Nitrogen Attached Directly Or Indirectly To The Hetero Ring By Acyclic Nonionic Bonding Patents (Class 549/419)
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Patent number: 7902376Abstract: A novel process is provided for the preparation of chiral trans-2,3-disubstituted 5-oxotetrahydropyrans of structural formula (I): wherein Ar is optionally substituted phenyl and P is a primary amine protecting group. These compounds are useful in the synthesis of dipeptidyl peptidase-IV inhibitors for the treatment of Type 2 diabetes. Also provided are useful intermediates obtained from the process.Type: GrantFiled: January 22, 2009Date of Patent: March 8, 2011Assignees: Merck Sharp & Dohme Corp., Banyu Pharmaceutical Co., Ltd.Inventors: Feng Xu, Mary M. Kim, Yoshinori Kohmura, Tricia Sladicka, Jonathan D. Rosen, Michael J. Zacuto
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Publication number: 20110052504Abstract: The present invention relates to a class of compounds and to diagnostic compositions containing such compounds where the compounds are iodine containing compounds.Type: ApplicationFiled: March 2, 2009Publication date: March 3, 2011Inventor: Hanno Priebe
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Publication number: 20110039925Abstract: The invention encompasses a novel class of cyclobutyl sulfone derivatives which inhibit the processing of APP by the putative ?-secretase while sparing Notch signaling pathway, and thus are useful in the treatment or prevention of Alzheimer's disease without the development of Notch inhibition mediated gastrointestinal issues. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: April 17, 2009Publication date: February 17, 2011Inventors: Richard W. Heidebrecht, Chaomin Li, Benito Munoz, Andrew Rosenau, Laura M. Surdi, Paul Tempest
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Patent number: 7825267Abstract: The present invention provides novel analogs of FR901464, as well as an improved methodology for preparing FR901464 and its analogs. These compounds display an anti-cancer activity and are candidates for therapies against a number of disease states associated with dysfunctional RNA splicing.Type: GrantFiled: September 8, 2007Date of Patent: November 2, 2010Assignee: University of Pittsburgh-of the Commonwealth System of Higher EducationInventors: Kazunori Koide, Brian J. Albert, Ananthapadmanabhan Sivaramakrishnan
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Patent number: 7820714Abstract: The invention relates to Siglec inhibitors that have an increased affinity for the receptor molecule. The Siglec inhibitors provided by the invention are preferably selective of a given Siglec molecule. The invention further relates to a method for producing Siglec inhibitors and to a method for increasing the binding selectivity for a given Siglec molecule. The invention also relates to pharmaceutical compositions that contain the Siglec inhibitors and to medical indications for the Siglec inhibitors.Type: GrantFiled: June 7, 2002Date of Patent: October 26, 2010Inventors: Sorge Kelm, Reinhard Brossmer
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Patent number: 7795457Abstract: Carbamate compounds having a structure represented by formula I (where R1, R2, R3, R4, R5 and R6 are as defined herein) are useful as anti-tumor agents.Type: GrantFiled: February 20, 2008Date of Patent: September 14, 2010Assignee: Kosan Biosciences IncorporatedInventors: Hong Fu, Yaoquan Liu
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Patent number: 7790900Abstract: An optically active nitro compound having two hydrogen atoms on its ?-carbon atom and having ?-asymmetric carbon atom can be produced by making ?,?-unsaturated nitroolefin having a hydrogen atom on its ?-carbon atom react with at least two organosilicon compounds having at least one silicon-hydrogen bond in the molecule in the presence of an asymmetric copper complex, or react with an organosilicon compound having at least one silicon-hydrogen bond in the molecule in the presence of an asymmetric copper complex and water.Type: GrantFiled: May 17, 2004Date of Patent: September 7, 2010Assignees: Sumitomo Chemical Company, LimitedInventor: Erick M. Carreira
