Chalcogen And Acyclic Nitrogen Bonded Directly To The Same Carbon Patents (Class 546/291)
-
Publication number: 20120035157Abstract: There are provided novel compounds of formula (I), wherein R1, R2, R4, G1, G2, L, Y and n are as defined in the Specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of neutrophil elastase.Type: ApplicationFiled: October 14, 2011Publication date: February 9, 2012Applicant: AstraZeneca ABInventors: Marjana Andersson, Peter Hansen, Hans Lönn, Antonios Nikitidis, Petter Sjölin
-
Publication number: 20120010183Abstract: The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula (I): or a pharmaceutically acceptable salt thereof, wherein Het1, X, R1, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.Type: ApplicationFiled: July 11, 2011Publication date: January 12, 2012Applicant: PFIZER LIMITEDInventors: Andrew Simon Bell, Alan Daniel Brown, Marcel John De Groot, Russell Andrew Lewthwaite, Ian Roger Marsh, David Simon Millan, Manuel Perez Pacheco, David James Rawson, Nunzio Sciammetta, Robert Ian Storer, Nigel Alan Swain, Steven Matthieu Gaulier
-
Patent number: 8088926Abstract: The present invention provides novel substituted 2-methyl-2-phenoxy-N-propyl-propionamides and derivatives thereof that are useful as cannabinoid receptor antagonists/inverse agonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, and/or cardiometabolic disorders.Type: GrantFiled: May 19, 2008Date of Patent: January 3, 2012Assignee: Jenrin Discovery, Inc.Inventors: John F. McElroy, Robert J. Chorvat
-
Publication number: 20110280803Abstract: The present invention provides a method for the synthesis of radioiodinated compounds which is advantageous over prior art methods. Using a hydrazine or an aminoxy in place of a primary amine for indirect radioiodination facilitates a much quicker reaction thus reducing reaction time and increasing the yield. In addition, where there are primary amines in the molecule to be radioiodinated, such as the N-terminus of a peptide or lysine residues, reaction at the hydrazine or aminoxy is greatly favoured.Type: ApplicationFiled: January 29, 2010Publication date: November 17, 2011Applicant: GE HEALTHCARE UK LIMITEDInventors: Michelle Avory, Jane Brown, Peter Brian Iveson
-
Patent number: 8013241Abstract: Disclosed is a novel ionic liquid gel electrolyte having high photoelectric conversion efficiency. Also disclosed are a novel dye-sensitized photoelectric conversion device using such an ionic liquid gel electrolyte, and a solar cell composed of such a dye-sensitized photoelectric conversion device. Specifically disclosed is an ionic liquid gel electrolyte obtained by gelling a liquid electrolyte by using an ionic organic oligomer gelling agent represented by the general formulae (1) and (2) below. Also specifically disclosed are a dye-sensitized photoelectric conversion device, wherein the ionic liquid gel electrolyte is arranged between a counter electrode and a dye-absorbed semiconductor substrate which is arranged in contact with a transparent conductive substrate, and a solar cell.Type: GrantFiled: October 16, 2006Date of Patent: September 6, 2011Assignee: National Institute of Advanced Industrial Science and TechnologyInventors: Nagatoshi Koumura, Koujirou Hara, Zhong-Sheng Wang, Masaru Yoshida, Nobuyuki Tamaoki
-
Patent number: 7989478Abstract: The present invention relates to a cinnamoyl compound represented by the formula (I):Type: GrantFiled: September 16, 2004Date of Patent: August 2, 2011Assignee: Sumitomo Chemical Company, LimitedInventors: Yoshitaka Tomigahara, Kiyoshi Higashi, Junya Takahashi, Chizuko Takahashi
-
Publication number: 20110184020Abstract: Vanilloid receptor ligand compounds corresponding to formula I: a process for producing such compounds, pharmaceutical compositions containing them, and the use of such compounds to treat pain and various other vanilloid receptor mediated conditions.Type: ApplicationFiled: March 31, 2011Publication date: July 28, 2011Applicant: Gruenenthal GmbHInventors: Robert FRANK, Gregor Bahrenberg, Thomas Christoph, Klaus Schiene, Jean De Vry, Derek Saunders, Michael Przewosny, Bernd Sundermann, Jeewoo Lee
-
