Nitrogen Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 514/349)
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Publication number: 20100331321Abstract: The invention provides compounds of formula (I) wherein R1,R3,L1,L2,G1,G2, A and m are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of microsomal prostaglandin E synthase-1.Type: ApplicationFiled: December 18, 2008Publication date: December 30, 2010Applicant: ASTRAZENECA ABInventors: Johan Bylund, Maria E. Ek, Ylva Gravenfors, Jorg Holenz, Alexander Minidis, Gunnar Nordvall, Daniel Sohn, Karl S.A. Vallin, Jenny Viklund, Stefan Von Berg
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Patent number: 7858643Abstract: Enantiomerically pure compound of formula 1 are provided, as well as methods for their synthesis and use. Preferred compounds are potent inhibitors of the c-Met protein kinase, and are useful in the treatment of abnormal cell growth disorders, such as cancers.Type: GrantFiled: August 26, 2005Date of Patent: December 28, 2010Assignee: Agouron Pharmaceuticals, Inc.Inventors: Jingrong Jean Cui, Lee Andrew Funk, Lei Jia, Pei-Pei Kung, Jerry Jialun Meng, Mitchell David Nambu, Mason Alan Pairish, Hong Shen, Michelle Tran-Dube
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Publication number: 20100324061Abstract: Enantiomerically pure compound of formula 1 are provided, as well as methods for their synthesis and use. Preferred compounds are potent inhibitors of the c-Met protein kinase, and are useful in the treatment of abnormal cell growth disorders, such as cancers.Type: ApplicationFiled: September 1, 2010Publication date: December 23, 2010Inventors: Jingrong Jean Cui, Lee Andrew Funk, Lei Jia, Pei-Pei Kung, Jerry Jialun Meng, Mitchell David Nambu, Mason Alan Pairish, Hong Shen, Michelle Tran-Dube
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Publication number: 20100317865Abstract: Covalent conjugates of an ?,?-disubstituted glycine ester and a modulator of the activity of a target intracellular enzyme or receptor, wherein the ester group of the conjugate is hydrolysable by one or more intracellular carboxylesterase enzymes to the corresponding acid and the ?,?-disubstituted glycine ester is conjugated to the modulator at a position remote from the binding interface between the inhibitor and the target enzyme or receptor pass into cells and the active acid hydrolysis product accumulates within the cells.Type: ApplicationFiled: February 27, 2009Publication date: December 16, 2010Applicant: c/o Chroma Therapeutics Ltd.Inventors: Alan Hornsby Davidson, Alan Hastings Drummond, David Festus Charles Moffat, Alistair David Graham Donald, Stephen John Davies
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Publication number: 20100298325Abstract: a compound of formula (I) or a pharmaceutically acceptable salt or prodrug thereof: wherein X and Y are independently NR5 or O; W and Z are independently a bond or (CH2)mCH(R7)(CH2)n; m=0-1, n=0-2; R is hydrogen or halogen; R1 and R2 are independently selected from hydrogen halogen, CF3, CN, OR8, NR9R10, NR9COR11, NR9SO2R11 or C1-6 alkyl optionally substituted by hydroxyl, C1-6 alkoxy or NR9R10; R3 is hydrogen, halogen, CF3, CN, OR8, SR8 or SO2R11; R4 is hydrogen, halogen, CF3, OR9, NR9R10, NR9COR11, NR9SO2R11 or C1-6 alkyl optionally substituted by hydroxyl, C1-6 alkoxy or NR9R10; R5 is hydrogen or C1-6 alkyl optionally substituted by hydroxyl, C1-6 alkoxy or NR9R10; R6 is hydrogen, fluorine, C1-6 alkyl, or C1-6 alkoxy; R6 is hydrogen, fluorine, C1-6 alkyl, or C1-6 alkoxy; R7 is hydrogen, C1-6 alkyl, phenyl or C1-3 alkylphenyl wherein said phenyl groups are optionally substituted by one or more substituents selected from halogen, C1-6 alkyl, CF3, OCF3 or OR9; R8 is hydrogen or C1-6 alkyl optionally substitutType: ApplicationFiled: October 6, 2008Publication date: November 25, 2010Applicant: SENEXIS LIMITEDInventors: David Ian Carter Scopes, David Christopher Horwell
