Nitrogen Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/304)
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Publication number: 20100035924Abstract: This invention relates to novel 4-amino-pyridine derivative useful as modulators of small-conductance calcium-activated potassium channels (SK channels). In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.Type: ApplicationFiled: November 13, 2007Publication date: February 11, 2010Applicant: NeuroSearch A/SInventors: Ulrik Svane Sørensen, Birgitte L. Eriksen, Lene Teuber, Dan Peters, Dorte Strøbæk, Tina Holm Johansen, Palle Christophersen
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Patent number: 7659272Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.Type: GrantFiled: October 16, 2007Date of Patent: February 9, 2010Assignee: Millennium Pharmaceuticals, Inc.Inventors: Paul Fleming, Geraldine C. B. Harriman, Zhan Shi, Chen Shaowu
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Publication number: 20090326229Abstract: To provide methods for preparing alpha-carboline derivatives in few steps, as well as conveniently and industrially advantageously.Type: ApplicationFiled: August 2, 2007Publication date: December 31, 2009Applicant: Takeda Phamaceutical Company LimitedInventors: Masahiro Mizuno, Hideya Mizufune, Misayo Sera, Masahiro Mineno, Tsuyoshi Ueda
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Patent number: 7632951Abstract: Novel biphenyl derivatives of the general formula (I) in which R1, R1?, R1?, R2, R2?, R3 and n are as defined in claim 1, their stereoisomers and their physiologically acceptable salts or solvates are novel integrin inhibitors which preferentially inhibit the ?v?6 integrin receptor. The novel compounds can be used, in particular, as medicaments.Type: GrantFiled: February 21, 2002Date of Patent: December 15, 2009Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Oliver Schadt, Alfred Jonczyk, Wolfgang Staehle, Simon Goodman
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Patent number: 7629337Abstract: Heterocyclic compounds that bind chemokine receptors and inhibit the binding of their natural ligands are disclosed. The invention compounds are protective against infection by HIV and exert effects characteristic of antagonists to the CXCR4 receptor.Type: GrantFiled: July 27, 2006Date of Patent: December 8, 2009Assignee: Genzyme CorporationInventors: Gary J. Bridger, Renato Skerlj, Al Kaller, Curtis Harwig, David Bogucki, Trevor R. Wilson, Jason Crawford, Ernest J. McEachern, Bem Atsma, Siqiao Nan, Yuanxi Zhou, Dominique Schols
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Publication number: 20090291978Abstract: Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers, wherein R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxyesterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid; Y is a bond, C(?O)—, —S(?O)2—, —C(—O)O—, —C(O)NR3—, —C(?S)—NR3, —C(?NH)NR3 or —S(?O)2NR3— wherein R3 is hydrogen or optionally substituted C1-C6 alkyl; L is a divalent radical of formula -(Alk1)m(O)n(Alk2)p— wherein m, n and p are independently 0 or 1, Q is (i) an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic radical having 5-13 ring members, or (ii), in the case where both m and p are 0, a divalent radical of formula —X2-Q1- or -Q1-X2— wherein X2 is —O—, S— or NRA— wherein RA is hydrogen or optionally substituted C1-C3 alkyl, and Q1 is an optionally substituted divalent mono- or bicyclic carbocyclic or hetero-cyclic rType: ApplicationFiled: May 4, 2006Publication date: November 26, 2009Applicant: CHROMA THERAPEUTICS LTD.Inventors: Alan Hornsby Davidson, Sanjay Ratilal Patel, Francesca Ann Mazzei, Stephen John Davies, Alan Hastings Drummond, David Festus Moffat, Kenneth William John Baker, Alistair David Graham Donald
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Patent number: 7622486Abstract: The present invention provides new heterocyclic compounds, particularly substituted pyridines, methods and compositions for making and using these heterocyclic compounds, and methods for treating a variety of diseases and disease states, including atherosclerosis, arthritis, restenosis, diabetic nephropathy, or dyslipidemia, or disease states mediated by the low expression of Perlecan.Type: GrantFiled: September 23, 2005Date of Patent: November 24, 2009Assignee: Reddy US Therapeutics, Inc.Inventors: Manojit Pal, Christopher W. Alexander, Ish Khanna, Javed Iqbal, Ram Pillarisetti, Santanu Maitra, Gayla W. Roberts, Lavanya Sagi, Chintakunta Vamsee Krishna, Jennepalli Sreenu