Publication number: 20110184028Abstract: The present invention relates to compounds of Formula I or pharmaceutically acceptable salts, solvates or formulations thereof. Compounds of Formula I inhibit HIV-integrase enzyme and are useful for preventing and treating of HIV infection and AIDS.Type: ApplicationFiled: January 11, 2011Publication date: July 28, 2011Inventors: Brent Richard Stranix, Guy Milot, Jean-Emmanuel Bouchard
-
Publication number: 20110178136Abstract: Disclosed are amino acid and phosphate prodrugs of compounds of the Formula V 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: March 31, 2011Publication date: July 21, 2011Applicant: ARRAY BIOPHARMA INC.Inventors: Allison L. Marlow, Eli Wallace, Jeongbeob Seo, Joseph P. Lyssikatos, Hong Woon Yang, James Blake
-
Publication number: 20110136877Abstract: The present invention provides novel phenoxyacetic acids useful for the prevention and treatment of inflammatory disorders, including those affecting the respiratory system and skin.Type: ApplicationFiled: January 6, 2009Publication date: June 9, 2011Applicant: LIGAND PHARMACEUTICALS INC.Inventors: Brian F. McGuinness, Thuy X. H. Le, Jingqi Duo, Koc-Kan Ho
-
Publication number: 20110118470Abstract: Compounds represented by the following general formula: wherein Ag is an optionally substituted 5- to 14-membered heterocyclic group, etc.; Xg is —O—, —S—, etc.; Yg is an optionally substituted C6-14 aryl group, an optionally substituted 5- to 14-membered heterocyclic group, etc.; and Tg1 is a group represented by the following general formula: (wherein Eg is a single bond or —N(Rg2)—), Rg1 and Rg2 each independently represent a hydrogen atom, an optionally substituted C1-6 alkyl group, etc. and Zg represents a C1-8 alkyl group, a C3-8 alicyclic hydrocarbon group, a C6-14 aryl group, etc.), salts thereof or hydrates of the foregoing.Type: ApplicationFiled: January 7, 2011Publication date: May 19, 2011Inventors: Yasuhiro FUNAHASHI, Akihiko Tsuruoka, Masayuki Matsukura, Toru Haneda, Yoshio Fukuda, Junichi Kamata, Keiko Takahashi, Tomohiro Matsushima, Kazuki Miyazaki, Ken-ichi Nomoto, Tatsuo Watanabe, Hiroshi Obaishi, Atsumi Yamaguchi, Sachi Suzuki, Katsuji Nakamura, Fusayo Mimura, Yuji Yamamoto, Junji Matsui, Kenji Matsui, Takako Yoshiba, Yasuyuki Suzuki, Itaru Arimoto
-
Publication number: 20110112151Abstract: There is provided a compound of formula R1—CO—X—Y—Z—R2 wherein X and Z are each optional groups that are, independently, saturated or unsaturated carbon chains having a length of 1 to 3 carbons; Y is SO, S, SO2, CH?CH, CH2CH2 or O; R1 is wherein denotes the point of attachment; R2 is a heteroaryl group comprising an optionally substituted 5 or 6 membered ring, which ring contains only carbon and at least one nitrogen, or contains only carbon, and at least two nitrogens and at least one sulfur; and wherein (i) when R1 is and —CO—X—Y—Z— is CO—CH2—SO, CO—CH2—S, or CO—CH2—SO2, R2 is other than and; (ii) when R1 is and —CO—X—Y—Z— is —CO—CH2—O—, R2 is other thanType: ApplicationFiled: February 25, 2009Publication date: May 12, 2011Inventors: Nigel Vicker, Xiangdong Su, Fabienne Pradaux-Caggiano, Barry Victor Lioyd Potter
-
Publication number: 20110009407Abstract: The present invention provides compounds that are alpha4 integrin antagonists having a structure according to the following formula: or a tautomer, mixture of tautomers, salt or solvate thereof, wherein Cy, ring A, m, n, p, R1, R2, R3, R4, R5 and R6 are defined in the specification. The invention further provides pharmaceutical compositions including the compounds of the invention as well as methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various conditions and disorders, such as Crohn's disease and ulcerative colitis.Type: ApplicationFiled: April 27, 2010Publication date: January 13, 2011Inventors: Ying-Zi Xu, Shendong Yuan, David Wone, Andrei Konradi
-
Publication number: 20100331303Abstract: The present disclosure relates to HIF-1? prolyl hydroxylase inhibitors, compositions which comprise the HIF-1? prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.Type: ApplicationFiled: August 20, 2010Publication date: December 30, 2010Inventors: Richard Masaru Kawamoto, Shengde Wu, Namal C. Warshakoon, Artem G. Evdokimov, Kenneth D. Greis, Angelique Sun Boyer
-
