The Other Cyclo In The Bicyclo Ring System Is Also Six-membered (e.g., Naphthyridines, Etc.) Patents (Class 546/122)
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Publication number: 20100137290Abstract: The invention relates to antibacterial compounds of formula I wherein R1 is hydrogen, halogen, hydroxy, alkoxy or cyano; Y1 and Y2 each represent CH, one or two of U, V, W and X represent(s) N and the remaining each represent CH or, in the case of X, may also represent CRa, Ra being halogen, and, in the case of W, may also represent CRb, or each of U, V, W, X, Y1 and Y2 represents CH, or each of U, V, W, X and Y1 represents CH and Y2 represents N, or also one or, provided R1 is hydrogen, two of U, V, W, X, Y1 and Y2 represent(s) CRC and the remaining each represent CH, Rb being alkoxy, alkoxycarbonyl or alkoxyalkoxy and Rc being, each time it occurs, independently represents hydroxy or alkoxy; A-B-D represents a chain of 4 to 6 atoms, which 4 to 6 atoms are seleted from carbon, oxygen and nitrogen and may be substituted; E is one of the following groups: in which Z is CH or N and Q is O or S, or E is a phenyl group which is substituted once or twice in the meta and/or para position(s); and to salts ofType: ApplicationFiled: April 10, 2008Publication date: June 3, 2010Applicant: Actelion Pharmaceuticals Ltd.Inventors: Markus Gude, Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
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Publication number: 20100130517Abstract: New inhibitors of the p38 mitogen-activated protein kinase having the general formula (I) are disclosed herein, as well as processes for their preparation, pharmaceutical compositions comprising them, and their use in therapy.Type: ApplicationFiled: April 25, 2008Publication date: May 27, 2010Inventors: Wenceslao Lumeras Amador, Paul Robert Eastwood
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Publication number: 20100130540Abstract: The present invention provides compounds and methods for treating or preventing the development of a disease, disorder, or condition in a subject or patient.Type: ApplicationFiled: November 13, 2009Publication date: May 27, 2010Applicant: Link Medicine CorporationInventor: Mark E. Duggan
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Publication number: 20100130469Abstract: The present invention relates to novel organic compounds comprising a naphthyridine which may be mediators of a selective subset of kinases belonging to the AGC kinase family, such as for example PKC, PKD, PKN-1/2, CDK-9, MRCK-beat, PASK, PRKX, ROCK-I/II or mediators of other kinases, the selectivity of which would be depending on the structural variation thereof.Type: ApplicationFiled: April 4, 2008Publication date: May 27, 2010Inventors: Maurice van Eis, Walter Schuler, Anette Von Matt, Nicolas Soldermann, Lauren G. Monovich, Christoph Gaul
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Patent number: 7723355Abstract: The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an DPP4 modulated disease or disorder such as, for example, diabetes, by administration of a therapeutically effective dose of a compound according to Formula I. wherein X, Z, A, R2, Y, R1, n, and b are as defined herein.Type: GrantFiled: November 16, 2007Date of Patent: May 25, 2010Assignee: Bristol-Myers Squibb CompanyInventors: John M. Fevig, Jianxin Feng
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Publication number: 20100121051Abstract: Compounds of the formula (I) wherein R1, R2, R3, R4, R5, R6, W, and Y are as described herein, or a tautomer, prodrug, solvate, or salt thereof. These compounds are useful as inhibitors of Urotensin II and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the interaction of Urotensin II with its receptor, including cardiovascular diseases. 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: ApplicationFiled: May 12, 2008Publication date: May 13, 2010Applicant: Boehringer Ingelheim International GmbHInventors: Brian Nicholas Cook, Anne Bettina Eldrup, Ingo Andreas Mugge, Fariba Soleymanzadeh, Sanxing Sun, Yunlong Zhang