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Patent number: 7595332Abstract: The present invention relates to compounds of formula (I) that are novel VR1 antagonists useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence, or bladder overactivity.Type: GrantFiled: January 19, 2006Date of Patent: September 29, 2009Assignee: Abbott LaboratoriesInventors: Chih-Hung Lee, John R. Koenig, Brian S. Brown
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Patent number: 7595321Abstract: The present invention relates to new compounds of formula (I) wherein Z is N; Y is CONR5, NR5CO, SO2NR5, NR5SO2, CH2NR5, NR5, NR5CONR5, CH2CO, CO, O or CH2O; X is CH or N; P is phenyl or a 5 or 6 membered heteroaromatic ring containing one or more heteroatoms selected from N, O or S and said phenyl ring or 5 or 6 membered heteroaromatic ring may optionally be fused with a 5 or 6 membered saturated, partially saturated or unsaturated ring containing one or more atoms selected from C, N, O or S; Q is C1-6alkyl, C2-6alkenyl or C2-6alkynyl, a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy, such as provide compounds having a selective inhibiting effect at GSK3.Type: GrantFiled: December 15, 2003Date of Patent: September 29, 2009Assignee: AstraZeneca ABInventors: Stefan Berg, Sven Hellberg
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Publication number: 20090215828Abstract: Substituted indole derivatives, processes for the preparation thereof, medicinal products and pharmaceutical compositions containing these compounds and the use of substituted indole derivatives to treat pain and other conditions and for other medical purposes.Type: ApplicationFiled: February 19, 2009Publication date: August 27, 2009Applicant: GRUNENTHAL GMBHInventors: Stefan Schunk, Stefan Oberborsch, Werner Englberger, Bernd Sunderman
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Publication number: 20090216015Abstract: The present invention relates to novel base stable ionic liquids and uses thereof as solvents in chemical reactions, especially base catalysed chemical reactions and reactions comprising the use of strong basis.Type: ApplicationFiled: January 4, 2006Publication date: August 27, 2009Applicant: The Queen's University of BelfastInventors: Martyn J. Earle, Ute Frohlich, Susanne Huq, Suhas Katdare, Rafal Marcin Lukasik, Ewa Bogel, Natalia Vladimirovna Plechkova, Kenneth Richard Seddon
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Patent number: 7576098Abstract: The present invention relates generally to compounds that inhibit serine proteases. In particular it is directed to novel heterocyclic compounds, or a stereoisomer or pharmaceutically acceptable salt, solvate, or prodrug form thereof, which are useful as selective inhibitors of serine protease enzymes of the coagulation cascade; for example thrombin, factor VIIa, factor Xa, factor XIa, factor IXa, and/or plasma kallikrein. In particular, it relates to compounds that are factor VIIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of using the same.Type: GrantFiled: December 7, 2005Date of Patent: August 18, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Peter W. Glunz, Nicolas Wurtz, Xuhong Cheng
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Patent number: 7572817Abstract: The present invention concerns compounds of formula (I), and pharmaceutically acceptable salts or solvates thereof, or solvates of such salts, which compounds inhibit carboxypeptidase U and thus can be used in the prevention and treatment of diseases where inhibition of carboxypeptidase U is beneficial. In further aspects, the invention relates to compounds of the invention for use in therapy; to processes for preparation of such new compounds; to pharmaceutical compositions containing at least one compound of the invention, or a pharmaceutically acceptable salt or solvate thereof, as active ingredient; and to the use of the active compounds in the manufacture of medicaments for the medical use indicated above.Type: GrantFiled: June 10, 2003Date of Patent: August 11, 2009Assignee: AstraZeneca ABInventor: Magnus Polla