Publication number: 20100311980Abstract: There is provided a process for preparing sorafenib or a salt thereof comprising the use of a compound of formula (A) wherein R? is selected from the group consisting of hydrogen, —C(O)OA, —C(O)CX3, —C(O)NH2, —C(O)—NHOH or There is also provided intermediate compounds of general formula (A), N-methyl-4-(4-ureidophenoxy)picolinamide, 4-(2-(methylcarbamoyl)pyridin-4-yloxy)phenylcarbamate derivative and N-methyl-4-(4-(2,2,2-trihaloacetamido)phenoxy)picolinamide, processes for their preparation and their use in the preparation of sorafenib.Type: ApplicationFiled: September 10, 2008Publication date: December 9, 2010Applicant: CIPLA LIMITEDInventors: Dharmaraj Ramachandra Rao, Rajendra Narayanrao Kankan, Maruti Ghagare, Sandip Chikhalikar
-
Publication number: 20100305131Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, B1, X and n are defined herein. The invention also relates a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: May 27, 2010Publication date: December 2, 2010Inventors: Gary Mark Coppola, Yuki Iwaki, Rajeshri Ganesh Karki, Toshio Kawanami, Gary Michael Ksander, Muneto Mogi, Robert Sun
-
Publication number: 20100298270Abstract: Described herein are novel HDAC modulators, formulations containing them and methods of using them. In some embodiments, the HDAC modulators possess specific stereo chemistry. In other embodiments, the compounds described herein are used in the treatment or prevention of histone deacetylase mediated disorders.Type: ApplicationFiled: July 23, 2008Publication date: November 25, 2010Applicant: SYNDAX PHARMACEUTICALS, INC.Inventors: John F.W. Keana, Peter Ordentlich, Robert Goodenow
-
Patent number: 7838540Abstract: Compounds of formula (I): or pharmaceutically acceptable derivatives thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors.Type: GrantFiled: August 9, 2004Date of Patent: November 23, 2010Assignee: GlaxoSmithKline LLCInventor: Ann Louise Walker
-
Publication number: 20100286207Abstract: The present invention is related to new 2-oxo-cyclic compound, the process for preparing them and a pharmaceutical composition comprising the same. The present invention provides a pharmaceutical composition for preventing and treating the inflammatory disease comprising the pain or inflammation caused by rheumatic disease, for example, rheumatoid arthritis, spondyloarthopathies, gout, osteoarthritis, systemic lupus erythematosus and juvenile arthritis, and inflammatory syndrome for example, from myositis, gingivitis, synovitis, ankylosing spondylitis, burstitis, burns and scar, inflammatory Crohn's disease, Types I diabetes. therefore, it can be used as the therapeutics for treating and preventing inflammatory diseases.Type: ApplicationFiled: July 20, 2010Publication date: November 11, 2010Applicant: Korea Research Institute of Bioscience and BiotechnologyInventors: Yung Hee KHO, Gyoon Hee HAN, Ho Jae LEE, Bum Woo PARK, Hyo Kon CHUN, Hwan Mook KIM, Song Kyu PARK, Sang Bae HAN, Dong Kyu RYU, Tae Gyu CHUN, Jin Ha LEE, Chang Woo LEE, Ki Hoon LEE, Hee Yoon LEE
-
Publication number: 20100261675Abstract: Conventional many fungicidal compositions have had practical problems such that either a preventive effect or a curing effect is inadequate, the residual effect tends to be inadequate, or the controlling effect against plant diseases tends to be inadequate depending upon the application site, and a fungicidal composition to overcome such problems has been desired.Type: ApplicationFiled: June 24, 2010Publication date: October 14, 2010Applicant: ISHIHARA SANGYO KAISHA, LTD.Inventors: Yuji Nakamura, Shigeru Mitani, Tetsuo Yoneda
-
Publication number: 20100210593Abstract: There is disclosed pyridine- and pyrimidinecarboxamide compounds useful as pharmaceutical agents, synthesis processes, and pharmaceutical compositions which include pyridine- and pyrimidinecarboxamides compounds. More specifically, there is disclosed a genus of CXCR2 inhibitor compounds that are useful for treating a variety of inflammatory and neoplastic disorders.Type: ApplicationFiled: February 17, 2010Publication date: August 19, 2010Applicant: Syntrix Biosystems, Inc.Inventors: Dean Y. Maeda, John A. Zebala
-