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Publication number: 20100266539Abstract: The present invention relates to a compound represented by formula (I), a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof, and medical use thereof (the symbols in the formula are as described in the specification). The compound represented by formula (I) has chemokine receptor (especially in CCR4 and/or CCR5) antagonistic activity. Therefore it is useful for prevention and/or treatment of a chemokine receptor-mediated disease such as inflammatory and/or allergic diseases [systemic inflammatory response syndrome (SIRS), anaphylaxis, anaphylactoid reaction, allergic angiitis, transplant rejection reaction, hepatitis, nephritis, nephropathy, pancreatitis, rhinitis, arthritis, inflammatory ocular disease, inflammatory bowel disease, disease in cerebro and/or circulatory system, respiratory disease, dermatosis, autoimmune disease, and the like], infection [viral disease (human immunodeficiency virus infection, acquired immunodeficiency syndrome, SARS, etc.Type: ApplicationFiled: March 25, 2010Publication date: October 21, 2010Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Hiromu HABASHITA, Hiroshi Ochiai, Natsuko Tokuda, Shiro Shibayama, Noriki Watanabe, Takaki Komiya, Kazuhiko Takeda
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Publication number: 20100267774Abstract: Compounds of formula (I) are inhibitors of p38 MAP kinase, and are therefore of utility in the treatment of, inter alia, inflammatory conditions including rheumatoid arthritis and COPD: formula (I) wherein: G is —N? or —CH?; D is an optionally substituted divalent mono- or bi-cyclic aryl or heteroaryl radical having 5-13 ring members; R6 is hydrogen or optionally substituted C1-C3 alkyl; P represents hydrogen and U represents a radical of formula (IA); or U represents hydrogen and P represents a radical of formula -A-(CH2)z—X1-L1-Y—NH—CHR1R2 wherein A represents an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic radical having 5-13 ring members; z, Y, L1, and X1 are as defined in the specification; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular esterase enzymes to a carboxylic acid group; and R2 is the side chain of a natural or non-natural alpha amino acid.Type: ApplicationFiled: November 7, 2007Publication date: October 21, 2010Applicant: CHROMA THERAPEUTICS LTD.Inventors: David Festus Charles Moffat, Stéphane Pintat, Stephen Davies
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Patent number: 7816382Abstract: The present invention provides novel urea mimics and analogues of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, W, and R6 are as defined herein. These compounds are selective inhibitors of the human P2Y1 receptor which can be used as medicaments.Type: GrantFiled: June 26, 2006Date of Patent: October 19, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Hannguang J. Chao, R. Michael Lawrence, Rejean Ruel, James C. Sutton
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Patent number: 7812038Abstract: A method for the inhibition of the binding of ?4?1 integrin to its receptors, for example VCAM-1 (vascular cell adhesion molecule-1) and fibronectin; compounds that inhibit this binding; pharmaceutically active compositions comprising such compounds; and to the use of such compounds either a above, or in formulations for the control or prevention of diseases states in which ?4?1 is involved.Type: GrantFiled: June 14, 2005Date of Patent: October 12, 2010Assignee: Encysive Pharmaceuticals, Inc.Inventors: Ronald J. Biediger, Qi Chen, E. Radford Decker, George W. Holland, Jamal M. Kassir, Wen Li, Robert V. Market, Ian L. Scott, Chengde Wu, Jian Li
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Patent number: 7812037Abstract: Compounds with antiplatelet aggregation and anticoagulant characteristics for the treatment of cardiovascular, cerebrovascular, and cardiovascular related diseases and symptoms, are described. The methods are directed to administering pharmaceutical compositions comprising aryl sulfonic pyridoxine and/or substituted pyridoxine analogs.Type: GrantFiled: October 28, 2005Date of Patent: October 12, 2010Assignee: Medicure International, Inc.Inventors: Wasimul Haque, James Diakur, Vinh Pham, Atiq Rehman, Tara Whitney, Mohammed Omar, Seng Yi, A. Qasim Khan
