Ring Nitrogen Is Shared By Two Cyclos Patents (Class 544/263)
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Publication number: 20120041003Abstract: The present invention relates to compounds of formula (I): wherein R1, R2, and R3, are defined herein. Pharmaceutical compositions and methods for treating DGAT-1 related diseases or conditions are also disclosed.Type: ApplicationFiled: October 20, 2011Publication date: February 16, 2012Applicant: Abbott LaboratoriesInventors: Gang Liu, Zhili Xin, Philip R. Kym, Andrew J. Souers
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Publication number: 20120004203Abstract: The present invention relates to novel heterocyclically fused diaryldihydropyrimidine derivatives, to processes for their preparation, to their use alone or in combination for the treatment and/or prevention of diseases and also to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of disorders of the lung and the cardiovascular system.Type: ApplicationFiled: December 29, 2009Publication date: January 5, 2012Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Franz Von Nussbaum, Dagmar Karthaus, Sonja Anlauf, Martina Delbeck, Volkhart Min-Jian Li, Daniel Meibom, Klemens Lustig
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Patent number: 8076344Abstract: The present invention relates to compounds of formula (I): wherein R1, R2, and R3, are defined herein. Pharmaceutical compositions and methods for treating DGAT-1 related diseases or conditions are also disclosed.Type: GrantFiled: April 30, 2008Date of Patent: December 13, 2011Assignee: Abbott LaboratoriesInventors: Gang Liu, Zhili Xin, Philip R. Kym, Andrew J. Souers
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Publication number: 20110295003Abstract: 5-Substituted-8-alkoxy[1,2,4]triazolo[1,5-c]pyrimidin-2-amines are manufactured from 2-substituted-4-amino-5-methoxypyrimidines in a process that avoids hydrazine and cyanogen halide.Type: ApplicationFiled: May 24, 2011Publication date: December 1, 2011Applicant: DOW AGROSCIENCES LLCInventors: Craig Bott, Christopher T. Hamilton, Gary A. Roth
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Publication number: 20110288087Abstract: Provided is a novel compound represented by the following formula Wherein each symbol is as defined in the specification, or a salt thereof, which has an angiotensin II receptor antagonistic activity and a peroxisome proliferator-activated receptor ? agonistic activity, and is useful as an agent for the prophylaxis or treatment of circulatory diseases such as hypertension and the like and/or metabolic diseases such as diabetes and the like, and the like.Type: ApplicationFiled: January 29, 2010Publication date: November 24, 2011Inventors: Tsuyoshi Maekawa, Hideyuki Igawa
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Publication number: 20110281859Abstract: Compounds of the formula I, in which D, X, Y, Z, R and R1 have the meanings indicated in Claim 1, are inhibitors of methionine aminopeptidase and can be employed for the treatment of tumours.Type: ApplicationFiled: December 22, 2009Publication date: November 17, 2011Applicant: Merck Patent Gesellschaft MIT Beschrankter HaftungInventors: Timo Heinrich, Frank Zenke, Mireille Krier, Kai Schiemann
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Publication number: 20110257172Abstract: Compounds of the formula I, in which R1, R2, R3, R3, R4 have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: November 18, 2009Publication date: October 20, 2011Inventors: Oliver Schadt, Dieter Dorsch, Frank Stieber, Andree Blaukat
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Publication number: 20110237575Abstract: The present invention relates to novel heterocyclic compounds as Fatty Acid Binding Protein (“FABP”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.Type: ApplicationFiled: November 10, 2009Publication date: September 29, 2011Inventors: Gerald W. Shipps, JR., Cliff C. Cheng, Xiaohua Huang, Abdelghani Abe Achab, Peter Orth, Johannes H. Voigt, Kyle Ann Soucy
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Publication number: 20110237565Abstract: The present invention relates to compounds and methods which may be useful as inhibitors of H4R for the treatment or prevention of inflammatory, autoimmune, allergic, and ocular diseases.Type: ApplicationFiled: March 10, 2011Publication date: September 29, 2011Applicant: KALYPSYS, INC.Inventors: Allen Borchardt, Robert Davis, Stewart A. Noble
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Publication number: 20110237599Abstract: The present invention relates to compounds and methods which may be useful as inhibitors of H1R and/or H4R for the treatment or prevention of inflammatory, autoimmune, allergic, and ocular diseases.Type: ApplicationFiled: March 9, 2011Publication date: September 29, 2011Applicant: Kalypsys, Inc.Inventors: Allen Borchardt, Robert Davis, Clay Beauregard, Daniel Gamache, Mark Hellberg, Peter Klimko, John Yanni