Publication number: 20100179137Abstract: [Solving Means] The present inventors have conducted extensive studies on an EP4 receptor agonist, and as a result, found that a novel pyridone compound characterized in that the 1-position in the pyridone ring is substituted with a group having an acidic group such as a carboxyl group and the 6-position is bonded with an aromatic ring group via lower alkyl, lower alkylene, ether, or thioether, has an excellent EP4 receptor agonistic action, thereby completing the present invention. Since the compound of the present invention has an excellent EP4 receptor agonistic action and a blood flow increasing action in the hindlimb of a rat, it is useful as a pharmaceutical, in particular, an agent for treating peripheral arterial occlusive disease.Type: ApplicationFiled: June 6, 2008Publication date: July 15, 2010Inventors: Takashi Kamikubo, Fukushi Hirayama, Masanori Miura, Yuriko Komiya, Takao Okuda, Keisuke Maki
-
Publication number: 20100173952Abstract: The present invention relates to metalloprotein inhibitors comprising: a. an organic substituent and at least one zinc binding group (ZBG) covalently attached thereto; or b. a ZBG substituted by a side chain wherein the ZBG is of formula (I): wherein X is O or S and each R1, R2, R3, and R4 is individually hydrogen or an organic radical. The metalloprotein inhibitors are useful for preventing or treating a pathological disease, condition, or symptom that is associated with pathological metalloprotein activity and/or that is alleviated by inhibition of said activity.Type: ApplicationFiled: March 12, 2010Publication date: July 8, 2010Applicant: The Regents of The University of California Office of Technology TransferInventors: David T. Puerta, Seth M. Cohen, Jana A. Lewis
-
Publication number: 20100152098Abstract: Disclosed are compounds having polybasic functionalities. The compounds inhibit bacterial efflux pump inhibitors and are used in combination with an anti-bacterial agent to treat or prevent bacterial infections. These combinations can be effective against bacterial infections that have developed resistance to anti-bacterial agents through an efflux pump mechanism.Type: ApplicationFiled: November 5, 2009Publication date: June 17, 2010Applicant: Mpex Pharmaceuticals, Inc.Inventors: Tomasz Glinka, Olga Rodny, Keith A. Bostian, David M. Wallace, Robert I. Higuchi, Chun Chow, Chi Ching Mak, Gavin Hirst, Brian Eastman
-
Publication number: 20100125090Abstract: The present invention provides compounds of Formula I useful as modulators of ABC transporter activity, or a pharmaceutically acceptable salt thereof, wherein RB, n, B, RC, RD, RE, A, and Z are described generally and in classes and subclasses below. The present invention also provides pharmaceutical compositions, methods and kits associated with Formula I, useful for as modulators, and for the treatments of disease and disease conditions associated with ABC transporter proteins.Type: ApplicationFiled: August 14, 2009Publication date: May 20, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara S. Hadida Ruah, Mark Miller, Ashvani Singh, Matthew Hamilton, Peter D.J. Grootenhuis
-
Patent number: 7692020Abstract: The invention relates to a process for the preparation of pyridylcarboxylic amides and esters I, Formula (I) wherein Hal, X and R1 have the meanings given in claim 1, which comprises the following steps: (a) heating a mixture consisting essentially of trichloromethylpyridine II, Formula (II), wherein Hal has the meaning given, and 1.0 to 1.5 equivalents of concentrated sulfuric acid, characterized in that the trichloromethylpyridine II in a liquid form is added to the concentrated sulfuric acid at a temperature from 110° C. to 160° C.; and (b) reacting the intermediate product obtained in step (a) with an amine or alcohol III, HXR1, wherein X and R1 have the meaning given, optionally in the presence of a solvent and/or a base.Type: GrantFiled: October 26, 2006Date of Patent: April 6, 2010Assignee: BASF SEInventors: Monika Brink, Marcus Knell, Jan Hendrik Wevers
-
Patent number: 7678796Abstract: The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.Type: GrantFiled: April 25, 2007Date of Patent: March 16, 2010Assignee: AstraZeneca ABInventors: Andreas Wallberg, Karolina Nilsson, Björn Holm, Mats Nagard, Kenneth Granberg, Abdelmalik Slassi, Louise Edwards, Methvin Isaac, Tao Xin, Tomislav Stefanac