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Publication number: 20100247617Abstract: The present invention generally relates to the transdermal administration of (2S)-(4E)-N-methyl-5-(3-(5-isopropoxypyridin)yl)-4-penten-2-amine, or pharmaceutically acceptable salts thereof. The transdermal administration can be effected using transdermal drug delivery devices, semi-solid dosage forms, or iontophoresis. The drug delivery devices and/or semi-solid dosage forms can provide instantaneous release, sustained release, or combinations thereof, and can include permeation enhancers and other components to assist in drug transport across the dermis, especially the epidermis. The compositions can be used to treat and/or prevent any indication which the active ingredients are capable of treating and preventing, but deliver (2S)-(4E)-N-methyl-5-(3-(5-isopropoxypyridin)yl)-4-penten-2-amine, or pharmaceutically acceptable salts thereof, in an efficacious manner. Disorders that can be treated and/or prevented include central nervous system disorders, addictions, pain, and inflammation.Type: ApplicationFiled: July 30, 2008Publication date: September 30, 2010Applicants: TARGACEPT, INC., ASTRAZENECA ABInventors: Merouane Bencherif, John W. James, Michael G. Williams, Johannes Antonius Maria Neelissen
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Publication number: 20100234428Abstract: The invention relates to substituted 2-mercapto-3-aminopyridines, methods for the preparation thereof, medicaments containing these compounds and the use of these compounds for the preparation of medicaments.Type: ApplicationFiled: March 10, 2010Publication date: September 16, 2010Applicant: GRUNENTHAL GMBHInventors: Sven Kühnert, Beatrix Merla, Achim Kless, Gregor Bahrenberg, Wolfgang Schröder
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Patent number: 7786130Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: GrantFiled: August 28, 2006Date of Patent: August 31, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Sharn Ramaya, Steven Durrant, Juan-Miguel Jimenez, Guy Brenchley, Ronald Knegtel, Michael Mortimore
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Patent number: 7781428Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I: wherein R1, R2, R3A, R3B, R4, R5, R6, R7, R8, and X are as defined in the detailed description of the invention. Corresponding pharmaceutical compositions, methods of treatment, and intermediates are also disclosed.Type: GrantFiled: October 24, 2007Date of Patent: August 24, 2010Assignee: Pfizer Inc.Inventors: Marvin J. Meyers, Graciela B. Arhancet, Xiangyang Chen, Susan Hockerman, David B. Reitz, Joseph G. Rico
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Patent number: 7772258Abstract: An agent for the treatment of allergic eye disease containing a 3-anilino-2-cycloalkenone derivative having the formula (I): wherein R1 is an unsubstituted or substituted C1 to C8 alkyl group provided that an unsubstituted methyl group is excluded, a C3 to C7 cycloalkyl group, a C6 to C10 bicycloalkyl group or an indanyl group, etc., R2 is a C1 to C4 alkyl group, R3 is a hydrogen atom, a C1 to C5 alkyl group, a C3 to C7 cycloalkyl group, etc., R4 is a hydrogen atom, an unsubstituted or substituted C1 to C5 alkyl group, a halogen atom, etc., R5, R6, R7 and R8 are independently a hydrogen atom, a C1 to C5 alkyl group, etc., X is —(CR11R12)n— or NR13—, wherein n is 0 to 2, R11, R12 and R13 are independently a hydrogen atom, a C1 to C5 alkyl group, etc.Type: GrantFiled: August 8, 2008Date of Patent: August 10, 2010Assignee: Nikken Chemicals Co., Ltd.Inventors: Shinji Ina, Akane Takahama
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Publication number: 20100183606Abstract: The present invention is directed to compounds having the formula and methods for using them for the treatment of cancer.Type: ApplicationFiled: March 19, 2010Publication date: July 22, 2010Inventors: ROBERT M BORZILLERI, Lyndon A.M. Cornelius, Robert J. Schmidt, Gretchen M. Schroeder, Kyoung S. Kim
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Publication number: 20100173951Abstract: The invention relates to the novel chemical compounds of the formula (I): (I) in free or salt form, its use in the treatment of NET and/or SERT mediated conditions, e.g., depression, vasomotor symptoms, e.g., hot flashes and other diseases or conditions mediated by NET and/or SERT.Type: ApplicationFiled: June 4, 2008Publication date: July 8, 2010Inventors: Lawrence Wennogle, Peng Li, Jun Zhao
