Nitrogen Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/297)
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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: 7790757Abstract: Compounds incorporating aryl substituted olefinic amine are provided. Representative compounds are (4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-pyrimidinyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-methoxy-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(6-amino-5-methyl-3-pyridyl)-4-penten-2-amine, (2R)-(4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (2R)-(4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-bromo-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-ethoxy-3-pyridyl)-4-penten-2-amine, (2S)-(4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine and (2S)-(4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine.Type: GrantFiled: October 31, 2007Date of Patent: September 7, 2010Assignee: Targacept, Inc.Inventors: William Scott Caldwell, Gary Maurice Dull, Balwinder Singh Bhatti, Srishailkumar B. Hadimani, Haeil Park, Jared Miller Wagner, Peter Anthony Crooks
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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: 7732442Abstract: 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: GrantFiled: September 3, 2004Date of Patent: June 8, 2010Assignee: 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: 20100130739Abstract: Provided is a compound that has the ability to promote axonal outgrowth in combination with the ability to promote angiogenesis and can therefore be used to reduce central nerve injuries such as head injury and spinal cord injury, cerebral infarction, ischemic heart diseases such as myocardial infarction and organic angina, peripheral arterial occlusive diseases such as critical limb ischemia, or after-effects of these diseases. Specifically, the compound is represented by the following formula (I): in which Nx group is preferably a 6-membered aromatic ring containing two nitrogen atoms; R0, R1 and R2 are each independently a hydrogen atom, an alkyl group, an amino group or the like; E is an oxygen atom or an —NR8 group (wherein R8 is an alkyl group or the like); n is an integer of 0 to 5; X and Y are each a connecting bond, a cycloalkyl group, —CO— or the like; and Q is a hydrogen atom or a phenyl group.Type: ApplicationFiled: April 25, 2008Publication date: May 27, 2010Applicant: ASUBIO PHARMA CO., LTD.Inventors: Naohiro Takemoto, Kenji Murata, Norihito Murayama, Chikaomi Yamada
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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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Publication number: 20100113523Abstract: Disclosed herein are novel compounds and pharmaceutical compositions comprising these compounds. In some embodiments, the compounds are inhibitors of the tryptase enzyme and are useful for treating allergic rhinitis, asthma, vascular injury (e.g., restenosis and atherosclerosis), inflammatory bowel disease, arthritis, psoriasis, anaphylaxis, wounds, infections, and other allergy and inflammatory related diseases.Type: ApplicationFiled: October 29, 2009Publication date: May 6, 2010Inventors: Randall S. Alberte, William P. Roschek, JR.
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Patent number: 7678792Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit, PDGFR?, PDGFR?, CSF1R, Abl, BCR-Abl, CSK, JNK1, JNK2, p38, p70S6K, TGF?, SRC, EGFR, trkB, FGFR3, FLT3, Fes, Lck, Syk, RAF, MKK4, MKK6, SAPK2?, BRK, KDR, c-raf or b-raf kinase, or mutant forms thereof.Type: GrantFiled: October 16, 2007Date of Patent: March 16, 2010Assignee: IRM LLCInventors: Donatella Chianelli, Christopher Cow, Yun He, Songchun Jiang, Xiaolin Li, Xiaodong Liu, Zuosheng Liu, Jon Loren, Valentina Molteni, Juliet Nabakka, Pingda Ren, Taebo Sim, Xiaodong Wang, Shuli You
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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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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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Publication number: 20100004438Abstract: An object of the present invention is to provide a medicinal drug much improved in anti tumor activity and excellent in safety. According to the present invention, there is provided a medicinal drug containing a compound represented by the following general formula (1) or a salt thereof as an active ingredient: [Formula 1] wherein X1 represents a nitrogen atom or a group —CH?, R1 represents a group -Z-R6, in which Z represents a group —CO—, a group —CH(OH)— or the like, R6 represents a 5- to 15-membered monocyclic, dicyclic or tricyclic saturated or unsaturated heterocyclic group having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms, R2 represents a hydrogen atom or a halogen atom, Y represents a group —O—, a group —CO—, a group —CH(OH)— or a lower alkylene group, and A represents [Formula 2] wherein R3 represents a hydrogen atom, a lower alkoxy group or the like, p represents 1 or 2, R4 represents an imidazolyl lower alkyl group or the like.Type: ApplicationFiled: December 4, 2006Publication date: January 7, 2010Inventors: Hironori Matsuyama, Kenji Ohnishi, Takashi Nakagawa, Hideki Takasu, Makoto Sakamoto, Kumi Higuchi, Keisuke Miyajima, Satoshi Yamada, Masaaki Motoyama, Yutaka Kojima, Koichi Yasumura, Takeshi Kodama, Shun Otsuji, Keizo Kan, Takumi Sumida