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Publication number: 20090163515Abstract: The present invention relates to a compound and a group of compounds which are inhibitors of Rho kinase (ROK, ROCK). In addition, the invention relates to methods of treatment and use of the compounds in the manufacture of a medicament for application to a number of therapeutic indications including cardiovascular disease (coronary vasospasm, hypertensive disease, arteriosclerosis), stroke, cancer, erectile dysfunction, asthma, osteoporosis, glaucoma and AIDS. The compounds can be used in screening programmes against protein kinases. The invention also provides methods for making compounds and libraries that include these compounds.Type: ApplicationFiled: July 1, 2004Publication date: June 25, 2009Inventors: Veronique Birault, C. John Harris
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Patent number: 7550481Abstract: The present invention is directed to phenylamide and pyridylamide derivative compounds of which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.Type: GrantFiled: December 15, 2004Date of Patent: June 23, 2009Assignee: Merck & Co., Inc.Inventors: James C. Barrow, Craig A. Coburn, Philippe G. Nantermet, Harold G. Selnick, Shawn J. Stachel, Matthew G. Stanton, Shaun R. Stauffer, Linghang Zhuang, Jennifer R. Davis
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Patent number: 7528159Abstract: Compounds of formula (I): as well as pharmaceutically acceptable salts and esters thereof used in the form of pharmaceutical compositions.Type: GrantFiled: July 26, 2005Date of Patent: May 5, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Kurt Amrein, Daniel Hunziker, Bernd Kuhn, Alexander Mayweg, Werner Neidhart
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Publication number: 20090105291Abstract: Phenylalanine enamide derivatives of formula (1) are described: wherein R1 is a group Ar1 L2Ar2Alk- in which: Ar1 is an optionally substituted aromatic or heteroaromatic group; L2 is a covalent bond or a linker atom or group; Ar2 is an optionally substituted arylene or heteroarylene group; and Alk is a chain —CH2—CH(R)—, —CH?C(R)— or in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; X is an —O— or —S— atom or —N(R2)— group in which: Rx, Ry and Rz which may be the same or different is each a hydrogen atom or an optional substituent; or Rz is an atom or group as previously defined and Rx and Ry are joined together to form an optionally substituted spiro linked cycloaliphatic or heterocycloaliphatic group; and the salts, solvates, hydrates and N-oxides thereof.Type: ApplicationFiled: December 3, 2008Publication date: April 23, 2009Applicant: Rigel Pharmaceuticals, Inc.Inventors: Stephen Brand, Stuart Bailey, Julien A. Brown, James A. Johnson, John R. Porter, John C. Head
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Publication number: 20090093479Abstract: The present invention is in the area of novel compounds and salts thereof, their syntheses, and their use as anti-cancer agents. The compounds include compounds of Formula I: and solvates, hydrates and pharmaceutically-acceptable salts thereof, wherein A1 is N or CR1; A3 is N or CR3; A5 is N or CR5; R1, R3-R6 and L are defined in the specification; n is 0 or 1; and X is an optionally-substituted aryl group having 6-10 carbons in the ring portion, an optionally-substituted 6-membered heteroaryl group having 1-3 nitrogen atoms in the ring portion, an optionally-substituted 5-membered heteroaryl group having 0-4 nitrogen atoms in the ring portion and optionally having 1 sulfur atom or 1 oxygen atom in the ring portion, or an optionally-substituted heteroaryl group in which a 6-membered ring is fused either to a 5-membered ring or to a 6-membered ring, wherein in each case 1, 2, 3 or 4 ring atoms are heteroatoms independently selected from nitrogen, oxygen and sulfur.Type: ApplicationFiled: December 17, 2008Publication date: April 9, 2009Applicant: LOCUS PHARMACEUTICALS, INC.Inventors: Martha KELLY, Younghee LEE, Bin LIU, Ted FUJIMOTO, Joel FREUNDLICH, Bruce D. DORSEY, Gary A. FLYNN, Arifa HUSAIN
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Patent number: 7514564Abstract: Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: May 2, 2006Date of Patent: April 7, 2009Assignee: Amgen Inc.Inventors: Guoqing Chen, Jeffrey Adams, Jean Bemis, Lucian Di Pietro, Celia Dominguez, Daniel Elbaum, Julie Germain, Qi Huang, Joseph L. Kim, Xiaohu Ouyang, Vinod F. Patel, Leon M. Smith, Andrew Tasker, Ning Xi, Shimin Xu, Chester Chenguang Yuan, Michael Croghan, Tae-Seong Kim