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Publication number: 20100160292Abstract: Methods of inhibiting BTK activity by inhibiting phosphorylation of Y551 of BTK, methods of treating patients by inhibiting BTK activity by inhibiting phosphorylation of Y551 of BTK, chemical entities that bind to BTK and inhibited complexes are provided.Type: ApplicationFiled: September 11, 2007Publication date: June 24, 2010Applicant: CGI PHARMACEUTICALS, INCInventors: James A. Whitney, Julie Di Paolo, Mark Velleca, David R. Brittelli, Kevin S. Currie, James W. Darrow, Jeffrey E. Krope, Seung H. Lee, Steven L. Gallion, Scott A. Mitchell, Doughlas A.I. Pippen, Peter A. Blomgren, Doughlas Gregory Stafford
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Patent number: 7723364Abstract: Compound of general formula (I): Process for preparing this compound. Fungicidal composition comprising a compound of general formula (I). Method for treating plants by applying a compound of general formula (I) or a composition comprising it.Type: GrantFiled: July 19, 2004Date of Patent: May 25, 2010Assignee: Bayer Cropscience SAInventors: Darren James Mansfield, Pierre-Yves Coqueron, Philippe Desbordes, Heiko Rieck, Marie-Claire Grosjean-Cournoyer, Pierre Genix, Alain Villier, Isabelle Christian
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Publication number: 20100120869Abstract: The present invention provides a method of selectively inhibiting PKC? in the presence of PKC?, by administering to a subject in need thereof, a therapeutically effective amount of a compound of Formula I. The present invention also provides a method of inhibiting cytokine synthesis in a T cell, a method of inhibiting T cell proliferation, and a method of inhibiting the replication of and cytokine production by T lymphocytes, while not stimulating or inhibiting the replication of B lymphocytes.Type: ApplicationFiled: September 17, 2009Publication date: May 13, 2010Applicant: CompleGen, Inc.Inventors: Janet Ajioka, Heidi S. Hummel, Rich B. Meyer, John Swindle
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Patent number: 7714138Abstract: The present invention is directed to compounds having the formula and methods for using them for the treatment of cancer.Type: GrantFiled: October 17, 2008Date of Patent: May 11, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Robert M. Borzilleri, Lyndon A. M. Cornelius, Robert J. Schmidt, Gretchen M. Schroeder, Kyoung S. Kim
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Patent number: 7714002Abstract: The present invention provides novel urea mimics and analogues of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, W, and R6 are as defined herein. These compounds are selective inhibitors of the human P2Y1 receptor which can be used as medicaments.Type: GrantFiled: June 26, 2006Date of Patent: May 11, 2010Assignee: Bristol-Myers Squibb CompanyInventor: James C. Sutton
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Patent number: 7687500Abstract: Oxetane-containing nucleosides, particularly non-reducing psiconucleoside oxetanes are described herein. Therapeutic application of these oxetane compounds toward the treatment of nucleoside analog related disorders such as disorders involving cellular proliferation and infection are also described.Type: GrantFiled: January 24, 2008Date of Patent: March 30, 2010Assignee: The University of ConnecticutInventors: Amy R. Howell, Rosa C. Taboada, Stewart K. Richardson
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Publication number: 20100063053Abstract: Disclosed are compounds of the Formulas I and V and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8 and R9, W, X and Y are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: October 12, 2009Publication date: March 11, 2010Applicant: ARRAY BIOPHARMA INC.Inventors: Allison L. Marlow, Eli Wallace, Jeongbeob Seo, Joseph P. Lyssikatos, Hong Woon Yang, James Blake