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Publication number: 20090247762Abstract: An O-aryl N-(6-alkoxy-2-pyridyl)-N-alkylthiocarbamate represented by the following formula (I): (wherein R1, R2 and Ar are as defined below) is produced by treating a phenol represented by the following general formula (IV): Ar—OH ??(IV) (wherein Ar represents an aryl group) with a base in a solvent and then adding thereto an alkali metal salt of N-(6-alkoxy-2-pyridyl)-N-alkyldithiocarbamic acid represented by the following general formula (III): (wherein R1 and R2 independently represent a C1-C4 alkyl group and M represents an alkali metal) and a halomethane represented by the following general formula (V): CH2XmYn ??(V) (wherein X and Y represent different halogen atoms, m represents 0, 1 or 2, n represents 0, 1 or 2, and m+n equals 2) for causing a reaction.Type: ApplicationFiled: December 9, 2005Publication date: October 1, 2009Applicant: Zenyaku Kogyo KabushikikaishaInventors: Mitsuo Sakato, Sumio Terada, Kenichi Saitoh, Tetsuo Watanabe
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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: 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: 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: 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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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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Publication number: 20090143579Abstract: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, 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: January 20, 2009Publication date: June 4, 2009Applicant: ARRAY BIOPHARMA INC.Inventors: James F. Blake, Joseph P. Lyssikatos, Hong-Woon Yang, Eli M. Wallace, Jeongbeob Seo
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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: 20090124669Abstract: Novel compounds for the prevention and treatment of dermatological disorders with an immunoallergic, hyperproliferative and inflammatory component, and a method of producing such compounds. The compounds are bioisosteres of substances with avenanthramide structures.Type: ApplicationFiled: February 21, 2006Publication date: May 14, 2009Inventor: Carlo Ghisalberti
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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: 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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Publication number: 20090069294Abstract: The present disclosure relates to XIAP inhibitor compounds of the formula I.Type: ApplicationFiled: June 6, 2006Publication date: March 12, 2009Inventors: Zhuoliang Chen, Mark G. Palermo, Sushil K. Sharma, Troy Smith, Christopher S. Straub, Run-Ming D. Wang, Yaping Wang, Leigh Zawel
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Publication number: 20090029994Abstract: The present invention relates to a compound of the general formula (1): wherein, Y is a methylene group, and the like; A is an optionally substituted heterocyclic group, and the like; B is an optionally substituted phenyl group, and the like; R1 is an optionally substituted alkyl group, and the like; and R2 is an optionally substituted amino group, and the like; or a pharmaceutically acceptable derivative thereof, which has an inhibitory activity against cholesteryl ester transfer protein (CETP), thereby being useful for prophylaxis and/or treatment of arteriosclerotic diseases, hyperlipemia or dyslipidemia, and the like.Type: ApplicationFiled: July 28, 2008Publication date: January 29, 2009Applicant: Mitsubishi Tanabe Pharma CorporationInventors: Yoshinori Nakamura, Norimitsu Hayashi, Takanori Higashijima, Hitoshi Kubota, Kozo Oka
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Publication number: 20080319188Abstract: A compound represented by the following formula, a salt thereof or a hydrate of the foregoing has an excellent hepatocyte growth factor receptor (HGFR) inhibitory activity, and exhibits anti-tumor activity, angiogenesis inhibitory activity and cancer metastasis inhibitory activity. [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: August 23, 2006Publication date: December 25, 2008Applicant: Eisai R&D Management Co., Ltd.Inventors: Tomohiro Matsushima, Keiko Takahashi, Setsuo Funasaka, Hiroshi Obaishi, Shuji Shirotori
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Publication number: 20080287427Abstract: The invention relates to compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising en a compound of formula I and to the use of a compound of formula I for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in particular tumour diseases.Type: ApplicationFiled: September 14, 2005Publication date: November 20, 2008Inventors: Guido Bold, Hans-Georg Capraro, Giorgio Caravatti, Andreas Floersheimer, Pascal Furet, Paul W. Manley, Andreas Vaupel, Carole Pissot Soldermann, Francois Gessier, Christian Schnell, Amanda Jane Littlewood-Evans, Prasad Koteswara Kapa, Joginder S. Bajwa, Xinglong Jiang