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Patent number: 7507830Abstract: Methods are provided for the construction of unsymmetrical biaryl compounds and alkylated aromatic compounds from arylnitriles using a nickel or palladium catalyzed coupling in which the catalyst has at least one phosphine or phosphite ligand.Type: GrantFiled: September 23, 2004Date of Patent: March 24, 2009Assignee: Pharmacore, Inc.Inventor: Joseph A. Miller
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Publication number: 20090075823Abstract: The present invention relates to an improved process for the synthesis and purification of 3-chloro-N-(3-chloro-5-tri-fluoromethyl-2-pyridyl)-a,a,a-trifluoro-2,6-dinitro-p-toluidine (fluazinam) and other pyridinamines, which implements methyl isobutyl ketone (MIBK) as the reaction solvent. The process of the invention overcomes the drawbacks of prior art methods, by reducing the side reactions such as hydrolysis, eliminating the need for difficult and labor-intensive purification methods, and providing pure products in higher yields. The present invention relates to novel crystalline polymorphic forms fluazinam, and to mixtures of the polymorphs. The present invention also provides methods for preparing the novel polymorphs, as well as pharmaceutical compositions comprising same, and methods of using the polymorphs as pesticidal agents for combating noxious living organisms on agricultural and horticultural crops.Type: ApplicationFiled: November 23, 2006Publication date: March 19, 2009Inventors: Shlomi Cohen, Sharona Zamir
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Publication number: 20090075968Abstract: The present invention relates to a compound of formula or a pharmaceutically acceptable salt thereof, wherein the variables are as defined.Type: ApplicationFiled: December 27, 2006Publication date: March 19, 2009Inventors: Junichi Sakaki, Masashi Kishida, Naoko Matsuura, Ichiro Umemura, Eiji Kawahara, Ken Yamada, Kazuhide Konishi, Yuki Iwaki, Hidetomo Imase, Takahiro Miyake
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Publication number: 20090062507Abstract: A hydrazone compound represented by a General Formula (1) below, a hydrazone compound for forming a metal complex, which is represented by the General Formula (1) below and forms a metal complex by coordination to at least one metal species, a ligand for forming a metal complex including the hydrazone compound, and a monomer for manufacturing a polymer compound including the hydrazone compound: wherein, Py represents a 2-pyridyl group, a 3-pyridyl group, or a 4-pyridyl group.Type: ApplicationFiled: August 29, 2008Publication date: March 5, 2009Applicants: TOYOTA JIDOSHA KABUSHIKI KAISHA, IHARA CHEMICAL INDUSTRY CO., LTD.Inventors: Haruyuki NAKANISHI, Shinichi Matsumoto, Hidekazu Arikawa, Hironobu Kumagai
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Publication number: 20090054448Abstract: The present invention relates to compounds of formula (I): or pharmaceutically acceptable salts or stereoisomers thereof. The compounds of the present invention are inhibitors of histone deacetylase (HDAC) and are useful for treating cellular proliferative diseases, including cancer. Further, the compounds of the present invention are useful for treating neurodegenerative diseases, schizophrenia and stroke among other diseases.Type: ApplicationFiled: September 5, 2006Publication date: February 26, 2009Inventor: Philip Jones
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Patent number: 7482341Abstract: Compounds of formula as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R6 have the significance given in claim 1 can be used in the form of pharmaceutical compositions.Type: GrantFiled: September 29, 2005Date of Patent: January 27, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Kurt Amrein, Daniel Hunziker, Bernd Kuhn, Alexander Mayweg, Werner Neidhart
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Patent number: 7476452Abstract: The present invention is generally directed to electroluminescent Ir(III) compounds, the substituted 2-phenylpyridines that are used to make the Ir(III) compounds, and devices that are made with the Ir(III) compounds.Type: GrantFiled: February 6, 2004Date of Patent: January 13, 2009Assignee: E. I. du Pont de Nemours and CompanyInventors: Kerwin D. Dobbs, Norman Herron, Viacheslav A. Petrov