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Publication number: 20100113505Abstract: The present invention relates to new compounds having an amino-naphthyridine group. In particular, the present invention relates to new compounds, its stereoisomers and pharmaceutically acceptable salts or solvates thereof having a first unit (moiety) selected from the group of a phenyl derivative, a biphenyl derivative or a diphenyl alkane derivative and at least one amino-naphthyridine group linked with the first unit via a linking group. In specific embodiments, the present invention relates to compounds having a phenyl derivative unit and three amino-naphthyridine groups bound to the phenyl derivative unit via a linking group as well as salts or solvates thereof, in particular, pharmaceutically acceptable salts or solvates thereof. Further, the present invention relates to pharmaceutical compositions comprising said compounds. The compounds are particularly useful for treating or preventing infections, like viral infections.Type: ApplicationFiled: March 18, 2008Publication date: May 6, 2010Inventor: Monika Mazik
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Publication number: 20100113467Abstract: The invention relates to naphthalene carboxylic acid and isoquinoline carboxylic acid amides, and related compounds of formula I and their uses as pharmaceuticals.Type: ApplicationFiled: April 17, 2008Publication date: May 6, 2010Inventors: Paul W. Manley, Joseph Schoepfer
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Patent number: 7709496Abstract: 2H-chromen-2-one derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.Type: GrantFiled: April 5, 2007Date of Patent: May 4, 2010Assignee: Glaxo Group LimitedInventors: William Henry Miller, Alan T. Price
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Patent number: 7705151Abstract: Disclosed are compounds of formula (I): wherein R3, R5, R7 and R8 are defined herein, which are useful as inhibitors SYK kinase and are thus useful for treating diseases resulting from inappropriate mast cell activation, which include allergic and inflammatory diseases. Also disclosed are pharmaceutical compositions comprising these compounds and processes for preparing these compounds.Type: GrantFiled: March 6, 2009Date of Patent: April 27, 2010Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Charles L. Cywin, Scott E. Jakes, Joachim Heider, Mark A. Bobko, Renee L. Des Jarlais, Mark Player, James Rinker, Michael Winters, Bao-ping Zhao
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Patent number: 7705014Abstract: The instant invention provides for compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.Type: GrantFiled: April 10, 2006Date of Patent: April 27, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Chixu Chen, Brian W. Eastman, Essa H. Hu
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Patent number: 7700604Abstract: The invention provides compounds of formula (I): wherein R1, R2, A, A1 and B are as defined in the specification; processes for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy. The compounds are useful as MMP inhibitors.Type: GrantFiled: December 14, 2005Date of Patent: April 20, 2010Assignee: AstraZeneca ABInventors: Balint Gabos, Michael Lundkvist, Magnus Munck Af Rosenschold, Igor Shamovsky, Pavol Zlatoidsky
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Publication number: 20100093738Abstract: The present invention relates to compounds of the formula I and their use for controlling phytopathogenic fungi, and also to fungicidal mixtures comprising a compound of the formula I, where the variables and substituents have the meanings defined in the claims and in the description.Type: ApplicationFiled: October 8, 2006Publication date: April 15, 2010Applicant: BASF SEInventors: Bernd Müller, Jens Renner, Egon Haden
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Publication number: 20100093705Abstract: In part, the present invention is directed to antibacterial compounds.Type: ApplicationFiled: June 6, 2005Publication date: April 15, 2010Inventors: Bruce J. Sargent, Henry Pauls, Judd M. Berman, Jailall Ramnauth, Peter Sampson, Andras Toro, Fernando J. Martin, Matthew D. Surman, Helene Y. Decornez, David D. Manning