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Patent number: 7763657Abstract: This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salt thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRRPV1) antagonist; and a pharmaceutical composition containing the same. The present invention provides a pharmaceutical composition for preventing or treating a disease such as pain, migraine, arthralgia, neuralgia, neuropathies, nerve injury, skin disorder, urinary bladder hypersensitiveness, irritable bowel syndrome, fecal urgency, a respiratory disorder, irritation of skin, eye or mucous membrane, stomach-duodenal ulcer, inflammatory diseases, ear disease, and heart disease.Type: GrantFiled: March 15, 2006Date of Patent: July 27, 2010Assignee: Amorepacific CorporationInventors: Hee-Doo Kim, Young-Ger Suh, Hyeung-Geun Park, Uh Taek Oh, Seol Rin Park, Joo Hyun Kim, Mi Jung Jang, Young-Ho Park, Song Seok Shin, Sun-Young Kim, Jin Kwan Kim, Yeon Su Jeong, Ki-Wha Lee, Jin Kyu Choi, Kyung Min Lim, Hyun Ju Koh, Joo Hyun Moh, Sung-Il Kim, Byoung Young Woo
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Publication number: 20100184999Abstract: Methods of performing cycloadditions are described that include (a) combining a first reactant and a second reactant in a hydrogen bonding solvent to form a reaction mixture; and (b) reacting the first reactant and the second reactant to form a cycloadduct. Methods of performing asymmetric catalytic reactions are also described that include (a) combining a first reactant, a second reactant, and a catalytic amount of a chiral hydrogen-bond donor in a solvent to form a reaction mixture; and (b) reacting the first reactant and the second reactant to form an enantiomeric excess of a reaction product. Reaction mixtures corresponding to these methods are also described.Type: ApplicationFiled: June 11, 2007Publication date: July 22, 2010Inventors: Viresh H. Rawal, Yong Huang, Aditya K. Unni, Avinash N. Thadani
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Patent number: 7737287Abstract: This invention relates to combinatorial libraries of potentially biologically active mainly monosaccharide compounds and to methods of preparing same. These compounds are variously functionalized, with a view to varying lipid solubility, size, function and other properties, with the particular aim of discovering a drug or drug-like compound, or compounds with useful properties. The invention provides intermediates, processes and synthetic strategies for the solution or solid phase synthesis of monosaccharides, variously functionalized about the sugar ring, including the addition of aromaticity and charge, and the placement of amino acid and peptide side chain units of isosteres thereof.Type: GrantFiled: March 28, 2003Date of Patent: June 15, 2010Assignee: Alchemia LimitedInventors: Wim Meutermans, Michael Leo West, Thanh Le Giang, George Adamson, Karl Schafer, Giovanni Abbenante
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Publication number: 20100022637Abstract: Small molecule screening via high-throughput screening (HTS) methods was employed to identify compounds useful for treating or preventing cancer (such as compounds that enable cells to overcome E6-oncoprotein-mediated drug resistance) or neurodegenerative disorders (such as Huntington's disease, HD). Compounds were identified that potentiate the lethality of anti-tumor agents as well as rescue a disease-state lethality. These compounds are acylated secondary amines referred to herein as indoxins and revertins.Type: ApplicationFiled: September 29, 2006Publication date: January 28, 2010Applicant: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORKInventors: Brent R. Stockwell, Inese Smukste
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Publication number: 20100021847Abstract: An oxime compound represented by the formula (I): wherein Y represents an unsubstituted or substituted n-valent C6-C14 aromatic hydrocarbon group, n represents an integer of 1 to 6, R1) represents a C1-C30 aliphatic hydrocarbon group etc., R2 represents a linear or branched chain C1-C20 aliphatic hydrocarbon group etc., W represents —CO—O— etc., Q1 and Q2 each independently represent a fluorine atom etc., Z represents a C1-C20 halogenated aliphatic hydrocarbon group etc, and the resist composition containing the same.Type: ApplicationFiled: July 21, 2009Publication date: January 28, 2010Applicant: SUMITOMO CHEMICAL COMPANY, LTD.Inventors: Tatsuro MASUYAMA, Kazuhiko HASHIMOTO, Takashi HIRAOKA, Ichiki TAKEMOTO