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Publication number: 20110190269Abstract: The invention relates to compounds of formula wherein R1, R1?, R2, R3, n, A, and hetaryl are defined herein or to pharmaceutically active acid addition salts thereof. The present compounds of formula I are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposition of ?-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.Type: ApplicationFiled: January 24, 2011Publication date: August 4, 2011Inventors: Karlheinz Baumann, Erwin Goetschi, Luke Green, Synese Jolidon, Henner Knust, Anja Limberg, Thomas Luebbers, Andrew Thomas
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Publication number: 20110183992Abstract: Provided are therapeutic and/or preventive agents for migraine which comprise, as an active ingredient, a compound having a selective adenosine A2A receptor antagonistic activity or a pharmaceutically acceptable salt thereof; therapeutic and/or preventive agents for migraine which comprise, as an active ingredient, a compound having a selective adenosine A2A receptor antagonistic activity, which has an affinity for the adenosine A2A receptor 10 times or higher than that for the adenosine A1 receptor, or a pharmaceutically acceptable salt thereof; and the like.Type: ApplicationFiled: July 23, 2009Publication date: July 28, 2011Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Junichi Ikeda, Shunji Ichikawa, Masako Kurokawa, Tomoyuki Kanda
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Publication number: 20110165183Abstract: The invention provides a compound of formula (I): wherein W is a bicyclic heteroaromatic group; or a salt thereof. The compounds and salts thereof have beneficial therapeutic properties (e.g. immunosuppressant properties).Type: ApplicationFiled: July 31, 2009Publication date: July 7, 2011Applicant: BioCryst Pharmaceuticals, Inc.Inventors: Yarlagadda S. Babu, Pooran Chand, Pravin L. Kotian, V. Satish Kumar
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Publication number: 20110160226Abstract: The present invention relates to substituted triazolo-pyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted triazolo-pyrimidine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: ApplicationFiled: December 29, 2010Publication date: June 30, 2011Applicant: ArQule, Inc.Inventor: Syed M. Ali
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Publication number: 20110152257Abstract: The present invention relates to ethynyl compounds of formula wherein X, Y, Z, and R4 are as defined herein or to a pharmaceutically acceptable salt or acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5) and they are therefore useful for the treatment of diseases related to this receptor.Type: ApplicationFiled: December 10, 2010Publication date: June 23, 2011Inventors: Luke Green, Wolfgang Guba, Georg Jaeschke, Synese Jolidon, Lothar Lindermann, Heinz Stadler, Eric Vieira
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Publication number: 20110152256Abstract: Compounds of the Formula I wherein R1 and R2 together with the carbon atoms to which they are bonded optionally form a further heteroaromatic ring of the formula (II) as well as pharmaceutically acceptable salts, solvates, esters and prodrugs thereof are adenosine A2a receptor antagonists and, therefore, are useful in the treatment of central nervous system diseases, in particular Parkinson's disease.Type: ApplicationFiled: March 3, 2009Publication date: June 23, 2011Inventors: Joel M. Harris, Bernard R. Neustadt, Hong Liu, Jinsong Hao, Andrew W. Stamford
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Publication number: 20110144131Abstract: The invention relates to substituted imidazo- and triazolopyrimidines, imidazo- and pyrazolopyrazines and imidazotriazines and processes for their preparation, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, in particular of hematological disorders, preferably of leukopenias and neutropenias.Type: ApplicationFiled: May 2, 2009Publication date: June 16, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLESCHAFTInventors: Stephan Siegel, Andreas Wilmen, Niels Svenstrup, Mark Jean Gnoth, Adrian Tersteegen, Ulrich Rester
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Patent number: 7956061Abstract: The present invention is directed to novel substituted bicyclic pyrimidines which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: January 18, 2006Date of Patent: June 7, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Wallace T. Ashton, Charles G. Caldwell, Hong Dong, Ying-Duo Gao, Giovanna Scapin, Ann E. Weber
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Publication number: 20110105477Abstract: The present invention relates to HIV protease, and methods for inhibiting the function of HIV protease. In particular, present invention provides compounds that inhibit or block the biological activity of HIVp, thereby causing the replication of the HIV virus to be inhibited or to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS. The compounds and formulations also find use in diagnostic and research settings.Type: ApplicationFiled: September 12, 2008Publication date: May 5, 2011Applicant: The Regents of the University of MichiganInventors: Heather A. Carlson, Kelly L. Damm, Kristen L. Meagher