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Publication number: 20100087649Abstract: HIV inhibitory compounds of formula (I) including the stereoisomeric forms thereof, the pharmaceutically acceptable salts, and pharmaceutically acceptable solvates thereof; wherein R1 is cyano; R2 is H, C1-6alkyl, trifluoromethyl, amino, mono- or di-C1-6alkylamino, C1-6alkylamino wherein the C1-6alkyl group can be substituted; X1 is CH or N; R3 is phenyl or pyridyl, each unsubstituted or substituted; R4 is H, C1-6alkyl, (C1-6alkylcarbonylamino)C1-6alkyl-, Ar, potionally substituted thienyl, furanyl, pyridyl, pyrimidyl, pyrazinyl, pyrrolyl, pyrazolyl, imidazolyl, triazolyl, oxazolyl, thiazolyl, halo, trifluoromethyl, hydroxy, C1-6alkyloxy, —OPO(OH)2, amino, aminocarbonyl, cyano, —Y1—R6, —Y1-Alk-R6, or —Y1-Alk-Y2—R7; R3 is H, halo, hydroxy or C1-6alkyloxy; or R4 and R5 form —O—CH2—O—; Y1 is O or NR8; Y2 is O or NR9; Alk is bivalent C1-6alkyl; R6 is pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, 4-C1-6alkylpiperazinyl, 4-(C1-6alkylcarbonyl)piperazinyl, pyridyl, or imidazolyl; R7 is H, C1-6alkyl, hydroxyC1-Type: ApplicationFiled: September 28, 2007Publication date: April 8, 2010Inventors: Bart Rudolf Romanie Kesteleyn, Dominique Louis Nestor Ghislain Surleraux, Geerwin Yvonne Paul Haché
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Patent number: 7691850Abstract: Compounds of formula (I) and derivatives thereof: compositions containing them, their preparation and their use as antibacterials.Type: GrantFiled: June 15, 2005Date of Patent: April 6, 2010Assignee: Glaxo Group LimitedInventors: William Henry Miller, Israil Pendrak, Mark Andrew Seefeld
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Publication number: 20100081656Abstract: 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: ApplicationFiled: December 2, 2009Publication date: April 1, 2010Applicant: 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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Patent number: 7687629Abstract: The present invention relates to a process for the preparation of 4-aminomethyl-3-alkoxyiminopyrrolidine methanesulfonate, a key intermediate of quinolone antibiotics. According to the process of the present invention, the total number of steps has been shortened to 2-3 steps, the solid separation is not required, and the use of costly chemicals, particularly (BOC)2O (t-butoxycarbonyl anhydride), several organic solvents and reactants, is eliminated.Type: GrantFiled: August 7, 2007Date of Patent: March 30, 2010Assignee: LG Life Sciences Ltd.Inventors: Gyo-Hyun Hwang, Yeong-Dae Kim, Hyun Nam, Jay-Hyok Chang, Hyun-Ik Shin, Young-Keun Kim, Kyung Hee Lee, Jae Sung Lee, Hyun-Kuk Noh
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Patent number: 7678911Abstract: Disclosed are compounds of formula (I): wherein R3, R5, R7 and R8 are defined herein, which are useful as inhibitors SYK kinase and are thus useful for treating diseases resulting from inappropriate mast cell activation, which include allergic and inflammatory diseases. Also disclosed are pharmaceutical compositions comprising these compounds and processes for preparing these compounds.Type: GrantFiled: January 15, 2008Date of Patent: March 16, 2010Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Charles L. Cywin, Scott E. Jakes, Joachim Heider, Mark A. Bobko, Renee L. Des Jarlais, Mark Player, James Rinker, Michael Winters, Bao-ping Zhao
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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: 20100041694Abstract: An agricultural composition comprising an amide compound represented by the following formula (I), a salt thereof, or a hydrate thereof is effective for controlling or preventing plant diseases caused by plant pathogenic microbes when an effective amount of the agricultural composition is applied to useful crops.Type: ApplicationFiled: March 19, 2008Publication date: February 18, 2010Applicant: Sumitomo Chemical Company, LimitedInventors: Masanao Takaishi, Takashi Komori