-
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
-
Publication number: 20090312372Abstract: Compounds of formula (I): wherein variable groups are defined within; their use in the inhibition of 11?HSD1, processes for making them and pharmaceutical compositions comprising them are described.Type: ApplicationFiled: August 14, 2009Publication date: December 17, 2009Applicant: AstraZeneca ABInventors: William MCCOULL, Martin PACKER, James Stewart SCOTT, Paul Robert Owen WHITTAMORE
-
Publication number: 20090306020Abstract: The present invention relates to pharmaceutical compositions and combinations for treating cancer, comprising a diaryl urea compound and an PI3K/AKT signaling pathway inhibitor. Useful combinations include e.g. BAY-43-9006 as a diaryl urea compound.Type: ApplicationFiled: May 13, 2006Publication date: December 10, 2009Applicant: Bayer Healthcare AGInventors: Urban Scheuring, Ingo Bernard, Claus Garbe, Birgit Schittek, Friedegund Meier
-
Publication number: 20090227629Abstract: The present invention relates to compounds of formula (I), salts or solvates thereof, their use in the manufacture of medicaments for treating neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder. The invention further comprises processes to make these compounds and pharmaceutical formulations thereof. wherein R1, R2, R3, R4, R5, R6 and n are as defined in the description.Type: ApplicationFiled: January 8, 2007Publication date: September 10, 2009Inventors: Clive Leslie Branch, Jacqueline Anne Macritchie, Howard Marshall, Roderick Alan Porter, Simone Spada
-
Publication number: 20090215833Abstract: The present invention relates to a novel form, thermodynamically stable at room temperature, of the tosylate salt of 4-{4-[({[4-chloro-3-(trifluoromethyl)phenyl]amino}carbonyl)amino]phenoxy}-N-methylpyridine-2-carboxamide, to processes for its preparation, to medicaments comprising it and to its use in the control of disorders.Type: ApplicationFiled: September 20, 2005Publication date: August 27, 2009Applicant: Bayer HealthCare AGInventors: Alfons Grunenberg, Jana Lenz
-
Publication number: 20090209767Abstract: The invention relates to 2-(butyl-1-sulfonylamino)-N-[1(R)-(6-methoxy-pyridin-3-yl)propyl]benzamide of the formula I and to its pharmaceutically acceptable salts, their preparation and use, in particular for the treatment and prophylaxis of atrial arrhythmias, for example atrial fibrillation or atrial flutters.Type: ApplicationFiled: April 29, 2009Publication date: August 20, 2009Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBHInventors: Joachim BRENDEL, Heinz GOEGELEIN, Klaus WIRTH, Gert Ulrich KUERZEL
-
Patent number: 7547782Abstract: The present invention is directed to compounds having the formula I or II: including salts thereof, and methods for using them for the treatment of cancer.Type: GrantFiled: September 28, 2006Date of Patent: June 16, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Robert M. Borzilleri, Xiao-Tao Chen, David K. Williams, John S. Tokarski, Robert F. Kaltenbach
-
Publication number: 20090105239Abstract: The invention provides compounds of formula wherein R1, R3, R4, R5, R6, R14, X, W and Z 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 human neutrophil elastase.Type: ApplicationFiled: March 14, 2006Publication date: April 23, 2009Inventors: Thomas Brimert, Karolina Lawitz, Hans Lonn, Antonios Nikitidis, Asim Kumar Ray, Jenny Sandmark
-
Publication number: 20090099239Abstract: The present invention relates to novel compounds and compositions having antiviral activity. The invention also relates to methods for the therapeutic or prophylactic treatment of viral infections in mammals.Type: ApplicationFiled: June 23, 2006Publication date: April 16, 2009Inventors: Gary Dinneen Ewart, Wayne Morris Best
-
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
-
Publication number: 20090093416Abstract: The present invention provides a compound of formula I: wherein R1, R2, R3, R4, and R5 are as defined herein. The present invention also provides pharmaceutical compositions and methods using such compositions for treating a caspase-mediated diseases and processes for preparing the compounds of the invention.Type: ApplicationFiled: June 17, 2008Publication date: April 9, 2009Inventors: Guy Brenchley, Jean-Damien Charrier, Steven Durrant, Ronald Knegtel, Michael Mortimore, John R. Studley