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Publication number: 20090318481Abstract: This application relates to a substituted hydroxyphenyl ketone compound of formula I, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof and its use in treating migraine. This application also relates to processes for preparing a compound of formula I, and intermediate compounds useful therein.Type: ApplicationFiled: August 28, 2009Publication date: December 24, 2009Inventors: Thomas Daniel AICHER, Guillermo S. CORTEZ, Todd Michael GROENDYKE, Albert KHILEVICH, James Allen KNOBELSDORF, Fredrik Pehr MARMSATER, Jeffrey Michael SCHKERYANTZ, Tony Pisal TANG
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Publication number: 20090281062Abstract: The invention relates to nitroso derivatives including carboxylic acid and phosphoric acid esters of hydroxy nitroso compounds that donate nitroxyl (HNO) under physiological conditions. The compounds and compositions of the invention are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure, ischemia/reperfusion injury and cancer.Type: ApplicationFiled: May 7, 2009Publication date: November 12, 2009Inventors: Lisa M. Frost, Stephen M. Courtney, Frederick A. Brookfield, Vincent J. Kalish
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Patent number: 7615635Abstract: Novel N-formyl hydroxylamine compounds and their derivatives are disclosed. These N-formyl hydroxylamine compounds inhibit peptidyl deformylase (PDF), an enzyme present in prokaryotes. The compounds are useful as antimicrobials and antibiotics. The compounds of the invention display selective inhibition of peptidyl deformylase versus other metalloproteinases such as MMPs. Methods of preparation and use of the compounds are also disclosed.Type: GrantFiled: May 22, 2006Date of Patent: November 10, 2009Assignees: Novartis AG, Vicuron Pharmaceuticals, Inc.Inventors: Kathryn Rene Bracken, Simon Bushell, Karl Dean, Charles Francavilla, Rakesh K. Jain, Kwangho Lee, Mohindra Seepersaud, Lei Shu, Arathi Sundaram, Zhengyu Yuan
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Patent number: 7595340Abstract: Selective dual serotonin and norepinephrine reuptake inhibitors are provided. These compounds have a lower side-effect profile and are useful in compositions and products for use in treatment of a variety of conditions including depression, fibromyalgia, anxiety, panic disorder, agoraphobia, post traumatic stress disorder, premenstrual dysphoric disorder, attention deficit disorder, obsessive compulsive disorder, social anxiety disorder, generalized anxiety disorder, autism, schizophrenia, obesity, anorexia nervosa, bulimia nervosa, Gilles de la Tourette Syndrome, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction, borderline personality disorder, fibromyalgia syndrome, diabetic neuropathic pain, chronic fatigue syndrome, pain, Shy Drager syndrome, Raynaud's syndrome, Parkinson's Disease, and epilepsy.Type: GrantFiled: July 13, 2006Date of Patent: September 29, 2009Assignee: WyethInventors: Syed M. Shah, Mahdi B. Fawzi, Eric C. Ehrnsperger, Panolil Raveendranath
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Patent number: 7566724Abstract: The compounds of the disclosure, for example, the compound represented by the formula: has excellent therapeutic and prophylactic effects against inflammatory bowel disease. Further, they are excellent in absorption and in vivo stability when administered orally in comparison with conventional compounds. That is, the compounds can be administered orally, and can have excellent therapeutic or prophylactic effect sustained for a longer period of time.Type: GrantFiled: December 22, 2005Date of Patent: July 28, 2009Assignee: Toray Industries, Inc.Inventors: Noriyuki Hirano, Hideki Inoue, Takashi Nagahara, Tomofumi Ohyama, Mie Kaino, Kenichi Hayashi, Sunao Hara, Ryutaro Suzuki