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Patent number: 7662995Abstract: 1-Phenylalkanecarboxylic acid derivatives, the processes for the preparation thereof and the use thereof in the treatment and/or prevention of neurodegenerative diseases such as Alzheimer's disease.Type: GrantFiled: February 19, 2004Date of Patent: February 16, 2010Assignee: Chiesi Farmaceutici S.p.A.Inventors: Luca Raveglia, Ilaria Peretto, Stefano Radaelli, Bruno Pietro Imbimbo, Andrea Rizzi, Gino Villetti
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Publication number: 20100029623Abstract: The invention relates to compounds of formula (I) wherein R0 represents H or OH; R1 represents alkoxy; U and W represent N, V represents CH and R2 represents H or F, or U and V represent CH, W represents N and R2 represents H or F, or U and V represent N, W represents CH and R2 represents H, or U represents N. V represents CH, W represents CRa and R2 represents H; Ra represents CH2OH or alkoxycarbonyl; A represents the group CH?CH—B or a binuclear heterocyclic system D, B representing a mono- or di-substituted phenyl group wherein the substituents are halogen atoms and D representing one of the following groups wherein Z represents CH or N, and Q represents O or S; and to salts of such compounds. These compounds are useful as antibacterial agents.Type: ApplicationFiled: December 21, 2007Publication date: February 4, 2010Applicant: Actelion Pharmaceuticals Ltd.Inventors: Christian Hubschwerlen, Georg Rueedi, Jean-Phillippe Surivet, Cornelia Zumbrunn
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Patent number: 7655664Abstract: The invention provides compounds of formula (I): wherein R1, R2, A, A1 and B are as defined in the specification; processes for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy. The compounds are useful as MMP inhibitors.Type: GrantFiled: December 14, 2005Date of Patent: February 2, 2010Assignee: AstraZeneca ABInventors: Balint Gabos, Michael Lundkvist, Magnus Munck Af Rosenschold, Igor Shamovsky, Pavol Zlatoidsky
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Patent number: 7652020Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, TNF-? or combinations thereof.Type: GrantFiled: June 1, 2005Date of Patent: January 26, 2010Assignee: Schering CorporationInventors: Zhuyan Guo, Peter Orth, Zhaoning Zhu, Robert D. Mazzola, Tin-Yau Chan, Henry A. Vaccaro, Brian McKittrick, Joseph A. Kozlowski, Brian J. Lavey, Guowei Zhou, Sunil Paliwal, Shing-Chun Wong, Neng-Yang Shih, Pauline C. Ting, Kristin E. Rosner, Gerald W. Shipps, Jr., M. Arshad Siddiqui, David B. Belanger, Chaoyang Dai, Dansu Li, Vinay M. Girijavallabhan, Janeta Popovici-Muller, Wensheng Yu, Lianyun Zhao
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Publication number: 20100016578Abstract: Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula I, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.Type: ApplicationFiled: September 18, 2009Publication date: January 21, 2010Applicant: Idenix Pharmaceuticals, Inc.Inventors: Christophe Claude Parsy, Francois-Rene Alexandre, Dominique Surleraux, Michel Derock, Frederic Leroy
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Publication number: 20100016277Abstract: Compounds of formula I pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.Type: ApplicationFiled: August 19, 2009Publication date: January 21, 2010Applicant: ABBOTT LABORATORIESInventors: Michael R. Schrimpf, Karin R. Tietje, Richard B. Toupence, Jianguo Ji, Anwer Basha, William H. Bunnelle, Jerome F. Daanen, Jennifer M. Frost, Kevin B. Sippy
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Patent number: 7648984Abstract: Naphthalene, quinoline, quinoxaline and naphthyridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.Type: GrantFiled: July 13, 2005Date of Patent: January 19, 2010Assignee: Glaxo Group LimitedInventors: William Henry Miller, Jeffrey Michael Axten, Mark Andrew Seefeld
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Publication number: 20100009992Abstract: The present invention relates to compounds and pharmaceutically acceptable salts, esters and prodrugs of Formula (I) or (II): which are useful as AMPK modulators effective in treating diabetes, obesity and cancer in a subject.Type: ApplicationFiled: February 4, 2009Publication date: January 14, 2010Inventors: Neal C. Birnberg, Hong Liu, Qing Ping Weng, Haibo Shang, Pan Yin, Sharanappa B. Rajur, Hwa-Ok Kim, Paresh D. Salgaonkar, Norton P. Peet
