heterocyclic substituted 2-methylbenzimidazole derivatives for the treatment of respiratory syncytial virus infection.Type: GrantFiled: December 4, 2002Date of Patent: July 19, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Kuo-Long Yu, Xiangdong Wang, Yaxiong Sun, Christopher Cianci, Jan Willem Thuring, Keith Combrink, Nicholas Meanwell, Yi Zhang, Rita L. Civiello
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Patent number: 6900218Abstract: Certain known and novel pyruvate derivatives are particularly active in restoring or preserving metabolic integrity in oxidatively competent cells that have been subjected to oxygen deprivation. These pyruvate-derived compounds include, but are not limited to oximes, amides, pyruvate analogues, modified pyruvate analogues, esters of pyruvate (e.g., polyol-pyruvate esters, pyruvate thioesters, glycerol-pyruvate esters and dihydroxyacetone-pyruvate esters). Such pyruvate derivatives (including single tautomers, single stereoisomers and mixtures of tautomers and/or stereoisomers, and the pharmaceutically acceptable salts thereof) are useful in the manufacture of pharmaceutical compositions for treating a number of conditions characterized by oxidative stress.Type: GrantFiled: May 3, 2002Date of Patent: May 31, 2005Assignee: Galileo Pharmaceuticals, Inc.Inventors: Bing Wang, Guy Miller, Satyanarayana Janagani
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Patent number: 6888005Abstract: A process for the preparation of 2-phenylbenzimidazole-5-sulphonic acid, characterized in that 3,4-diaminobenzenesulphonic acid is reacted at a pH between 4 and 7 in aqueous solution with 0.9 to 1.5 mol of benzaldehyde per mole of 3,4-diaminobenzenesulphonic acid and with 1.0 to 3.0 mol of SO2 per mole of 3,4-diaminobenzenesulphonic acid, or an agent which comprises 1.0 to 3.0 mol of SO2 per mole of 3.4-diaminobenzenesulphonic acid, is described.Type: GrantFiled: September 16, 2003Date of Patent: May 3, 2005Assignee: Bayer AktiengesellschaftInventors: Günter Rauchschwalbe, Herbert Emde, Wolfram Kissener, Klaus-Christian Paetz
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Patent number: 6869950Abstract: The present invention provides novel benzimidazole derivatives of the following formula (I) and salts thereof: wherein R1 represents a lower alkyl group or a lower alkyloxy-lower alkyl group; R2 represents a hydrogen atom, a halogen atom, an alkyl group having 1 to 8 carbon atoms, an aryl group, and such; R3 represents a lower alkyl group, a lower alkenyl group, an aryl group, a lower alkylaryl group, an aryl-lower alkenyl group, a halothienyl group, a lower alkylamino group, or an aryl-lower alkylamino group; A represents a benzene ring, a naphthalene ring, or a pyridine ring; and X represents a halogen atom. The derivatives and their salts have blood sugar level-depressing activity or PDE5-inhibiting activity, and are useful as pharmaceutical preparations.Type: GrantFiled: December 22, 1999Date of Patent: March 22, 2005Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Noritsugu Yamasaki, Takafumi Imoto, Takahiro Hiramura, Miho Kawauchi, Noriko Oku, Chikako Oku, Tomohito Oku, Hiroshi Kayakiri, Hitoshi Sawada, Teruo Oku
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Patent number: 6855714Abstract: The invention relates to novel benzimidazole derivatives with general formula I, whereby radicals R1, R2, R3, A, B and Y have the meanings that are indicated in the description and the claims, the use of these compounds for the production of a pharmaceutical agent for treating and for preventing diseases that are associated with microglia activation, as well as pharmaceutical preparations that contain these compounds.Type: GrantFiled: July 5, 2002Date of Patent: February 15, 2005Assignee: Schering AktiengesellschaftInventors: Thorsten Blume, Wolfgang Halfbrodt, Joachim Kuhnke, Ursula Moenning, Herbert Schneider, Bernd Elger