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Publication number: 20090187028Abstract: A novel process is provided for the preparation of chiral trans-2,3-disubstituted 5-oxotetrahydropyrans of structural formula (I): wherein Ar is optionally substituted phenyl and P is a primary amine protecting group. These compounds are useful in the synthesis of dipeptidyl peptidase-IV inhibitors for the treatment of Type 2 diabetes. Also provided are useful intermediates obtained from the process.Type: ApplicationFiled: January 22, 2009Publication date: July 23, 2009Inventors: Feng Xu, Mary M. Kim, Yoshinori Kohmura, Tricia Sladicka, Jonathan D. Rosen, Michael J. Zacuto
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Publication number: 20090137530Abstract: A novel amine compound represented by the following formula (I), which is superior in immunosuppressive action, rejection suppressive action and the like, and shows reduced side effects such as bradycardia and the like, or a pharmaceutically acceptable acid addition salt thereof, or hydrates thereof, or solvate, as well as a pharmaceutical composition containing this compound and a pharmaceutically acceptable carrier. wherein R is a hydrogen atom or P(?O)(OH)2, X is an oxygen atom or a sulfur atom, Y is CH2CH2 or CH?CH, R1 is cyano or alkyl having a carbon number of 1 to 4 and substituted by a halogen atom(s), R2 is alkyl having a carbon number of 1 to 4 and optionally substituted by a hydroxyl group(s) or a halogen atom(s), R3 and R4 may be the same or different and each is a hydrogen atom or alkyl having a carbon number of 1 to 4, and n is 5-8.Type: ApplicationFiled: December 15, 2006Publication date: May 28, 2009Applicant: Mitsubishi Tanabe Pharma CorporationInventors: Masatoshi Kiuchi, Kaoru Marukawa, Nobutaka Kobayashi, Kunio Sugahara
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Publication number: 20090130020Abstract: This invention relates to novel compounds F-18 radio-labeled amino-alcohols suitable for labeling or already labeled by 18F methods of preparing such a compound, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging by positron emission tomography (PET).Type: ApplicationFiled: September 11, 2008Publication date: May 21, 2009Inventors: Lutz Lehmann, Mathias Berndt, Dietmar Berndorff, Sabine Zitzmann-Kolbe, Ulrike Bauder-Wust, Martin Schafer, Uwe Haberkorn, Michael Eisenhut, Armin Runz
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Patent number: 7521568Abstract: Enantiopure substituted 4-deoxypentenosides (4-DPs) and related dihydropyrans (DHPs) are prepared from common carbohydrates via a novel process. The 4-DPs and related DHPs are amenable to a broad range of stereoselective transformations and are used as synthetic intermediates to prepare a variety of enantiopure tetrahydropyrans (THPs), including rare or exotic sugars and other complex THPs of commercial or medicinal value. In one embodiment of the instant invention, 4-DPs are converted to L-sugars in a novel process that offers distinct advantages over known synthetic methods.Type: GrantFiled: December 13, 2002Date of Patent: April 21, 2009Assignee: Purdue Research FoundationInventors: Alexander Wei, Fabien P. Boulineau
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Publication number: 20090068587Abstract: The present invention relates to a novel (meth)acrylamide compound represented by the general formula (1), a (co)polymer of the (meth)acrylamide compound, and a chemically amplified photosensitive resin composition composed of the polymer and a photoacid generator. In the formula, R1 represents a hydrogen atom or a methyl group; R2 represents an acid-decomposable group; and R3 to R6 independently represent a hydrogen atom, a halogen atom or an alkyl group having 1 to 4 carbon atoms.Type: ApplicationFiled: May 12, 2006Publication date: March 12, 2009Applicant: NEC CorporationInventors: Katsumi Maeda, Kaichirou Nakano