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Publication number: 20110070187Abstract: The present invention relates to methods and compounds useful in the preparation of compounds of the formula (I).Type: ApplicationFiled: August 17, 2010Publication date: March 24, 2011Inventors: Christopher Frederick Matthews, Robert William Scott, John Lloyd Tucker
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Publication number: 20110065696Abstract: A compound represented by the formula (I): or a pharmacologically acceptable salt thereof, wherein Ar1 represents an imidazolyl group or the like which may be substituted with a C1-6 alkyl group, Ar2 represents a phenyl group or the like which may be substituted with a C1-6 alkoxy group, X1 represents a double bond or the like and Het represents a triazolyl group or the like which may be substituted with a C1-6 alkyl group or the like, is effective as a therapeutic or prophylactic agent for a disease caused by A?.Type: ApplicationFiled: November 19, 2010Publication date: March 17, 2011Inventors: Teiji KIMURA, Noritaka Kitazawa, Toshihiko Kaneko, Nobuaki Sato, Koki Kawano, Koichi Ito, Mamoru Takaishi, Takeo Sasaki, Yu Yoshida, Toshiyuki Uemura, Takashi Doko, Daisuke Shinmyo, Daiju Hasegawa, Takehiko Miyagawa, Hiroaki Hagiwara
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Publication number: 20110021521Abstract: The present invention relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein W1, W2, W3, R1, Q, X1, X2 and X3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.Type: ApplicationFiled: July 26, 2010Publication date: January 27, 2011Applicant: Gilead Palo Alto, Inc.Inventors: Britton Corkey, Elfatih Elzein, Robert Jiang, Rao Kalla, Tetsuya Kobayashi, Dmitry Koltun, Xiaofen Li, Gregory Notte, Eric Parkhill, Thao Perry, Jeff Zablocki
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Publication number: 20110015190Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I) wherein R2 is a fused bicyclic ring of the formula (II). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's disease using the compounds of formula (I).Type: ApplicationFiled: December 4, 2008Publication date: January 20, 2011Inventors: Xianhai Huang, Anandan Palani, Jun Qin, Robert Aslanian, Zhaoning Zhu, William Greenlee, Hubert Josien, Wei Zhou, Xiaohong Zhou, Chad E. Bennett, Dmitri Pissarnitski, Mihirbaran Mandal, Pawan Dhondi, Troy McCracken, Thomas Bara, Zhiqiang Zhao, Duane Burnett, John Clader
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Publication number: 20110009429Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, X, Y and Z are as defined in the specification.Type: ApplicationFiled: February 25, 2009Publication date: January 13, 2011Inventors: Paul Oakley, Neil John Press, Carsten Spanka, Simon James Watson
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Publication number: 20110009619Abstract: Disclosed is a compound represented by the formula (I): or a pharmacologically acceptable salt thereof, which is effective as a therapeutic or prophylactic agent for a disease induced by A?, wherein Ar1 represents an imidazolyl group which may be substituted with a C1-6 alkyl group, or the like; Ar2 represents a phenyl group which may be substituted with a C1-6 alkoxy group, or the like; X1 represents a double bond, or the like; and Het represents a triazolyl group or the like which may be substituted with a C1-6 alkyl group or the like, or the like.Type: ApplicationFiled: August 28, 2008Publication date: January 13, 2011Applicant: Eisai R&D Management Co., Ltd.Inventors: Teiji Kimura, Noritaka Kitazawa, Toshihiko Kaneko, Nobuaki Sato, Koki Kawano, Koichi Ito, Mamoru Takaishi, Takeo Sasaki, Yu Yoshida, Toshiyuki Uemura, Takashi Doko, Daisuke Shinmyo, Daiju Hasegawa, Takehiko Miyagawa, Hiroaki Hagiwara
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Publication number: 20100331348Abstract: Compounds of formula (I) wherein the substituents have the meanings assigned to them in claim 1, are useful as pesticides.Type: ApplicationFiled: July 10, 2008Publication date: December 30, 2010Applicants: SYNGENTA CROP PROTECTION, INC., SYNGENTA LIMITEDInventors: Patrice Selles, Eric Daniel Clarke, Alison Clare Elliot, Delphine Fawke, Ottmar Franz Hueter, Urs Mueller, Peter Renold, Sarah Targett, William Guy Whittingham
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Publication number: 20100324043Abstract: Compounds of Formula X: wherein A, X, Y, Z, R5, R6a, and R6b are as defined herein, and pharmaceutically acceptable salts thereof, are described as useful for the treatment of cognitive deficits associated with schizophrenia and other neurodegenerative and/or neurological disorders in mammals, including humans.Type: ApplicationFiled: June 16, 2010Publication date: December 23, 2010Inventors: Michelle M. Claffey, Amy B. Dounay, Matthew M. Hayward, Suobao Rong, Patrick R. Verhoest, Jamison B. Tuttle, Xinmin Gan