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Patent number: 6780992Abstract: The present invention relates to novel antidiabetic compounds, their tautomeric forms, their derivatives, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. This invention particularly relates to novel azolidinedione derivatives of the general formula (I), and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutical compositions containing them.Type: GrantFiled: December 26, 2001Date of Patent: August 24, 2004Assignees: Dr. Reddy's Laboratories Ltd., Dr. Reddy's Laboratories Inc.Inventors: Vidya Bhushan Lohray, Braj Bhushan Lohray, Rao Bheema Paraselli, Ranga Madhavan Gurram, Rajagopalan Ramanujam, Ranjan Chakrabarti, Sarma K.S. Pakala
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Publication number: 20040044055Abstract: The present invention relates to novel N-alkoxyalkyl-substituted benzimidazoles, to their preparation and to their use as agents against parasitic protozoa.Type: ApplicationFiled: April 3, 2003Publication date: March 4, 2004Inventors: Folker Lieb, Albrecht Marhold, Torsten Neugebauer, Gisela Greif
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Publication number: 20030232810Abstract: Described are heterocycle-substituted cyclohexylamines of formula (I), and their pharmaceutically acceptable salts thereof. The compounds of formula (I) are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, cerebral ischemia, cardiac arrest, stroke, and Parkinson's disease.Type: ApplicationFiled: December 3, 2002Publication date: December 18, 2003Inventors: Russell Joseph Deorazio, Sham Shridhar Nikam, Ian Leslie Scott, Brian Alan Sherer, Lawrence David Wise
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Patent number: 6603014Abstract: The use of compounds of the formula I in which R1 and R2 are identical or different, electron-withdrawing radicals chosen from the group consisting of cyano, alkyl- or arylcarbonyl, alkyloxy- or aryloxycarbonyl and optionally substituted aminocarbonyl, R3 is a hydrogen atom, a C1-C20-alkyl radical or a C3-C20-cycloalkyl radical or a radical of the formula —CH2—CH2—SO3—M+, where M+ is a cation, X is the divalent radical of oxygen, sulfur or the radical where R3 is as defined above, is the divalent radical of the formula II or III, which forms a fused system with the radical of the formula I where R4 can be bonded one or more times to the benzylidene ring I or naphthylidene ring II, and is hydrogen, alkyl, cycloalkyl, alkyloxy, cycloalkyloxy, alkoxycarbonyl, mono- or dialkylaminocarbonyl, alkylamino, dialkylamino, each having up to 20 carbon atoms, and also cyano, amino and SO3—M+, where M+ is a cation,Type: GrantFiled: January 23, 2002Date of Patent: August 5, 2003Assignee: BASF AktiengesellschaftInventors: Thorsten Habeck, Frank Prechtl, Thomas Wünsch, Horst Westenfelder
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Patent number: 6596751Abstract: The &agr;-substituted carboxylic acid derivatives having the formula (I): wherein R1 is an alkyl group, etc., R2 is a hydrogen atom, etc., R3 is a hydrogen atom, etc., A is ═CH-group, etc., B is an oxygen atom, etc., W1 is a C1-C8 alkylene group, W2 is a single bond or a C1-C8 alkylene group, X is a hydrogen atom, etc., Y is an oxygen atom, etc., and Z1 is an alkoxy group, etc., and pharmacologically acceptable salts, esters and amides thereof are useful for treatment and/or prevention of diabetes mellitus, impaired glucose tolerance, gestational diabetes mellitus, or the like. Some of the derivatives of the formula (I) are novel compounds.Type: GrantFiled: October 5, 2001Date of Patent: July 22, 2003Assignee: Sankyo Company LimitedInventors: Takashi Fujita, Kunio Wada, Minoru Oguchi, Hidehito Honma, Toshihiko Fujiwara, Haruo Iwabuchi