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Publication number: 20080280905Abstract: 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: ApplicationFiled: May 8, 2008Publication date: November 13, 2008Applicant: Bristol Myers Squibb CompanyInventors: Hannguang J. Chao, Huji Tuerdi, Timothy F. Herpin, Jaques 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: 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: 7432227Abstract: 4-Aminopicolinic acids having alkyl or alkenyl substituents in the 6-position and their amine and acid derivatives are potent herbicides demonstrating a broad spectrum of weed control.Type: GrantFiled: April 2, 2004Date of Patent: October 7, 2008Assignee: Dow AgroSciences LLCInventors: Terry William Balko, Ann Marie Buysse, Stephen Craig Fields, Nicholas Martin Irvine, William Chi-Leung Lo, Christian Thomas Lowe, John Sanders Richburg, Paul Richard Schmitzer
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Publication number: 20080200676Abstract: The present invention provides 3-benzyloxy-2-aminopyridine (BOPA), 3-(2-Hydroxyethyl)-2-methyl-9-hydoxy-4H-pyrido[1,2-a]pyrimidine-4-one (HMBP), 3-(2-Chloroethyl)-2-methyl-9-hydoxy-4H-pyrido[1,2-a]pyrimidine-4-one (CMHP) and 3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrrido[1,2-a]- pyrimidin-4-one (CMHTP) useful as intermediates for the preparation of paliperidone. The present invention also provides processes for preparing these intermediates and for preparing paliperidone.Type: ApplicationFiled: August 23, 2007Publication date: August 21, 2008Inventors: Ben-Zion Dolitzky, Evgeny Shapiro, Santiago Ini, Yaron Shmuely, Eli Lancry
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Publication number: 20080167468Abstract: The present invention relates to a diastereomeric mixture of Silacycle Compounds and methods for using the diastereomeric mixture of Silacycle Compounds for stereoselective synthesis.Type: ApplicationFiled: June 6, 2007Publication date: July 10, 2008Applicant: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORKInventors: James Lincoln Leighton, Richard Berger, Seiji Shirakawa, Gregory T. Notte
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Publication number: 20080153834Abstract: At least one chemical entity chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, and mixtures thereof is described herein. Pharmaceutical compositions comprising at least one chemical entity of the invention, together with at least one pharmaceutically acceptable vehicle chosen from carriers adjuvants, and excipients, are described. Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell activity are described. Methods for determining the presence of Btk in a sample are described.Type: ApplicationFiled: September 11, 2007Publication date: June 26, 2008Inventors: Peter A. Blomgren, Seung H. Lee, Scott A. Mitchell, Jianjun Xu, Aaron C. Schmitt, Jeffrey E. Kropf, Kevin S. Currie
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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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Publication number: 20080058383Abstract: Treatment of Diseases caused by Disturbances of the Activity of the Androgen Receptor uses of compounds of Formula (I): (as defined herein), for the treatment of diseases caused by disturbances of the activity of androgen receptor are provided: Formula (I). Isolated compounds of Formula (I) are also provided.Type: ApplicationFiled: October 21, 2004Publication date: March 6, 2008Inventors: Henrik Jernstedt, Neeraj Garg, Annika Gustavsson, Mikael Gillner, Ana Maria Garcia Collazo, Eva Koch
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Patent number: 7320993Abstract: The invention relates to new pyridylalkane, alkene, and alkine acid amides substituted with an aryl and/or heteroaryl residue according to the general formula (I), with a saturated or one or several-fold unsaturated hydrocarbon residue in the carboxylic acid group, methods for the synthesis of these compounds, medicaments containing these and their production as well as their therapeutic use, especially as cytostatic agents and immunosuppressive agents, for example in the treatment or prevention of various types of tumors and control of immune reactions such as autoimmune diseases.Type: GrantFiled: June 16, 2000Date of Patent: January 22, 2008Assignee: Astellas Deutschland GmbHInventors: Elfi Biedermann, Max Hasmann, Roland Löser, Benno Rattel, Friedemann Reiter, Barbara Schein, Klaus Seibel, Klaus Vogt, Katja Wosikowski, Isabel Schemainda
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Patent number: 7307092Abstract: Compounds incorporating aryl substituted olefinic amine are provided. Representative compounds are (4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-pyrimidinyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-methoxy-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(6-amino-5-methyl-3-pyridyl)-4-penten-2-amine, (2R)-(4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (2R)-(4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-bromo-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-ethoxy-3-pyridyl)-4-penten-2-amine, (2S)-(4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine and (2S)-(4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine.Type: GrantFiled: April 20, 2006Date of Patent: December 11, 2007Assignee: Targacept, Inc.Inventors: William Scott Caldwell, Gary Maurice Dull, Balwinder Singh Bhatti, Srishailkumar B. Hadimani, Haeil Park, Jared Miller Wagner, Peter Anthony Crooks