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Patent number: 7476727Abstract: The present invention provides a method for the measurement of an analyte in biological samples whereby an uncompetitive inhibitor is coupled to a ligand and utilized in a homogeneous assay. The analyte can be a drug or drug derivative, hormone, polypeptide, or oligonucleotide. The present invention also provides novel compounds, assay reagents and packaged kits useful for performing such measurements.Type: GrantFiled: February 9, 2007Date of Patent: January 13, 2009Assignee: Roche Diagnostics Operations, Inc.Inventors: Mitali Ghoshal, Gerald Sigler, Raymond A. Hui, Ronald Hawley, Eva Hoess, Erasmus J. Huber, John W. Patterson, Salvatore J. Salamone, Allan Dorn
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Patent number: 7468382Abstract: Disclosed are novel compounds of formula (I): wherein R1, R2 and R3 are as defined herein, which are useful as inhibitors of PKC-theta and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC-theta, including immunological disorders and type II diabetes. This invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: GrantFiled: March 27, 2006Date of Patent: December 23, 2008Assignee: Boehringer Ingelheim International GmbHInventors: Steven Richard Brunette, Jin Mi Kim, Rene′ Marc Lemieux, Matt Aaron Tschantz
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Patent number: 7459468Abstract: Aryl sulfonic pyridoxine compounds with antiplatelet aggregation characteristics for the treatment of cardiovascular and cardiovascular related disease, are described. The methods are directed to administering pharmaceutical compositions comprising aryl sulfonic pyridoxines.Type: GrantFiled: October 28, 2004Date of Patent: December 2, 2008Assignee: Medicure International, Inc.Inventors: Wasimul Haque, James Diakur
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Publication number: 20080280868Abstract: The present invention relates to novel pyridine derivatives such as compounds of the formula (I): and the use of such compounds or pharmaceutical compositions thereof in the treatment of diseases, particularly pain, which are mediated by the activity of the cannabinoid 2 receptor.Type: ApplicationFiled: February 22, 2005Publication date: November 13, 2008Inventors: Andrew John Eatherton, Gerard Martin Paul Giblin, William Leonard Mitchell, Alan Naylor
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Patent number: 7446117Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever and inflammation of a variety of conditions and diseases.Type: GrantFiled: September 12, 2003Date of Patent: November 4, 2008Assignee: Glaxo Group LimitedInventors: Paul Beswick, Neil Pegg, Martin Swarbrick, John Skidmore, Sandeep Modi
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Patent number: 7435815Abstract: The invention relates to novel sulfonylamino-acetic acid derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of such compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as orexin receptor antagonists.Type: GrantFiled: May 31, 2007Date of Patent: October 14, 2008Assignee: Actelion Pharmaceuticals Ltd.Inventors: Hamed Aissaoui, Martine Clozel, Walter Fischli, Ralf Koberstein, Thierry Sifferlen, Thomas Weller
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Publication number: 20080234488Abstract: The subject of the present invention is to provide a method for deuteration, which can obtain a compound having an aromatic ring and/or a heterocyclic ring at an improved deuteration ratio. The present invention relates to a method for deuteration of a compound having an aromatic ring and/or a heterocyclic ring, comprising reacting the compound having an aromatic ring and/or a heterocyclic ring with a heavy hydrogen source in the presence of an activated mixed catalyst of not less than two kinds of catalysts selected from among a palladium catalyst, a platinum catalyst, a rhodium catalyst, an iridium catalyst, a ruthenium catalyst, a nickel catalyst and a cobalt catalyst.Type: ApplicationFiled: December 21, 2004Publication date: September 25, 2008Applicant: WAKO PURE CHEMICAL INDUSTRIES, LTD.Inventors: Nobuhiro Ito, Tsuneaki Maesawa, Kazushige Muto, Kosaku Hirota, Hironao Sajiki
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Publication number: 20080221171Abstract: The invention relates to novel substituted 3-phenylamino-5-(3-aminophenyl)pyridines and corresponding pyrazines of formula (I), wherein A is CH, C-lower alkyl or N, R1 represents C(?O)R9, S(?O)2R10, P(?O)(OR11)2, optionally substituted phenyl or optionally substituted heteroaryl, and the other substituents have the meaning described in the specification, processes for the preparation thereof, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of neoplastic diseases and autoimmune diseases, and a method for the treatment of such diseases.Type: ApplicationFiled: September 5, 2005Publication date: September 11, 2008Applicant: BASILEA PHARMACEUTICA AGInventors: Martin Eberle, Felix Bachmann, Alessandro Strebel, Subho Roy, Goutam Saha, Godhuli Nandi