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Publication number: 20030119754Abstract: The present invention relates to novel benzimidazole compounds that have useful antiviral activity. More specifically, the invention encompasses benzimidazole compounds that inhibit membrane fusion associated events such as viral transmission, reduce viral load or otherwise treat viral infections. The invention also encompasses the use of benzimidazole compounds as inhibitors of membrane fusion associated events, such as viral transmission. In another embodiment, the invention encompasses processes for making benzimidazole compounds, methods of using the benzimidazole compounds and compositions comprising the benzimidazole compounds. Finally, the invention provides methods for treating, preventing or ameliorating symptoms associated with respiratory infection, particularly that caused by Respiratory Syncytial Virus utilizing the novel benzimidazole compounds of the invention.Type: ApplicationFiled: May 9, 2002Publication date: June 26, 2003Inventors: John William Lackey, Daniel S. Kinder, Nicolai A. Tvermoes
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Patent number: 6482859Abstract: The invention relates to novel pesticidally active compounds of the general formula I as well as possible isomers and mixtures of isomers thereof, wherein n is a number zero or one; and R1 is C1-C12alkyl that is unsubstituted or may be substituted by C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylsulfonyl, C3-C8cycloalkyl, cyano, C1C6alkoxycarbonyl, C3-C6alkenyloxycarbonyl or by C3-C6alkynyloxycarbonyl; C3-C8cycloalkyl; C2-C12alkenyl; C2-C12alkynyl; C1-C12haloalkyl: or a group NR11R12 wherein R11 and R12 are each independently of the other hydrogen or C1-C8alkyl, or together are tetra- or penta-methylene; R2 and R3 are each independently of the other hydrogen; C1-C8alkyl; C1-C8alkyl substituted by hydroxy, C1-C4alkoxy, mercapto or by C1-C4alkylthio; C3-C8alkenyl; C3-C8alkynyl; C3-C8cycloalkyl; C3-C8cycloalkyl-C1-C4alkyl; or the two groups R2 and R3 together with the carbon atom to which they are bonded form a three- to eight-membered ring; R4, R5, R6 and R7 are identical or different and are eaType: GrantFiled: February 4, 2000Date of Patent: November 19, 2002Assignee: Syngenta Crop Protection, Inc.Inventors: Martin Zeller, André Jeanguenat
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Patent number: 6465505Abstract: The present invention relates to benzimidazole derivatives of the formula (I), in which the phenyl moiety is substituted with lower alkyl in 2- and 6-position, which inhibit exogenously or endogenously stimulated gastric acid secretion and thus can be used in the prevention and treatment of gastrointestinal inflammatory diseases.Type: GrantFiled: July 17, 1997Date of Patent: October 15, 2002Assignee: AstraZeneca ABInventors: Kosrat Amin, Mikael Dahlström, Peter Nordberg, Ingemar Starke
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Patent number: 6465484Abstract: The present invention relates to compounds which inhibit tyrosine kinase enzymes, compositions which contain tyrosine kinase inhibiting compounds and methods of using tyrosine kinase inhibitors to treat tryrosine kinase-dependent diseases/conditions such as angiogenenesis, cancer, atherosclerosis, diabetic retinopathy or autoimmune diseases, in mammals.Type: GrantFiled: February 28, 2001Date of Patent: October 15, 2002Assignee: Merck & Co., Inc.Inventors: Mark T. Bilodeau, Randall W. Hungate, April M. Cunningham, Timothy J. Koester
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Publication number: 20020143024Abstract: Novel biphenyl sulfonamide compounds which are combined angiotensin and endothelin receptor antagonists are claimed along with methods of using such compounds in the treatment of conditions such as hypertension and other diseases, as well as pharmaceutical compositions containing such compounds.Type: ApplicationFiled: December 14, 2000Publication date: October 3, 2002Inventors: Natesan Murugesan, John E. Tellew, Jhon E. Macor, Zhengxiang Gu
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Patent number: 6444694Abstract: Disclosed herein are compounds of the formula: wherein R is phenyl or substituted phenyl; or R is furyl, pyridyl or quinolinyl; R1 and R2 are hydrogen, halogen, alkyl, alkoxy, nitro, carboxyl, alkoxy-carbonyl or aryloxycarbonyl; R3 is hydrogen, alkyl, aryl or arylalkyl; R4 and R5 are hydrogen or alkyl; or a pharmaceutically acceptable salt thereof, which are useful as inhibitors of smooth muscle cell proliferation.Type: GrantFiled: June 6, 1995Date of Patent: September 3, 2002Assignee: WyethInventors: Sie-Yearl Chai, Hassan M. Elokdah, Theodore S. Sulkowski