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Patent number: 7288559Abstract: The present invention is directed to compounds that are antagonists of CGRP receptors and that are useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: March 10, 2004Date of Patent: October 30, 2007Assignee: Merck + Co, Inc.Inventors: Ian M. Bell, Steven N. Gallicchio, Craig A. Stump, C. Blair Zartman
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Patent number: 7273877Abstract: The present invention relates to 5-substituted-4-(substituted)phenylamino-2-pyridone derivatives, pharmaceutical compositions and methods of use thereof.Type: GrantFiled: June 24, 2004Date of Patent: September 25, 2007Assignee: Warner-Lambert Company, LLCInventors: Shannon Leigh Black, Michael David Kaufman, Daniel Fred Ortwine, Mark Stephen Plummer, John Quin, III, Gordon William Rewcastle, Aurash B. Shahripour, Julie Ann Spicer, Christopher Emil Whitehead
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Patent number: 7271181Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: GrantFiled: May 10, 2002Date of Patent: September 18, 2007Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jeremy Green, Scott L Harbeson, John E Cochran
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Patent number: 7265213Abstract: A novel method of conjugating chelators to biomolecules such as proteins is provided. More particularly, the invention provides compositions and methods of using those compositions for the detection, purification and transport of divalent metal cation binding biomolecules.Type: GrantFiled: July 28, 2005Date of Patent: September 4, 2007Assignee: KPL, Inc.Inventors: Mekbib Astatke, Gordana Pajkovic, Danielle Lynee Russell
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Patent number: 7256295Abstract: The present invention relates to a novel process for producing 2,3-diamino-6-methxoypyridine. The process comprises neutralizing 2,3-diamino-6-methoxy pyridine dihydrochloride, which, in turn, is prepared by the reduction of 2-amino-6-methoxy-3-nitropyridine. The 2-amino-6-methoxy-3-nitropyridine is further prepared by methoxylation of 2-amino-6-chloro-3-nitropyridine by sodium methoxide in methanol.Type: GrantFiled: August 3, 2005Date of Patent: August 14, 2007Assignee: Jubilant Organosys LimitedInventors: D. B. Thakare, Yashbir Singh, Ashutosh Agarwal
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Patent number: 7230098Abstract: Aminopyridine and aminopyrazine compounds of formula (1), compositions including these compounds, and methods of their use are provided.Type: GrantFiled: February 26, 2004Date of Patent: June 12, 2007Assignee: Sugen, Inc.Inventors: Jingrong Jean Cui, Dilip Bhumralkar, Iriny Botrous, Ji Yu Chu, Lee A. Funk, Cathleen Elizabeth Hanau, G. Davis Harris, Lei Jia, Joanne Johnson, Stephen A. Kolodziej, Pei-Pei Kung, Xiaoyuan (Sharon) Li, Jason (Qishen) Lin, Jerry Jialun Meng, Mitchell David Nambu, Christopher G. Nelson, Mason Alan Pairish, Hong Shen, Michelle Tran-Dube, Allison Walter, Fang-Jie Zhang, Jennifer Zhang
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Patent number: 7223868Abstract: 2,3-Di-substituted N-heteroaromatic propionamides with said substitution at the 3-position being a substituted phenyl group and at the 2-position being a methyl cycloalkyl ring, said propionamides being glucokinase activators which increase insulin secretion in the treatment of type II diabetes.Type: GrantFiled: April 4, 2005Date of Patent: May 29, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Fred Thomas Bizzarro, Wendy Lea Corbett, Joseph Francis Grippo, Nancy-Ellen Haynes, George William Holland, Robert Francis Kester, Paige Erin Mahaney, Ramakanth Sarabu
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Patent number: 7223778Abstract: Novel 5-substituted-2-arylpyridine compounds are provided. Such compounds can act as selective modulators of CRF receptors. The 5-substituted-2-arylpyridine compounds provided herein are useful in the treatment of a number of CNS and periphereal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds provided are also useful as probes for the localization of CRF receptors and as standards in assays for CRF receptor binding. Methods of using the compounds in receptor localization studies are given.Type: GrantFiled: May 22, 2002Date of Patent: May 29, 2007Assignee: Neurogen CorporationInventors: Ge Ping, Taeyoung Yoon, Lu Yan Zhang, Raymond F. Horvath
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Patent number: 7196198Abstract: An agent comprising the benzoic acid of formula (I) wherein A, B, R6, R7 are carbocyclic ring, heterocyclic ring, etc.; R1 is hydroxy etc.; R2, R3, R4 are alkyl etc.; R5, D, E are alkylene, etc.; G is oxygen etc., as active ingredient. The compound of formula (I) is considered to be useful for the treatment and/or prophylaxis of bone diseases, cancer, systemic granuloma, immunological diseases, allergy, atopy, asthma, gumboil, gingivitis, periodontitis, neurocyte death, Alzheimer's diseases, lungs injury, pulmopathy, acute hepatitis, nephritis, myocardial ischemia, Kawasaki disease, ambustion, ulcerative colitis, Crohn's disease, multiple organ failure, sleeping disorder, platelet aggregation, etc.Type: GrantFiled: December 18, 2003Date of Patent: March 27, 2007Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Kousuke Tani, Kaoru Kobayashi, Takayuki Maruyama