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Publication number: 20080220286Abstract: The present invention relates to a dinaphthyl ethylene derivative of formula (I), a process for preparing it, a film prepared from it useful in the manufacure of an organic light emitting device (OLED), an OLED including the film, and the use of the dinaphthyl ethylene derivative in the manufacture of an OLED. Wherein R1 to R16 are defined as in the specification.Type: ApplicationFiled: January 30, 2008Publication date: September 11, 2008Applicants: Tsinghua University, Beijing Visionox Technology Co., LTDInventors: Yong Qiu, Han Chen, Yinkui Li
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Patent number: 7414064Abstract: Compounds of formula wherein A1, A2 and A3 are each independently of the others a bond or a C1-C6alkylene bridge; A4 is a C1-C6alkylene bridge; D is CH or N; W is, for example, O, NR7 or S; T is, for example, a bond, O, NH or NR7; Q is O, NR7, S, SO or SO2; Y is O, NR7, S, SO or SO2; X1 and X2 are each independently of the other fluorine, chlorine or bromine; R1, R2 and R3 are, for example, H, halogen, CN, nitro, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkylcarbonyl or C2-C6alkenyl; R4 is, for example, H, halogen, CN, nitro or C1-C6alkyl; R5 and R6 are, for example, H, CN, OH, C1-C6alkyl, C3-C8cycloalkyl, C3-C8cycloalkyl-C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy or C1-C6haloalkoxy; R7 is H, C1-C6alkyl, C1-C6alkoxyalkyl or C1-C6alkylcarbonyl; k, when D is nitrogen, is 1, 2 or 3; or, when D is CH, is 1, 2, 3 or 4; and m is 1 or 2; and, where applicable, their possible E/Z isomers, E/Z isomeric mixtures and/or tautomers, in each case in free form or in salt form, a process for the preparation of those compounds andType: GrantFiled: February 15, 2007Date of Patent: August 19, 2008Assignee: Syngenta Crop Protection, Inc.Inventors: Werner Zambach, Peter Renold, Arthur Steiger, Stephan Trah, Roger Graham Hall
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Patent number: 7410986Abstract: 4-aryl pyrimidine compounds of general formula and salts thereof: wherein X is CH or N; R1 is hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, etc.; R2 is hydrogen or hydroxy; R3 is hydrogen, C1-6 alkyl, etc.; R4 is hydrogen, hydroxy, halogen, amino, etc.; R5 is hydroxy, amino, carboxy, etc.; R6 is hydrogen, carbamoyl, cyano, carboxy, C1-6 alkoxycarbonyl, etc. and R7 is amino or C1-6 alkanoylamino. The compounds (I) or the salts thereof have an excellent anti-inflammatory activity and the like.Type: GrantFiled: November 19, 2001Date of Patent: August 12, 2008Assignee: Bayer AktiengesellschaftInventors: Toshiki Murata, Sachiko Sasaki, Takashi Yoshino, Yuka Ikegami, Tsutomu Masuda, Mitsuyuki Shimada, Takuya Shintani, Makoto Shimazaki, Timothy B. Lowinger, Karl B. Ziegelbauer, Kinji Fuchikami, Masaomi Umeda, Hiroshi Komura, Nagahiro Yoshida
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Publication number: 20080188490Abstract: The invention provides compounds of formula (I) wherein the substituents are as defined in the specification, to processes for their preparation and corresponding intermediates, and their use as pharmaceuticals.Type: ApplicationFiled: April 24, 2006Publication date: August 7, 2008Inventors: Ralf Glatthar, Thomas J. Troxler
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Patent number: 7399775Abstract: Provided are novel compounds having an inhibitory activity against production or secretion of ?-amyloid protein. They embrace compounds represented by the following formula (1): and capable of being replaced with a variety of substituents; and salts thereof, and solvates of any one of them.Type: GrantFiled: December 27, 2002Date of Patent: July 15, 2008Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Takanori Yasukouchi, Masayuki Ito, Hideki Kubota, Satoru Miyauchi, Masanori Saito