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Patent number: 6440401Abstract: Disclosed is a 2-phenyl-benzimidazolesulfonic acid according to the formula in which n is 0, 1 or 2 and m is 2 or 3, R1, R2, R3, R4 and R5, are each a radical such as H, C1-8-alkyl, C1-8-alkoxy, hydroxyl, sulfate, nitro, F, Cl, Br or I radicals, and R6 is a C1-8-alkyl or C1-8-alkoxy radical. This compound can be effectively used as a UV filter, and as part of a cosmetic formulation which comprise these compounds. A process for preparation of the compound is disclosed as well.Type: GrantFiled: November 21, 2001Date of Patent: August 27, 2002Assignee: Merck Patent Gesellschaft Mit Beschraenkter HaftungInventors: Ulrich Heywang, Michael Schwarz, Frank Pflücker
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Publication number: 20020107269Abstract: The invention relates to benzoxazoles and the use thereof to inhibit lysophosphatidic acid acyltransferase &bgr; (LPAAT-&bgr;) activity. The invention further relates to methods of treating cancer using said benzoxazoles. The invention also relates to methods for screening for LPAAT-&bgr; activity.Type: ApplicationFiled: October 31, 2001Publication date: August 8, 2002Applicant: CELL THERAPEUTICS, INC.Inventors: Lynn Bonham, J. Peter Klein, Robert E. Finney, David M. Hollenback, Scott A. Shaffer, Norina M. Tang, Thayer H. White, David W. Leung
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Patent number: 6410743Abstract: Tetrahydronaphatalene derivatives, and compositions comprising the compounds. The tetrahydronaphatalene derivates are useful in inhibiting a rise in intracellular calcium mediated by an influx through T-type calcium channels, and are thus useful for treatment of, for example, type 1 and type 2 diabetes and cardiovascular diseases associated with diabetes.Type: GrantFiled: March 27, 2001Date of Patent: June 25, 2002Assignees: Novo Nordisk A/S, South Alabama Medical Science FoundationInventors: Ming Li, John Bondo Hansen, Tina Moller Tagmose
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Patent number: 6387927Abstract: The invention relates to anti-tumour-effective compounds of formula (I), wherein the radicals have the meanings given in the description.Type: GrantFiled: June 1, 2001Date of Patent: May 14, 2002Assignee: Novatis AGInventors: Karl-Heinz Altmann, Guido Bold, Giorgio Caravatti, Andreas Flörsheimer
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Patent number: 6387938Abstract: This invention provides novel benzimidazole derivatives represented by the formula (I); a process for producing the same; a drug containing at least one of such compounds as its active ingredient, in particular, a drug for preventing and/or treating diseases exhibiting eosinophilia, bronchial asthma and allergic diseases; and an enhancer for IFN-&ggr; production, and in particular, an antitumor agent or an antiviral agent based on the action of enhancing the IFN-&ggr; production which exhibits excellent oral bioavailability.Type: GrantFiled: July 12, 2000Date of Patent: May 14, 2002Assignee: Mochida Pharmaceutical Co., Ltd.Inventors: Kiyoshi Mizuguchi, Nobuo Ohzawa, Yasuhiro Nakai, Kazuyuki Matsuura, Shuhei Ohnishi, Yutaka Kato, Tsutomu Satoh
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Patent number: 6376671Abstract: 2-Sulfamoylbenzoic acid derivatives of general formula (I): which have both an antagonistic effect on the leukotriene D4 receptor and an antagonistic effect on the thromboxane A2 receptor and salts thereof, pharmaceuticals, anti-allergic agents and leukotriene-thromboxane A2 antagonistic agents containing them as an active ingredient.Type: GrantFiled: April 27, 2001Date of Patent: April 23, 2002Assignee: Kaken Pharmaceutical Co., Ltd.Inventors: Yoshihiro Ichikawa, Tokiko Nishida, Jun Nakano, Mitsuru Watanuki, Masahiro Suda, Tsutomu Nakamura