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Patent number: 7666884Abstract: The present invention belongs to the field of agricultural fungicide and in particular disclosed N-(2-substituted phenyl)-N-methoxycarbamates and their preparation as well as use. Compounds according to the present invention are shown as the general formula I. Compounds according to the present invention have very good fungicidal activities and can be used for the control of plant fungicidal diseases, such as wheat powdery mildew, melon powdery mildew, apple powdery mildew, grape powdery mildew, strawberry powdery mildew, wheat rust, soybean rust, wheat Pythium root rot, cucumber Alternaria blight, rice “bakanae” disease, rice sheath blight, cucumber Fusarium wilt, cucumber anthracnose, rice blast, rice false smut, corn southern leaf blight.Type: GrantFiled: January 25, 2006Date of Patent: February 23, 2010Assignee: Shenyang Research Institute of Chemical IndustryInventors: Chunhe Yang, Liwen Geng, Defeng Zhou, Ling Peng, Hong Zhang, Dongliang Cui, Zhinian Li, Liangqing Wang, Shouguo Zang, Zeyong Zhang
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Publication number: 20100041658Abstract: The invention relates to hydroxyphenyl derivatives of formula (I); and uses thereof as anti-bacterial and/or anti-parasitic agents.Type: ApplicationFiled: April 16, 2007Publication date: February 18, 2010Inventors: Alexis Denis, Vincent Gerusz, Yannick Bonvin
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Patent number: 7652022Abstract: The invention relates to the use of diaryl urea derivatives in the treatment of protein kinase dependent diseases or for the manufacture of pharmaceutical compositions for use in the treatment of said diseases, methods of use of diaryl urea derivatives in the treatment of said diseases, pharmaceutical preparations comprising diaryl urea derivatives for the treatment of said diseases, diaryl urea derivatives for use in the treatment of said diseases, novel diaryl urea derivatives, pharmaceutical preparations comprising these novel diaryl urea derivatives, processes for the manufacture of the novel diaryl urea derivatives, the use or methods of use of the novel diaryl urea derivatives as mentioned above, and/or these novel diaryl urea derivatives for use in the treatment of the animal or human body.Type: GrantFiled: May 28, 2003Date of Patent: January 26, 2010Assignee: Novartis AGInventors: Andreas Floersheimer, Pascal Furet, Paul William Manley, Guido Bold, Eugen Boss, Vito Guagnano, Andrea Vaupel
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Publication number: 20100016286Abstract: The invention provides compounds, pharmaceutical compositions and uses of compounds and salts thereof of general formula (I), for the preparation of a medicament for treatment of an inflammatory disorder, but excluding (S)-3-(r-methylcyclohexyl-carbonylamino)-caprolactam: wherein z is 1, 2, 3 or 4; A is —CO— or —SO2-; Q is linear or branched alkyl, alkenyl, alkynyl, alkoxy, oxyalkyl, aminoalkyl, alkylamino, alkylaminoalkyl, haloalkyl, aryl or substituted aryl; T1 and T2 together constitute a cycloalkyl, cycloalkenyl or polycycloalkyl radical composed of n additional carbon atoms, where n is between 2 and 7; and each hydrogen atom bonded to the carbon atoms in the ring generated by T1 and T2 may be independently be substituted by a group R1, where R1 is independently selected from an alkyl, haloalkyl, alkoxy, haloalkoxy, alkenyl, alkynyl or alkylamino radical of 1 to 20 carbon atoms; or each R1 is independently selected from fluoro, chloro, bromo, iodo, hydroxy, oxyalkyl, amino, aminoalkyl or aminodialkyl radiType: ApplicationFiled: June 14, 2006Publication date: January 21, 2010Inventors: David J. Grainger, David John Fox
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Patent number: 7642277Abstract: Disclosed herein are compounds of formula Ar1—X—W—Ar2 wherein Ar1 and Ar2 represent aryl groups characterized generally as aromatic heterocycles (e.g. imidazolyl or tetrazolyl) or carbocycles (e.g. phenyl or naphthalenyl); the aryl groups are optionally substituted or fused with other heterocycles or carbocycles; the aryl groups can bear substituents such as alkyl, halo or O-alkyl. X is a heteroatom, a valence bond or an optionally substituted divalent methylene, and W represents a spacer; typical spacers include divalent alkylene or alkylene-amido, -amido or -oxy radicals, which may optionally be substituted (e.g. hydroxyl or oxo). A typical compound is a derivative of 2-(N-napthalenyltetrazolylthio)-N-(2-nitrophenyl)acetamide. The compounds have inhibitory activity against Wild Type and single or double mutant strains of HIV.Type: GrantFiled: November 21, 2003Date of Patent: January 5, 2010Assignee: Boehringer Ingelheim International GmbHInventors: Bruno Simoneau, Anne-Marie Faucher, Serge Landry, Jeffrey O'Meara, Bounkham Thavonekham, Christiane Yoakim