-
Patent number: 7511151Abstract: Fungicidal compounds of the general formula (1), or the corresponding pyridine N-oxide, wherein X, Y, R1, R2, R3, R4 and R5 are as defined in the description.Type: GrantFiled: October 23, 2003Date of Patent: March 31, 2009Assignee: Syngenta LimitedInventor: Patrick Jelf Crowley
-
Publication number: 20090018340Abstract: The present invention is directed to a practical process for the preparation of an enamide (II) by palladium catalyzed coupling of a primary amide (IV) with a compound of structural formula (III), as shown below: As well as to crystalline forms of a compound produced by this process, in particular, an anhydrous crystal form, Form B, and crystalline solvates falling into three patterns, Type 1, Type 2, and Type 3, and crystalline intermediate compounds produced in the process. Still further, the present invention relates to the stereoselective reduction of the tetrasubstituted enamide (II) to the corresponding amide (I).Type: ApplicationFiled: July 1, 2005Publication date: January 15, 2009Inventors: Kevin R. Campos, Artis Klapars, J. Christopher McWilliams, C. Scott Shultz, Debra J. Wallace, Alex M. Chen, Lisa F. Frey, Andrey V. Peresypkin, Yaling Wang, Robert M. Wenslow, Cheng-Yi Chen
-
Patent number: 7476683Abstract: The present invention relates to glycinamide derivatives of formula (I), the use of the compounds of formula (I) as inhibitors of raf-kinase, the use of the compounds of formula (I) for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient.Type: GrantFiled: July 31, 2003Date of Patent: January 13, 2009Assignee: Merck Patent GmbHInventors: Hans-Peter Buchstaller, Matthias Wiesner, Oliver Schadt, Christiane Amendt, Frank Zenke, Christian Sirrenberg, Matthias Grell
-
Patent number: 7456315Abstract: The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.Type: GrantFiled: February 26, 2004Date of Patent: November 25, 2008Assignee: Intrexon CorporationInventors: Robert Eugene Hormann, David W. Potter, Orestes Chortyk, Colin M. Tice, Glenn Richard Carlson, Andrew Meyer, Thomas R. Opie
-
Publication number: 20080280904Abstract: Disclosed are compounds active against soluble epoxide hydrolase (sEH), compositions thereof and methods of using and making same.Type: ApplicationFiled: October 4, 2006Publication date: November 13, 2008Inventors: Anne Bettina Eldrup, Fariba Soleymanzadeh, Steven John Taylor
-
Publication number: 20080255166Abstract: The invention relates to the use of dithiocarbamate derivatives for the therapeutic or prophylactic treatment of infectious diseases in mammals (humans and animals) caused by bacteria, especially diseases like tuberculosis (TB) and lepra caused by mycobacteria and infectious diseases caused by staphylococci. The invention further relates to novel dithiocarbamate derivatives of the formula (I), wherein X is a bivalent residue selected from the group consisting of formulae having excellent antibacterial activities, and to pharmaceutical preparations containing the same.Type: ApplicationFiled: June 6, 2008Publication date: October 16, 2008Applicant: NEED PHARMACEUTICALS S.r.I.Inventors: Ute Mollmann, Vadim Makarov
-
Publication number: 20080249313Abstract: The invention relates to a process for the preparation of pyridylcarboxylic amides and esters I, Formula (I) wherein Hal, X and R1 have the meanings given in claim 1, which comprises the following steps: (a) heating a mixture consisting essentially of trichloromethylpyridine II, Formula (II), wherein Hal has the meaning given, and 1.0 to 1.5 equivalents of concentrated sulfuric acid, characterized in that the trichloromethylpyridine II in a liquid form is added to the concentrated sulfuric acid at a temperature from 110° C. to 160° C.; and (b) reacting the intermediate product obtained in step (a) with an amine or alcohol III, HXR1, wherein X and R1 have the meaning given, optionally in the presence of a solvent and/or a base.Type: ApplicationFiled: October 26, 2006Publication date: October 9, 2008Applicant: BASF SEInventors: Monika Brink, Marcus Knell, Jan Hendrik Wevers
-