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Publication number: 20080161576Abstract: Disclosed herein is a method comprising: (a) adding an aqueous solution comprising a quaternary ammonium salt to an organic solvent in a vessel under an inert atmosphere, thereby forming a first mixture comprising the quaternary ammonium salt and the solvent; and (b) mixing the first mixture at a temperature and for a time sufficient to remove water and a portion of the solvent from the first mixture, wherein the mixing is performed in an inert atmosphere and the temperature is less than the decomposition temperature of the quaternary ammonium salt.Type: ApplicationFiled: December 28, 2006Publication date: July 3, 2008Applicant: GENERAL ELECTRIC COMPANYInventors: Thomas Link Guggenheim, Paul Edward Howson, Farid Fouad Khouri, Lioba Maria Kloppenburg, Matthew Hal Littlejohn, Jacob Lee Oberholtzer, Juan Rodriguez Ordonez, Suresh R. Sriram, David Winfield Woodruff
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Publication number: 20080146620Abstract: A dibenzylamine compound represented by the formula (1) wherein R1 and R2 are each a C1-6 allyl group optionally substituted by halogen atoms and the like; R3, R4 and R5 are each a hydrogen atom, a halogen atom and the like, or R3 and R4 may form, together with carbon atoms bonded thereto, a homocyclic or heterocyclic ring optionally having substituent(s); A is —N(R7)(R8) and the like; ring B is an aryl group or a heterocyclic residue; R6 is a hydrogen atom, a halogen atom, a nitro group, a C1-6 allyl group and the like; n is an integer of 1 to 3, a prodrug thereof and a pharmaceutically acceptable salt thereof show selective and potent CETP inhibitory activity, and therefore, they can be provided as therapeutic or prophylactic agents for hyperlipidemia or arteriosclerosis and the like.Type: ApplicationFiled: November 13, 2007Publication date: June 19, 2008Applicant: Japan Tobacco Inc.Inventors: Kimiya Maeda, Hironobu Nagamori, Hiroshi Nakamura, Hisashi Shinkai, Yasunori Suzuki, Daisuke Takahashi, Toshio Taniguchi
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Patent number: 7388021Abstract: The present invention provides novel pyridyl or phenyl ureas and analogues thereof, which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases responsive to modulation of P2Y1 receptor activity.Type: GrantFiled: May 10, 2005Date of Patent: June 17, 2008Assignee: Bristol Myers Squibb CompanyInventors: Hannguang J. Chao, Huji Tuerdi, Timothy F. Herpin, Jacques Yves Roberge, Yalei Liu, R. Michael Lawrence, Robert P. Rehfuss, Charles G. Clark, Jennifer X. Qiao, Timur Gungor, Patrick Y. S. Lam, Tammy Wang, Rejean Ruel, Alexandre L'Heureux, Carl Thibeault, Gilles Bouthillier, Dora M. Schnur
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Patent number: 7388022Abstract: A compound selected from those of formula (I): wherein: n represents an integer from 1 to 6 inclusive, R1 and R2 represent a hydrogen atom, a (C1-C6)alkyl group or an aryl-(C1-C6)alkyl group, R3 and R4 represent a hydrogen atom or a (C1-C6)alkyl group, R5 and R6 represent a hydrogen atom or a (C1-C6)alkyl, halogen, hydroxy, (C1-C6)alkoxy, cyano, nitro, (C2-C6)acyl, (C1-C6)alkoxycarbonyl, (C1-C6)trihaloalkyl or (C1-C6)-trihaloalkoxy group or an optionally substituted amino group, R7 represents a hydrogen atom, a (C1-C6)alkyl group or an arylalkyl group, its enatiomers, diastereoisomers and additional salts thereof with a pharmaceutically acceptable acid or base. Medicinal products containing the same which are useful in the treatment of conditions requiring a specific nicotinic ligand of ?4?2 receptors.Type: GrantFiled: July 26, 2006Date of Patent: June 17, 2008Assignee: Les Laboratoires ServierInventors: Solo Goldstein, Claude Guillonneau, Yves Charton, Brian Lockhart, Pierre Lestage
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Publication number: 20080119478Abstract: The present invention provides a 2,3-dihydro-6-nitroimidazo[2,1-b]oxazole compound represented by the following general formula: (1) in the above formula (1), R1 represents a hydrogen atom or C1-C6 alkyl group, n represents an integer of 0 to 6, R1 and —(CH2)nR2 may form a spiro ring represented by the formula (30) below, together with the adjacent carbon atom (in the formula below, RRR represents a piperidyl group which may have substituents on the piperidine ring), (30) and R2 represents a benzothiazolyloxy group, quinolyloxy group, pyridyloxy group or the like. The present compound has an excellent bactericidal action against Mycobacterium tuberculosis, multi-drug-resistant Mycobacterium tuberculosis, and atypical acid-fast bacteria.Type: ApplicationFiled: October 29, 2004Publication date: May 22, 2008Inventors: Hidetsugu Tsubouchi, Hirofumi Sasaki, Motohiro Itotani, Yoshikazu Haraguchi, Shin Miyamura, Makoto Matsumoto, Hiroyuki Hashizume, Tatsuo Tomishige, Masanori Kawasaki, Kinue Ohguro, Takumi Sumida, Takeshi Hasegawa, Kazuho Tanaka, Isao Takemura