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NOVEL POLYMORPH OF (5-AMINO-6-METHOXY-3-PYRIDINCARBONYL) CARBAMIC ACID 2-(S)-HYDROXYMUTILIN 14-ESTER
Publication number: 20090291987Abstract: The present invention relates to a novel polymorph, to processes for the preparation of the polymorph and to the use of the polymorph in medicine, particularly antibacterial therapy.Type: ApplicationFiled: December 9, 2005Publication date: November 26, 2009Inventors: Steven Geoffrey Aitken, Steven Dabbs, Eric Hunt -
Patent number: 7585883Abstract: The present invention is directed to substituted pyridines, methods for their preparation and methods for their use in the treatment and/or prevention of mast cell related conditions.Type: GrantFiled: October 31, 2005Date of Patent: September 8, 2009Assignee: Rigel Pharmaceuticals, Inc.Inventors: Ankush Argade, David Carroll, Alexander B. Rossi
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Publication number: 20090221649Abstract: The invention relates to substituted 2-thio-3,5-dicyano-4-phenyl-6-aminopyridines of formula (I) and their use in medicaments for the prophylaxis and/or treatment of reperfusion injury and damage.Type: ApplicationFiled: March 11, 2006Publication date: September 3, 2009Applicant: Bayer HealthCare AGInventors: Thomas Krahn, Thomas Krämer, Ulrich Rosentreter, James M. Downey, Natalia Solenkova
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Publication number: 20090215834Abstract: Disclosed are compounds of the Formula V and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8 and R9, and W are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, and inflammatory conditions in mammals. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases and inflammatory conditions in mammals and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: August 5, 2008Publication date: August 27, 2009Applicant: Array BioPharma Inc.Inventors: Allison L. Marlow, Eli Wallace, Jeongbeob Seo, Joseph P. Lyssikatos, Hong Woon Yang, James Blake
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Publication number: 20090215797Abstract: The use of an N,N-dimethyl alkylamide or an N-alkanoyl morpholine provides a stable emulsifiable concentrate composition that hinders de-esterification and transesterification of mixtures of a carboxylic acid herbicide and an ester of a different carboxylic acid herbicide. The N,N-dimethyl alkylamide or N-alkanoyl morpholine additionally stabilizes emulsifiable concentrates containing a triazolopyrimidine herbicide having at least one methoxy group on the triazolopyrimidine ring.Type: ApplicationFiled: February 20, 2009Publication date: August 27, 2009Applicant: Dow AgroSciences LLCInventors: Derek J. Hopkins, Robert M. Buttimor
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Publication number: 20090215800Abstract: Covalent conjugation of an alpha amino acid ester to a modulator of the activity of a target intracellular enzyme or receptor, wherein the ester group of the conjugate is hydrolysable by one or more intracellular carboxylesterase enzymes to the corresponding acid, leads to accumulation of the carboxylic acid hydrolysis product in the cell and enables improved or more prolonged enzyme or receptor modulation relative to the unconjugated modulator.Type: ApplicationFiled: May 4, 2006Publication date: August 27, 2009Applicant: CHROMA THERAPEUTICS LTDInventors: Alan Hornsby Davidson, Alan Hastings Drummond, Lindsey Ann Needham
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Publication number: 20090215754Abstract: The present invention relates to methods and compositions for treating neuropathic pain and neuropsychiatric disorders by administering agents that are effective in reducing the effective amount, inactivating, and/or inhibiting the activity of a Na+—K+-2Cl? (NKCC) cotransporter. In certain embodiments, the Na+—K+-2Cl? co-transporter is NKCC1.Type: ApplicationFiled: October 17, 2006Publication date: August 27, 2009Inventors: Daryl W. Hochman, John J. Partridge