Patent number: 7427618Abstract: Novel compounds of the formula (I), in which R1, R2, R3, X and Y have the meaning indicated in Patent claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumors.Type: GrantFiled: January 30, 2004Date of Patent: September 23, 2008Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Werner Mederski, Christos Tsaklakidis, Dieter Dorsch, Bertram Cezanne, Johannes Gleitz, Christoph van Amsterdam
-
Patent number: 7425570Abstract: The invention provides pyridoxal and pyridoxine analogues, pharmaceutical compositions containing pyridoxine and pyridoxal analogues, and methods of administering pharmaceutical compositions containing a therapeutically effective amount of at least one of these analogues. In accordance with the present invention, the pyridoxal and pyridoxine analogues can be used in the treatment or prevention of of heparin induced thrombocytopenia (HIT), stroke, and ischemia, and in the treatment of symptoms thereof. The the pyridoxal and pyridoxine analogues can be used in neuroprotection.Type: GrantFiled: December 21, 2004Date of Patent: September 16, 2008Assignee: Medicure International Inc.Inventor: Wasimul Haque
-
Publication number: 20080221020Abstract: Transport molecules include a dendrimer and a biologically active molecule. The dendrimer of such transport molecules includes at least one guanidine group, at least one protonated guanidine group, at least one protected guanidine group, at least one amidine group, at least one protonated amidine group, at least one protected amidine group, at least one ureido group, at least one protonated ureido group, at least one protected ureido group, at least one thioureido group, at least one protonated thioureido group, or at least one protected thioureido group. The biologically active molecule is bonded to the dendrimer. A method of increasing the bioavailability of a drug includes bonding the drug to a dendrimer of the invention.Type: ApplicationFiled: July 18, 2003Publication date: September 11, 2008Applicants: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA, LG LIFE SCIENCESInventors: Murray Goodman, Churl Min Seong, Guido Harms, Changhee Min, Byung Hyune Choi, Hyun-Ho Chung
-
Publication number: 20080210907Abstract: An ionic organic compound having a repeating unit of formula (I) can be synthesized easily from a readily available organic compound through a small number of reaction steps, can be produced without any purification technique such as chromatography, and can be used in a quite small amount for gelation of water or an ionic liquid without any other auxiliary solvent: [-(A-B-C)n-]•m(X) ??(I) wherein A represents a group having a quaternary ammonium cation which is formed from a heterocyclic compound having at least one nitrogen atom; B represents a functional group, which may have a substituent, selected from amide, urea, urethane and peptide groups; C represents a divalent hydrocarbon group, which may have a substituent, capable of linking between A and B; X represents an anion; n represents the number of repeating units; m represents the total number of anions; and n and m are the same integer.Type: ApplicationFiled: January 30, 2006Publication date: September 4, 2008Applicant: NAATIONAL INSTITUTE OF ADVANCED INDUSTRIAL SCIENCE AND TECHNOLOGYInventors: Masaru Yoshida, Nagatoshi Koumura, Nobuyuki Tamaoki, Hajime Kawanami, Hajime Matsumoto, Said Kazaoui, Nobutsugu Minami
-
Publication number: 20080171774Abstract: The present invention relates to nicotinanilides of the formula I in which: n=0, 1, 2; m=2, 3; X1=F, chlorine; X2=halogen; Y=CN, NO2, C1-C4-alkyl, C1-C4-haloalkyl, methoxy or methylthio; p=0, 1; R1=halogen, methyl, C1-C4-haloalkyl, methoxy, methylthio, methylsulfinyl or methylsulfonyl; R2=hydrogen, methyl or ethyl; W=O, S; processes for preparing these compounds, compositions and seed comprising them and also methods for controlling harmful fungi.Type: ApplicationFiled: March 15, 2006Publication date: July 17, 2008Applicant: BASF AkitengesellschaftInventors: Markus Gewehr, Jochen Dietz, Thomas Grote, Carsten Blettner, Wassilios Grammenos, Udo Hunger, Bernd Muller, Frank Schieweck, Anja Schwogler, Jan Klaas Lohmann, Joachim Rheinheimer, Peter Schafer, Siegfried Strathmann, Reinhard Stierl, Jan Rether, Karl Eicken