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Patent number: 7375121Abstract: The present invention concerns compounds of formula (I), and pharmaceutically acceptable salts or solvates thereof, or solvates of such salts, which compounds inhibit carboxypeptidase U and thus can be used in the prevention and treatment of diseases where inhibition of carboxypeptidase U is beneficial. In further aspects, the invention relates to compounds of the invention for use in therapy; to processes for preparation of such new compounds; to pharmaceutical compositions containing at least one compound of the invention, or a pharmaceutically acceptable salt or solvate thereof, as active ingredient; and to the use of the active compounds in the manufacture of medicaments for the medical use indicated above.Type: GrantFiled: September 23, 2002Date of Patent: May 20, 2008Assignee: AstraZeneca ABInventor: Magnus Polla
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Patent number: 7371753Abstract: Disclosed are new dihydropteridinones of general formula (I) wherein the groups R1 to R5, Ra to Rc, W, Q1 and Q2 have the meanings given in the claims and specification, the isomers thereof and the use thereof for preparing a pharmaceutical composition for the treatment of diseases characterised by excessive or abnormal cell proliferation.Type: GrantFiled: August 25, 2005Date of Patent: May 13, 2008Assignee: Boehringer Ingelheim International GmbHInventors: Heinz Stadtmueller, Harald Engelhardt, Andreas Schoop, Martin Steegmaier, Matthias Hoffmann, Matthias Grauert
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Patent number: 7368572Abstract: The present invention is directed to certain hydroxamate derivatives that are inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.Type: GrantFiled: August 19, 2004Date of Patent: May 6, 2008Assignee: Pharmacyclics, Inc.Inventor: Martin Sendzik
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Patent number: 7342115Abstract: 3-substituted-6-aryl pyridines of Formula I are provided: wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptor. Preferred compounds of Formula I bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 3-substituted-6-aryl pyridines, which are useful as probes for the localization of C5a receptors.Type: GrantFiled: November 7, 2003Date of Patent: March 11, 2008Assignee: Neurogen CorporationInventors: Alan J. Hutchison, Jun Yuan, Kyungae Lee, George D. Maynard, Bertrand L. Chenard, Nian Liu, Qin Guo, Zihong Guo, Peter Hrnciar
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Patent number: 7332498Abstract: A method of modulating KSP kinesin activity in vitro comprising contacting KSP kinesin with at least one chemical entity chosen from compounds represented by Formula I: and pharmaceutically acceptable salts thereof, where the variables are as defined further herein.Type: GrantFiled: November 23, 2005Date of Patent: February 19, 2008Assignees: Cytokinetics, Inc., SmithKline Beecham CorporationInventors: Pu-Ping Lu, David J. Morgans, Jr., Bing Yao, Dashyant Dhanak, Steven David Knight
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Publication number: 20080039633Abstract: The invention relates to a process for preparing arylamines or heteroarylamines or arylamides or heteroarylamides by cross-coupling of primary or secondary amines or amides with substituted aryl or heteroaryl compounds in the presence of a Brønsted base and a catalyst or precatalyst, wherein the catalyst comprises a) a transition metal, a complex, a salt or a compound of this transition metal selected from the group consisting of Ni, Pd and b) at least one ligand selected from the group consisting of bidentate bis(phosphino)alkanediyls having the following formula in a solvent or solvent mixture, where the radicals Ar1-4 are each, independently of one another, an aryl or heteroaryl substituent selected from the group consisting of phenyl, naphthyl, pyridyl and biphenyl or Ar1-4 is hydrogen, C1-, C2-alkyl, straight-chain, branched or cyclic C3-C8-alkyl, and L is an alkanediyl bridge which has from 1 to 20 carbon atoms.Type: ApplicationFiled: August 9, 2007Publication date: February 14, 2008Inventors: Joerg JUNG, Andreas Meudt, Bernd Wilheilm Lehnemann