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Publication number: 20100010035Abstract: The present invention relates to new compounds of the formula [Chemical formula should be inserted here. Please see paper copy] wherein R1, R2, R3, and R31 are as specified herein. The invention also relates to a method for preparation thereof, as well as combinations of the new compounds with previously known agents. The invention also relates to the use of the above-mentioned compounds and combinations for the preparation of a medicament for treating hypertension of different kinds, alleviating organ damage of different kinds, treating or preventing diabetic nephropathy, treating endothelin and angiotensin mediated disorders, and treating prostate cancer.Type: ApplicationFiled: March 1, 2007Publication date: January 14, 2010Inventors: Ramesh Chandra Gupta, Vikrant Vijaykumar Jagtap, Appaji Baburao Mandhare, Tim Perkins, Christer Westerlund
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Patent number: 7645770Abstract: Phenylalanine enamide derivatives of formula (1) are described: wherein R1 is a group Ar1L2Ar2Alk- 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: GrantFiled: December 3, 2008Date of Patent: January 12, 2010Assignee: UCB Pharma S.A.Inventors: Stephen Brand, Stuart Bailey, Julien A. Brown, James A. Johnson, John R. Porter, John C. Head
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Publication number: 20100004222Abstract: Compounds are disclosed that have a formula represented by the following: Formula (I). The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.Type: ApplicationFiled: February 22, 2007Publication date: January 7, 2010Applicant: Renovis, Inc.Inventors: Michael G. Kelly, Carl J. Kaub, John Kincaid, Satyanarayana Janagani, Guoxian Wu, Zhi-Liang Wei, Kiran Sahasrabudhe, Matthew Duncton, Ravindra B. Upasani, Yunfeng Fang, Matthew Cox, Jianhua He
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Publication number: 20090325985Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, diketopiperidine derivatives that possess unique antiviral activity are provided. These compounds are useful for the treatment of HIV and AIDS.Type: ApplicationFiled: June 24, 2009Publication date: December 31, 2009Inventors: Alicia Regueiro-Ren, Jacob Swidorski, Zheng Liu, Tao Wang, Zhongxing Zhang, Lawrence G. Hamann, Nicholas A. Meanwell, David J. Carini, Wenying Li
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Patent number: 7638513Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, aggrecanase, ADMP, LpxC, ADAMs, TACE, TNF-? or combinations thereof.Type: GrantFiled: December 1, 2005Date of Patent: December 29, 2009Assignee: Schering CorporationInventors: M. Arshad Siddiqui, Umar Faruk Mansoor, Panduranga A. Reddy, Vincent S. Madison
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Publication number: 20090312321Abstract: Described are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat or prevent disease or disordered associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activity of kinases such as Abl, ALK, AMPK, Aurora, Axl, Bcr-Abl, BIK, Bmx, BRK, BTK, c-Kit, CSK, cSrc, CDK1, CHK2, CK1, CK2, CaMKII, CaMKIV, DYRK2, EGFR, EphB1, FES, FGFR1, FGFR2, FGFR3, Flt1, Flt3, FMS, Fyn, GSK3?, IGF-1R, IKK?, IKK?, IR, IRAK4, ITK, JAK2, JAK3, JNK1?1, JNK2?, KDR, Lck, LYN, MAPK1, MAPKAP-K2, MEK1, MET, MKK4, MKK6, MST2, NEK2, NLK, p70S6K, PAK2, PDGFR, PDGFR?, PDK1, Pim-2, Plk3, PKA, PKB?, PKC?, PKCtheta, PKD2, c-Raf, RET, ROCK-I, ROCK-II, Ron, Ros, Rsk1, SAPK2a, SAPK2b, SAPK3, SAPK4, SGK, SIK, Syk, Tie2, TrkB, WNK3, and ZAP-70.Type: ApplicationFiled: April 6, 2007Publication date: December 17, 2009Applicant: IRM LLCInventors: Pingda Ren, Guobao Zhang, Shuli You, Taebo Sim, Nathanael S. Gray, Yongping Xie, Xing Wang, Yun He