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Publication number: 20090203711Abstract: Compounds of formula (I) are inhibitors of p38 MAP kinase, and are therefore of utility in the treatment of, inter alia, inflammatory conditions including rheumatoid arthritis and COPD: wherein: G is —N? or —CH?; B is an optionally substituted divalent mono- or bicyclic aryl or heteroaryl radical having 5-13 ring members; R2 is hydrogen or optionally substituted C1-C3 alkyl; P represents hydrogen and U represents a radical of formula (IA); or U represents hydrogen and P represents a radical of formula -A-(CH2)z-L1-Y1—R wherein A, z, Y1, and L1 are as defined in the specification; R is a radical of formula (X) or (Y) wherein R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxylesterase enzymes to a carboxylic acid group; R4 is hydrogen; or optionally substituted C1-C6 alkyl, C3-C7cycloalkyl, aryl or heteroaryl or —(C?O)R3, —(C?O)OR3, or —(C?O)NR3 wherein R3 is hydrogen or optionally substituted (C1-C6)alkyl; and D is a monocyclic heterocyclType: ApplicationFiled: May 1, 2007Publication date: August 13, 2009Applicant: CHROMA THERAPEUTICS LTD.Inventor: David Charles Festus Moffat
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Publication number: 20090176797Abstract: A compound represented by the following formula, a salt thereof or a hydrate of the foregoing is useful as a pharmaceutical composition for treating esophageal cancer treating esophageal cancer. [R1 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; R2 and R3 represent hydrogen; R4, R5, R6, and R7 may be the same or different and each represents hydrogen, halogen, C1-6 alkyl or the like; R8 represents hydrogen or the like; R9 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; n represents an integer of 1 or 2; X represents —CH?, nitrogen or the like.Type: ApplicationFiled: December 1, 2008Publication date: July 9, 2009Applicant: Eisai R&D Management Co., Ltd.Inventors: Hiroshi Obaishi, Takayuki Nakagawa
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Patent number: 7550453Abstract: The invention relates particularly to 2-alkoxy-3,4,5-trihydroxy-alkylamides, preparation thereof, compositions containing them and use thereof as a medicament, particularly as anti-cancer agents.Type: GrantFiled: May 24, 2007Date of Patent: June 23, 2009Assignee: Aventis Pharma SAInventors: Jidong Zhang, Neerja Bhatnagar, Jean-Marie Ruxer
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Publication number: 20090156578Abstract: In part, the present invention is directed towards compounds with FabI inhibiting properties. Such compounds may also inhibit other enzymes, including those similar to FabI either structurally or functionally, for example, Fab K. Kits and compositions that include the disclosed compounds are also provided. Methods of treating a subject with a bacterial illness is also disclosed.Type: ApplicationFiled: December 1, 2006Publication date: June 18, 2009Inventors: Henry Pauls, Judd M. Berman
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Patent number: 7544702Abstract: Bisaryl-sulfonamide compounds having the formula wherein Ar, R1, R2, L, B, W, X, Y, and Z, compositions and methods are provided that are useful in the treatment or prevention of a condition or disorder mediated by PPAR? or PPAR?. In particular, the compounds of the invention modulate the function of PPAR? or PPAR?. The subject methods are particularly useful in the treatment and/or prevention of diabetes, obesity, hypercholesterolemia, rheumatoid arthritis and atherosclerosis.Type: GrantFiled: August 11, 2005Date of Patent: June 9, 2009Assignee: Amgen Inc.Inventors: Philippe Bergeron, Christopher N. Farthing, Stuart D. Jones, John W. Liebeschuetz, Sarah E. Lively, Lawrence R. McGee, Sharon McKendry, David Sheppard, Stephen C. Young
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Publication number: 20090143383Abstract: The present invention relates to aryloxyethylamine compounds of the formula I and the physiologically tolerated acid addition salts thereof. The variables have the meanings given in the claims and the description. The invention also relates to the use of a compound of the formula I or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand.Type: ApplicationFiled: April 13, 2007Publication date: June 4, 2009Applicant: Abbott GMBH & Co. KGInventors: Roland Grandel, Wilfried Martin Braje, Andreas Haupt, Sean Colm Turner, Udo Lange, Karla Drescher, Liliane Unger