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Publication number: 20090062553Abstract: There is provided a process for the preparation of a compound of formula (7) or salts thereof: wherein R1 represents a hydrogen or a hydrocarbyl group, R2 represents a hydrogen or substituent group, R3 represents a hydrogen or a hydrocarbyl group, and X represents a hydrogen or substituent group which comprises a) cyanating a compound of formula (1): wherein Y represents a halo group, preferably CI or Br; P1 represents hydrogen or a protecting group, and W represents ?O or —OP2, in which P2 represents hydrogen or a protecting group, to give a compound of formula (2): b) reducing the compound of formula (2) to give a compound of formula (3): coupling the compound of formula (3) with a compound of formula (4): to give a compound of formula (5): when W represents —OP2, deprotecting and then oxidising the compound of formula (5) to give a compound of formula (6): and e) subjecting the compound of formula (5) when W represents ?O, or compound of formula (6) to ring-opening, and removal of any remaining protectingType: ApplicationFiled: August 14, 2008Publication date: March 5, 2009Applicant: NPIL PHARMACEUTICALS (UK) LIMITEDInventors: David John Moody, Jonathan William Wiffen
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Publication number: 20090053641Abstract: [PROBLEMS] Providing a charge control agent that has a negative charge providing property at a practical level, is colorless to light-colored and usable in color toners, produces static charges stable to environmental changes by electrifying the resin powder of a toner and the like, is excellent in storage stability and durability, and is highly safe, as well as a method of controlling the charge of resin powder using the charge control agent, and a toner. [MEANS OF SOLVING THE PROBLEMS] A charge control agent having a compound represented by the formula shown below as the active ingredient, as well as a method of controlling the charge of resin powder using the charge control agent, and a toner.Type: ApplicationFiled: March 22, 2006Publication date: February 26, 2009Inventors: Kazuyoshi Kuroda, Masashi Yasumatsu
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Publication number: 20080275230Abstract: An antimicrobial composition comprising: a complex of a polysaccharide covalently bonded with an antibiotic. A medical device having an antimicrobial composition comprising: a complex of an oxidized regenerated cellulose covalently bonded with gentamicin.Type: ApplicationFiled: May 3, 2007Publication date: November 6, 2008Inventors: Hongbo Liu, Xintian Ming
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Publication number: 20080214617Abstract: Carbamate compounds having a structure represented by formula I (where R1, R2, R3, R4, R5 and R6 are as defined herein) are useful as anti-tumor agents.Type: ApplicationFiled: February 20, 2008Publication date: September 4, 2008Inventors: Hong Fu, Yaoquan Liu
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Publication number: 20080188399Abstract: Monodisperse macromolecular conjugate compositions of a peptidic carrier irreversibly or reversibly conjugated with one or more effectors and one or more therapeutic agents, wherein at least one effector or therapeutic agent is attached to a pendant reactive group on said peptidic carrier via a water-soluble polymer. Monodispersity is obtained through the use of orthogonal and separate conjugation reactions.Type: ApplicationFiled: February 16, 2006Publication date: August 7, 2008Applicant: Ruthers, The State University of New JerseyInventors: Patrick J. Sinko, Stanley Stein, Simi Gunaseelan, Shahriar Pooyan, Li Wan, Xiaoping Zhang
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Patent number: 7402687Abstract: Compounds of formula I are described herein which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. or pharmaceutically acceptable salts thereof, wherein each of R1, R2, R3, R4, Rx, Ry, and n are as defined herein. Such compounds, and compositions thereof, are useful for treating a variety of central nervous system disorders such as schizophrenia.Type: GrantFiled: April 21, 2006Date of Patent: July 22, 2008Assignee: WyethInventors: Gary Paul Stack, Jianyao Wang, William Demaio, Ronald Jordan, John Chuck Lem Erve, Rasmy Elsayed Talaat, Matthew John Hoffmann
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Publication number: 20080167478Abstract: Novel 3,6-disubstituted pyrans, optionally with a further substituent at the 4-position, are monoamine reuptake inhibitors with activity profiles of anti-depressants.Type: ApplicationFiled: March 17, 2008Publication date: July 10, 2008Applicant: WAYNE STATE UNIVERSITYInventor: Aloke K. Dutta