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Publication number: 20090312326Abstract: This invention relates to a range of alpha substituted 2-benzyl substituted imidazole compounds and pharmaceutically acceptable salts and solvates thereof, to compositions comprising such compounds, processes for their synthesis and their use as parasiticides.Type: ApplicationFiled: August 4, 2009Publication date: December 17, 2009Applicant: PFIZER LIMITEDInventors: Nathan Anthony Logan Chubb, Mark Roger Cox, Jerome Sebastien Dauvergne, Richard Andrew Ewin, Christelle Lauret
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Publication number: 20090306125Abstract: The present invention is a mitochondria-targeted antioxidant prodrug useful for the prevention or treatment of diseases or conditions associated with mitochondrial dysfunction resulting from changes in the mitochondrial redox environment. Antioxidant prodrugs of the invention are produced by modifying an antioxidant to a fatty acid so that the resulting prodrug is targeted to and activated by an enzyme of mitochondrial fatty acid beta-oxidation.Type: ApplicationFiled: November 20, 2006Publication date: December 10, 2009Inventors: Marion W. Anders, James L. Robotham, Shey-Shing Sheu
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Patent number: 7622481Abstract: Cyclohexane and cyclohexene derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly man.Type: GrantFiled: June 25, 2003Date of Patent: November 24, 2009Assignee: Glaxo Group LimitedInventors: Jeffrey Michael Axten, Robert A Daines, David Thomas Davies, Timothy Francis Gallagher, Graham Elgin Jones, William Henry Miller, Neil David Pearson, Israil Pendrak
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Publication number: 20090286767Abstract: Substituted quinolin-4-ylamine analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.Type: ApplicationFiled: February 9, 2009Publication date: November 19, 2009Applicant: Neurogen CorporationInventors: Rajagopal Bakthavatchalam, Timothy M. Caldwell, Bertrand L. Chenard, Stéphane De Lombaert, Kevin J. Hodgetts
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Publication number: 20090275537Abstract: Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, pharmaceutical compositions and methods of treatment of diseases and conditions associated with smooth muscle myosin and/or non-muscle myosin are described.Type: ApplicationFiled: August 11, 2008Publication date: November 5, 2009Inventors: Xiangping Qian, Chihyuan (Grace) Chuang, Pu-Ping Lu, Bing Yao, Qing (Kevin) Lu, Hong Jiang, Wenyue Wang, Bradley P. Morgan, David J. Morgans, JR.
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Publication number: 20090270444Abstract: There are provided according to the invention novel compounds of formula (I) and pharmaceutically acceptable salts and solvates thereof, wherein: R1 is phenyl which may be unsubstituted or substituted by one or two substituents selected from fluorine, chlorine, C1-2alkoxy-, —CN; phenyl fused to a 5-membered saturated ring containing one oxygen atom; pyridinyl which may be unsubstituted or substituted by one or two substituents selected from fluorine or chlorine; or C-linked pyrazolyl which may be unsubstituted or substituted by the substituent C1-2alkyl; R2 is C1-4alkyl; R3 is C1-2alkyl; and n is 0, 1 or 2.Type: ApplicationFiled: November 17, 2005Publication date: October 29, 2009Inventors: Colin David Eldred, John Edward Robinson, Alison Judith Steel
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Publication number: 20090270374Abstract: Bicyclic nitrogen containing compounds and their use as antibacterials.Type: ApplicationFiled: July 18, 2007Publication date: October 29, 2009Inventors: Llius Ballell, David Barros, Gerald Brooks, Julia Castro Pichel, Steven Dabbs, Robert A. Daines, David Thomas Davies, Jose Maria Fiandor Roman, Israil Pendrak, Modesto J. Remuinan Blanco, Jason Anthony Rossi, Ilaria Giordano, Alan Joseph Hennessy, James B. Hoffman, Graham Elgin Jones, Timothy James Miles, Neil David Pearson, Lihua(lily) Zhang
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Publication number: 20090264459Abstract: Compounds of formula (I) in free or a pharmaceutically acceptable salt form, wherein X1, L and Q have the meanings as indicated in the specification, are useful for treating obstructive or inflammatory airways diseases. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: ApplicationFiled: June 28, 2007Publication date: October 22, 2009Inventors: Stephen Paul Collingwood, Robin Alec Fairhurst, Neil John Press