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Publication number: 20090131435Abstract: Disclosed are compounds of the Formula and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9, W, and X are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: January 20, 2009Publication date: May 21, 2009Applicant: Array BioPharma Inc.Inventors: Allison L. Marlow, Eli Wallace, Jeongbeob Seo, Joseph P. Lyssikatos, Hong Woon Yang, James Blake
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Publication number: 20090124668Abstract: The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the treatment of rheumatoid arthritis, multiple sclerosis, atherosclerosis and asthma.Type: ApplicationFiled: January 15, 2009Publication date: May 14, 2009Inventors: Percy H. Carter, Robert J. Cherney, Douglas G. Batt, John V. Duncia, Daniel S. Gardner, Soo S. Ko, Anurag S. Srivastava, Michael G. Yang
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Publication number: 20090118268Abstract: This invention relates to the use of a group of aryl ureas in treating p38 mediated diseases, and pharmaceutical compositions for use in such therapy.Type: ApplicationFiled: October 10, 2008Publication date: May 7, 2009Inventors: Bernd Riedl, Jacques Dumas, Uday Khire, Timothy B. Lowinger, William J. Scott, Roger A. Smith, Jill E. Wood, Mary-Katherine Monahan, Reina Natero, Joel Renick, Robert N. Sibley
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Publication number: 20090105304Abstract: The present application describes a method of treating conditions treatable with a CB2 cannabinoid receptor agonist with reduced CB1-mediated side effects using a combination therapy comprising a CB2 agonist and a CB1 ligand, which can be a CB1 antagonist or a CB1 inverse agonist.Type: ApplicationFiled: October 16, 2008Publication date: April 23, 2009Applicant: ABBOTT LABORATORIESInventor: William A. Carroll
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Publication number: 20090099185Abstract: Compounds of formula (I) are inhibitors of p38 MAP kinase, and are therefore of utility in the treatment of, inter alia, inflammatory conditions including rheumatoid arthritis and COPD: wherein: G is —N? or —CH?; D is an optionally substituted divalent mono- or bi-cyclic aryl or heteroaryl radical having 5-13 ring members; R6 is hydrogen or optionally substituted C1-C3 alkyl; P represents hydrogen and U represents a radical of formula (IA); or U represents hydrogen and P represents a radical of formula -A-(CH2), —X1-L1-Y—NH—CHR1R2 wherein A represents an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic radical having 5-13 ring members; z, Y, L1, and X1 are as defined in the specification; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular esterase enzymes to a carboxylic acid group; and R2 is the side chain of a natural or non-natural alpha amino acid.Type: ApplicationFiled: May 1, 2007Publication date: April 16, 2009Applicant: CHROMA THERAPEUTICS LTD.Inventors: David Charles Festus Moffat, Stephane Pintat, Stephen Davies
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Patent number: 7517994Abstract: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8 and R9, W, X and Y are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.Type: GrantFiled: May 18, 2005Date of Patent: April 14, 2009Assignee: Array Biopharma Inc.Inventors: Allison L. Marlow, Eli Wallace, Jeongbeob Seo, Joseph P. Lyssikatos, Hong Woon Yang, James Blake
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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: 7501413Abstract: The invention is concerned with novel dicarboxamide derivatives of formula (I) wherein A, B, Rc, D and E are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used as medicaments.Type: GrantFiled: October 31, 2005Date of Patent: March 10, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Markus Boehringer, Katrin Groebke Zbinden, Wolfgang Haap, Hans Hilpert, Jacques Himber, Roland Humm, Hans Iding, Dietmar Knopp, Narendra Panday, Fabienne Ricklin, Christoph Martin Stahl