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Publication number: 20080139505Abstract: The present invention provides compounds of formula (I): pharmaceutical compositions thereof, and methods of using the same, processes or preparing the same, and intermediates thereof.Type: ApplicationFiled: November 15, 2005Publication date: June 12, 2008Inventors: Thomas Daniel Aicher, Guillermo S. Cortez, Todd Michael Groendyke, Albert Khilevich, James Allen Knobelsdorf, Fredrik Pehr Marmsater, Jeffrey Michael Schkeryantz, Tony Pisal Tang, Nicholas Andrew Magnus
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Patent number: 7365215Abstract: The present invention relates to a process for preparing 4-aminotetrahydropyran compound and an acid salt thereof represented by the formula (1): wherein R represents a hydrogen atom or a hydrocarbon group, which comprises subjecting a 4-hydrazinotetrahydropyran compound or an acid salt thereof represented by the formula (2): wherein R has the same meaning as defined above, to decomposition reaction in the presence of at least one compound selected from Raney nickel, a noble metal catalyst and a metal oxide, and a synthetic intermediate thereof and a process for preparing the same.Type: GrantFiled: July 14, 2004Date of Patent: April 29, 2008Assignee: Ube Industries, Ltd.Inventors: Shigeyoshi Nishino, Kenji Hirotsu, Hidetaka Shima, Keiji Iwamoto, Takashi Harada, Shinobu Suzuki
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Patent number: 7361388Abstract: The invention relates to liquid-crystalline compounds of formula (I), wherein R11, X11, Z11, Z12, Z13, L11, L12, L13, L14, L15 and L16 have the meanings as cited in Claim 1, and to a method for the production thereof, their use in liquid-crystalline media, liquid-crystalline media containing at least one compound of formula (I), and to electro-optical displays containing a liquid-crystalline medium of this typeType: GrantFiled: May 24, 2004Date of Patent: April 22, 2008Assignee: Merck Patent GmbHInventors: Peer Kirsch, Eike Poetsch, Atsutaka Manabe
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Patent number: 7354936Abstract: The present invention relates to 2-(4-sulphonylphenyl)pyran-4-one derivatives of general formula processes for their preparation, pharmaceutical compositions containing them, and their medical uses.Type: GrantFiled: September 16, 2002Date of Patent: April 8, 2008Assignee: Almirall AGInventors: Maria Isabel Crespo Crespo, Juan Miguel Jimenez Mayorga, Josep Lluis Matallana Julia, Joan Feixas Gras
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Patent number: 7297802Abstract: An epoxytriazole derivative (V) useful as an intermediate for anti-fungal agents and an intermediate therefor having high quality can be produced economically and efficiently by the following industrial means. A compound of the following formula (I) is reacted with trimethyloxosulfonium salt and the like in the presence of a base to give compound (II), this compound is converted to compound (IV), and this compound is reacted with 1,2,4-triazole in the presence of a base. wherein Ar is a phenyl group optionally substituted by 1 to 3 halogen atom(s) or trifluoromethyl group, R is a hydrogen atom or lower alkyl group, and X is a leaving group.Type: GrantFiled: May 10, 2004Date of Patent: November 20, 2007Assignee: Sumitomo Chemical Company, LimitedInventors: Weiqi Wang, Tetsuya Ikemoto
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Patent number: 7259166Abstract: 2,3-Di-substituted N-heteroaromatic propionamides with said substitution at the 2-position being a substituted phenyl group and at the 3-position being a polar ring, said propionamides being glucokinase activators which increase insulin secretion in the treatment of type II diabetes.Type: GrantFiled: April 10, 2006Date of Patent: August 21, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Wendy Lea Corbett, Joseph Samuel Grimsby, Nancy-Ellen Haynes, Robert Francis Kester, Paige Erin Mahaney, Jagdish Kumar Racha, Ramakanth Sarabu, Ka Wang