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Patent number: 7605169Abstract: Napthyridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed.Type: GrantFiled: January 24, 2006Date of Patent: October 20, 2009Assignee: Glaxo Group LimitedInventors: William Henry Miller, Mark Andrew Seefeld
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Publication number: 20090258868Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.Type: ApplicationFiled: December 10, 2008Publication date: October 15, 2009Inventors: Zhaoning Zhu, Brian A. McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey Strickland, Elizabeth M. Smith, Andrew Stamford, William J. Greenlee, Robert Mazzola, John Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X.H. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter, Michelle L. Morris, Huizhong Gu, Gang Qian, Dawit Tadesse
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Patent number: 7601736Abstract: The invention relates to novel pyridine derivatives having an inhibitory effect on production of cytokines, which are involved in inflammatory responses, thus suggesting its usefulness as therapeutic agents for treating diseases related to inflammation, immune, chronic inflammation as well as an agent having an anti-inflammatory and analgesic effect. Further, this invention relates to a method of manufacturing the same and a pharmaceutical composition containing the same.Type: GrantFiled: December 30, 2004Date of Patent: October 13, 2009Assignee: SK Chemicals Co., Ltd.Inventors: Hyung Ook Kim, Nam Kyu Lee, Joo Hyon Kim, Hae In Rhee, Yong-Baik Cho, Je Ho Ryu, Nam Ho Kim, Keun Ho Ryu, Jung Bum Yi, Jae Yoon Jung
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Publication number: 20090246198Abstract: Compounds of the following formula are provided: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: March 31, 2009Publication date: October 1, 2009Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Qing Dong, Bohan Jin
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Publication number: 20090239897Abstract: Novel substituted 1,5,7-trisubstituted-1,8-napthyridin-2(1H)-one compounds; 1,5,7 trisubstituted-1,6-napthyridine-2-(1H)-one compounds and 1,5,7-trisubstituted quinoline-2(1H)-one compounds, processes for the preparation thereof, the use thereof in treating CSBP/p38 kinase mediated diseases and pharmaceutical compositions for use in such therapy.Type: ApplicationFiled: May 15, 2009Publication date: September 24, 2009Inventors: JEFFREY CHARLES BOEHM, JAMES FRANCIS CALLAHAN, RALPH F. HALL, XICHEN LIN, KATHERINE LOUISE WIDDOWSON
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Publication number: 20090221564Abstract: Heterocyclic compounds of the formula (I) are provided: wherein ring A, ring B, R1, R2, R3, R4, Y, m, n and q are as identified herein. R1 is in particular amidino. The invention further provides particular benzothiophene compounds. Compounds of the invention may be useful as inhibitors of Factor IXa and in the therapy of cardiovascular conditions and diseases, e.g. thrombosis.Type: ApplicationFiled: February 20, 2007Publication date: September 3, 2009Applicant: TRIGEN LIMITEDInventors: Shouming Wang, Toby Jonathan Blench, Frederic Marlin, Richard Beck, Roger Peter Dickinson
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Publication number: 20090221828Abstract: A process for preparing 1-halo-2,7-naphthyridinyl derivatives is described (I), wherein X is Cl or Br; which process comprises the following steps: (i) reaction of a 3-cyano-4-methylpyridine derivative of formula (A): with a compound of formula (II), in the presence of an N,N-dimethylformamide diC1-6alkylacetal; to give an enamine derivative of formula (III), (ii) cyclisation of the enamine of formula (III), to obtain the compound of formula (IV), (iii) reaction of the compound of formula (IV) with a halogenating agent, to obtain a compound of formula (I).Type: ApplicationFiled: March 21, 2007Publication date: September 3, 2009Applicant: UCB PHARMA, S.A.Inventors: Nicholas David Tyrrell, Neil Tremayne, Graham Robert Evans