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Patent number: 6365584Abstract: Arylsulphonamide-substituted benzimidazole derivatives of formula (I) having tryptase-inhibiting activity. Exemplary are: 1-Methyl-2-[2-(4-amidinophenyl)-ethyl]-5-[N-(2-diethylaminoethyl)-benzenesulphonylamino]-benzimidazole; 1-Methyl-2-[2-(4-amidinophenyl)-ethyl]-5-[N-(2-diethlylaminoethyl)-benzylsulfonylamino]-benzimidazole; and, 1-Methyl-2-[2-(4-amidinophenyl)-ethyl]-5-[N-(3-diethylaminopropyl)-benzenesulphonylamino]-benzimidazole.Type: GrantFiled: September 21, 2000Date of Patent: April 2, 2002Assignee: Boehringer Ingelheim Pharma KGInventors: Ralf Anderskewitz, Christine Braun, Hans Briem, Bernd Disse, Christoph Hoenke, Hans Michael Jennewein, Georg Speck
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Patent number: 6348482Abstract: Compounds, pharmaceutically acceptable salts, and compositions thereof of the general formula: wherein Ar is aryl and heteroaryl; R1, R2, R3, and R4 are hydrido, alkyl, cyano, heteroaryl, hydroxy, amino, acylamino, halo, alkoxy, aryloxy, carboxyamido, alkenyl, cycloalkyl, heterocyclyl, acyl, acyloxy, carboalkoxy, carboxy, thio, sulfinyl, sulfonyl and sulfoxy, R5, R6, R7, and R8 are hydrido and lower alkyl; and Het is a nitrogen-containing heterocyclic ring.Type: GrantFiled: May 5, 2000Date of Patent: February 19, 2002Assignees: Merck & Co., Inc., Cubist Pharmaceuticals, Inc.Inventors: Milton L. Hammond, Aaron H. Leeman, Milana Maletic, Gina M. Santorelli, Sherman T. Waddell, John Finn, Michael Morytko, Jason Hill, Dennis Keith
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Patent number: 6326369Abstract: A compound of the formula: wherein R1 and R2 each represents a lower alkyl, or R1 and R2 may be bonded together to form a ring; X represents a spacer of which the number of atoms constituting the principal chain is 1 to 15; Y represents an acyl, or a hydroxy, an amino or an aromatic group, each of which may be substituted; and ring A represents a 5- to 8-membered ring which may be further substituted apart from —X—Y, or a salt thereof is useful as a pharmaceutical composition for preventing or treating disease related to mitochondrial dysfunction.Type: GrantFiled: July 6, 1999Date of Patent: December 4, 2001Assignee: Takeda Chemicals Industries, Ltd.Inventors: Kaneyoshi Kato, Taiichi Ohra, Masaomi Miyamoto
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Patent number: 6316474Abstract: Benzimidazoles, substituted in the 2-position by substituted benzyl groups or heteroaryl groups are effective as NMDA NR2B antagonists and are useful for relieving pain.Type: GrantFiled: October 25, 2000Date of Patent: November 13, 2001Assignee: Merck & Co., Inc.Inventors: John A. McCauley, Cory R. Theberge, Nigel J. Liverton, David A. Claremon, Christopher F. Claiborne
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Patent number: 6291499Abstract: Novel 4-substituted cyclohexanes substituted in the 1-position with 2-benzimidazoles, 2-imidazopyridines, or 4-imidazoles either directly or through a C1-C4alkyl, cycloalkyl, hydroxyalkyl, alkoxy or aminoalkyl chain are effective as NMDA NR2B antagonists useful for relieving pain.Type: GrantFiled: October 25, 2000Date of Patent: September 18, 2001Assignee: Merck & Co., Inc.Inventors: Wayne Thompson, David A. Claremon, Peter M. Munson, John A. McCauley
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Patent number: 6288100Abstract: Disclosed herein are compounds of formula I or II: wherein R is alkyl phenyl or substituted phenyl; R2 is hydrogen, halogen, alkoxy or alkyl; R1 is hydrogen, alkyl, aryl, arylalkyl, or substituted benzyl; or a pharmaceutically acceptable salt thereof, which are useful as inhibitors of smooth muscle cell proliferation.Type: GrantFiled: June 6, 1995Date of Patent: September 11, 2001Assignee: American Home Products CorporationInventors: Hassan M. Elokdah, Sie-Yearl Chai, Theodore S. Sulkowski