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Patent number: 7205333Abstract: The invention relates to a multimeric compound or a pharmaceutically acceptable salt or derivative thereof which comprises three or more neuraminidase-binding groups attached to a spacer or linking group, in which the neuraminidase-binding group is a compound which binds to the active site of influenza virus neuraminidase, but is not cleaved by the neuraminidase. The invention also relates to processes for the preparation of the multimeric compound defined above, pharmaceutical compositions containing them or methods for the treatment and/or prophylaxis of a viral infection involving them.Type: GrantFiled: September 7, 2001Date of Patent: April 17, 2007Inventors: Wen-Yang Wu, Michael Dennis Dowle, Betty Jin, Simon John Fawcett Macdonald, Andrew McMurtrie Mason, Darryl McConnell, Keith Watson
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Patent number: 7189879Abstract: A new process for the production of 1-hydroxymethyl-1,3,5-triazapentane, trihydrochloride is described.Type: GrantFiled: May 24, 2005Date of Patent: March 13, 2007Assignee: Schering AGInventors: Johannes Platzek, Jan Huebner, Orlin Petrov
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Patent number: 7186709Abstract: The present invention provides novel dihydropyrancarboxamide compounds of formula (I): and collections of these compounds, and provides methods for the synthesis of these compounds; wherein R1–R6 are as defined herein. Additionally, the present invention provides pharmaceutical compositions and methods for treating disorders such as proliferative diseases, and cancer, to name a few.Type: GrantFiled: August 27, 2003Date of Patent: March 6, 2007Assignee: President and Fellows of Harvard CollegeInventors: Stuart L. Schreiber, Robert A. Stavenger, Timothy J. Mitchison, Zoltan Maliga
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Patent number: 7148240Abstract: The invention relates to benzofuran or benzothiophene derivatives of general formula: These compounds are of use as medicinal products, in particular in the treatment of pathological syndromes of the cardiovascular system.Type: GrantFiled: August 23, 2001Date of Patent: December 12, 2006Assignee: Sanofi-AventisInventors: Jean-Louis Assens, Claude Bernhart, Frédérique Cabanel-Haudricourt, Dino Nisato
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Patent number: 7129238Abstract: The invention is concerned with novel mandelic acid derivatives of formula (I) wherein R1 to R10, X and Y are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds inhibit the formation of coagulation factors Xa, IXa and thrombin induced by factor VIIa and tissue factor.Type: GrantFiled: November 21, 2003Date of Patent: October 31, 2006Assignee: Hoffmann-La Roche Inc.Inventors: David William Banner, Luca Claudio Gobbi, Katrin Groebke Zbinden, Ulrike Obst, Christoph Martin Stahl
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Patent number: 7091221Abstract: According to the present invention, there are provided a novel partial ester of a nitrogenous carboxylic acid ester with cellulose, the partial ester being useful as an antibacterial agent, a flame retardant, etc., and a simple and convenient process for preparing the same. Fibers made of said partial ester have washing-resistant antibacterial property and flame retardancy. There can be prepared the partial ester of a nitrogenous carboxylic acid ester with cellulose by contacting a nitrogenous carboxylic acid ester with cellulose and heat-treating the mixture.Type: GrantFiled: December 19, 2000Date of Patent: August 15, 2006Assignee: Ajinomoto Co., Inc.Inventors: Masahiko Kurauchi, Kiyonori Furuta, Hiroyuki Sato
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Patent number: 7045535Abstract: Certain cyclic compounds are presented as well as their use for inhibiting paramyxovirus neuraminidase.Type: GrantFiled: March 8, 2002Date of Patent: May 16, 2006Assignee: BioCryst Pharmaceuticals, Inc.Inventors: Pooran Chand, Yarlagadda S. Babu, R. Scott Rowland, Tsu-Hsing Lin
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Patent number: 7034015Abstract: The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compounds, and to the use of said compounds in the manufacture of pharmaceutical preparations.Type: GrantFiled: August 28, 2002Date of Patent: April 25, 2006Assignee: Leo Pharma A/SInventors: Erik Rytter Ottosen, Anne Marie Horneman, Xifu Liang
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Patent number: 6949538Abstract: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.Type: GrantFiled: July 17, 2003Date of Patent: September 27, 2005Assignees: Cytokinetics, Inc., Smithkline Beecham CorporationInventors: Andrew McDonald, Gustave Bergnes, David J. Morgans, Jr., Dashyant Dhanak, Steven David Knight
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Patent number: 6905786Abstract: A compound represented by the following formula (I): wherein R1, R2 and R3each represents an aryl group, a heterocyclic group or an aliphatic hydrocarbon group, provided that at least one of R1, R2 and R3 represents an aryl group or a heterocyclic group and at least one of the aryl group and heterocyclic group contains a group represented by formula (II), R1, R2 and R3 may be linked to each other to form a ring, wherein R4, R5 and R6, each represents a hydrogen atom or a substituent; X1 represents an oxygen atom, a sulfur atom, N—RX1 or CRX2RX3; RX1, RX2,RX3 each represents a hydrogen atom or a substituent; R4, R5, R6 and X1 may be linked to each other to form a ring; Y represents an oxygen atom, a sulfur atom, or N—RY1; and RY1 represents a hydrogen atom or a substituent.Type: GrantFiled: December 3, 2002Date of Patent: June 14, 2005Assignee: Fuji Photo Film., Ltd.Inventor: Kazumi Nii
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Patent number: 6906085Abstract: The present invention relates compounds of the formula (I): wherein R1, R2, R3, R4, R5, R6, R7 and R8 represent a variety of substituents; and pharmaceutically acceptable salts thereof. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.Type: GrantFiled: January 16, 2002Date of Patent: June 14, 2005Assignee: Merck Sharp & Dohme Ltd.Inventors: Jose Luis Castro Pineiro, Piotr Antoni Raubo, Christopher John Swain
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Patent number: 6852717Abstract: Disclosed are compounds useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are processes of making such compounds.Type: GrantFiled: May 10, 2002Date of Patent: February 8, 2005Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Pier Francesco Cirillo, Daniel R. Goldberg, Abdelhakim Hammach, Neil Moss, John Robinson Regan
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Patent number: 6852866Abstract: Disclosed is an invention concerning triazolyloligosaccharides, oligosaccharides wherein the bonding between the saccharide groups is via a triazole group and methods for their preparation.Type: GrantFiled: August 15, 2003Date of Patent: February 8, 2005Assignee: E. I. du Pont de Nemours and CompanyInventor: Subramaniam Sabesan
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Patent number: 6849660Abstract: Provided are antibacterial compounds having Formula I: In such compositions, X is O or S; Y is CH2; n is 0 or 1. One of R1 and R1? is —C(O)NR5R5?, —C(O)—Q—NR5R5?, —CH2NR5R5? or —S(O)2NR5R5? and the other is H or R3. One of R2 and R2? is —NHC(O)R6 or —NHS(O)2R6 and the other is H or R4. Q is an amino acid or peptide. R3 is H, halogen, —NR5R5? or —NHC(O)R6; and R4 is selected from the group consisting of H, halogen, hydroxyl, amino, carboxyl, alkyl, alkenyl and alkynyl. R5 is selected from the group consisting of H, alkyl, alkenyl or alkynyl optionally substituted with halogen, OH, amino, amidinyl, guanidinyl, urea, alkyl, carboxyl, oxo, carboxamide; R5? is H or R5 and R5? together form a 5-16 member heterocycle optionally substituted with halogen, OH, amino, alkyl, carboxyl, carbonyl or carboxamide.Type: GrantFiled: August 1, 2000Date of Patent: February 1, 2005Assignee: ISIS Pharmaceuticals, Inc.Inventors: Elizabeth Jefferson, Eric Swayze
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Publication number: 20040116400Abstract: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.Type: ApplicationFiled: July 17, 2003Publication date: June 17, 2004Applicants: CYTOKINETICS, INC., SMITHKLINE BEECHAM CORPORATIONInventors: Andrew McDonald, Gustave Bergnes, David J. Morgans, Dashyant Dhanak, Steven David Knight