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Publication number: 20100305070Abstract: The disclosure relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. Also provided are pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. Provided are methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1B1 and allelic variants thereof. Finally, provided is a method for determining the efficacy of a compound as described herein in treating cancer.Type: ApplicationFiled: April 30, 2010Publication date: December 2, 2010Applicant: The University Court of the University of DundeeInventors: Steven Albert Everett, Saraj Ulhaq
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Publication number: 20100298339Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain triazolo compounds (referred to herein as TAZ compounds), and especially certain [1,2,4]triazolo[1,5-a]pyridine and [1,2,4]triazolo[1,5-c]pyrimidine compounds, which, inter alia, inhibit AXL receptor tyrosine kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit AXL receptor tyrosine kinase function, and in the treatment of diseases and conditions that are mediated by AXL receptor tyrosine kinase, that are ameliorated by the inhibition of AXL receptor tyrosine kinase function, etc., including proliferative conditions such as cancer, etc.Type: ApplicationFiled: October 10, 2008Publication date: November 25, 2010Applicant: CANCER RESEARCH TECHNOLOGY LIMITEDInventors: Grégoire Alexandre Pavé, James Donald Firth, Lorna Stewart, Laurent Jean Martin Rigoreau, Emma Louise Wynne
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Publication number: 20100290992Abstract: The present invention concerns the field of nanoparticle bioconjugates which form an i-motif or an i-motif related structure (compositions) without or with at least one further nucleic acid binding compound. The i-motif base pairs can be charged or non-charged. Their assembly can be controlled by the pH value or temperature. At least one of these nucleic acid binding compounds has to be attached at least to a nanoparticle. The methods provide compositions used for DNA driven programmable nanoparticle assemblies, electronic circuits, diagnostic detection tools, biosensors, memory storage devices, diagnostic devices for biomolecule sequencing and detection, drug delivery, application in tumour diagnostics and treatment, nanomachines, nanofabrication, nanocatalysis, nanoarrays, and nanoscaled enzyme reactors.Type: ApplicationFiled: February 9, 2009Publication date: November 18, 2010Inventors: Frank Seela, Simone Budow, Peter Leonard
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Publication number: 20100267952Abstract: The invention provides a reagent for detecting amyloid in a biological tissue which can be detect amyloid in vitro and in vivo with high sensitivity using a compound which has affinity with amyloid and is suppressed in toxicity such as mutagenicity. The reagent for detecting amyloid deposited in a biological tissue comprises a compound represented by the following formula (1) or a salt thereof: wherein A1, A2, A3 and A4 independently represents a carbon or nitrogen; R1 is a halogen substituent; R2 is a halogen substituent; and m is an integer of 0 to 2, provided that at least one of R1 and R2 is a radioactive halogen substituent, at least one of A1, A2, A3 and A4 represents a carbon, and R1 binds to a carbon represented by A1, A2, A3 and A4.Type: ApplicationFiled: October 28, 2008Publication date: October 21, 2010Applicant: NIHON MEDI-PHYSICS CO., LTD.Inventors: Shigeyuki Tanifuji, Daisaku Nakamura, Shinya Takasaki
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Patent number: 7795245Abstract: The present invention relates generally to amide group containing pharmaceutical agents, and in particular, to amide containing heterobicyclic metalloprotease inhibitor compounds having the following formulas: wherein R1, R2, R3, and R4 are as defined in the specification. More particularly, the present invention provides a new class of heterobicyclic MMP-13 inhibiting and MMP-3 inhibiting compounds amide containing heterobicyclic compounds, that exhibit an increased potency in relation to currently known MMP-13 and MMP-3 inhibitors.Type: GrantFiled: December 7, 2007Date of Patent: September 14, 2010Assignee: Atlantos Pharmaceuticals Holding, Inc.Inventors: Christoph Steeneck, Christian Gege, Frank Richter, Heiko Kroth, Matthias Hochgurtel, Michael Essors, Joshua Van Veldhuizen, Bert Nolte, Brian M. Gallagher, Jr., Tim Feuerstein, Matthias Schneider, Torsten Arndt, Hongbo Deng, Ralf Biesinger, Xinyuan Wu, Harald Bluhm, Irving Sucholeiki, Arthur G. Taveras
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Publication number: 20100222321Abstract: The instant invention provides for substituted naphthyridine 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: ApplicationFiled: June 7, 2006Publication date: September 2, 2010Inventors: Donna J. Armstrong, Essa H. Hu, Michael J. Kelly, III, Mark E. Layton, Yiwei Li, Jun Liang, Kevin J. Rodzinak, Michael A. Rossi, Philip E. Sanderson, Jiabing Wang
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Patent number: 7781582Abstract: Process for the preparation of unsubstituted or substituted 2-amino-[1,2,4]triazolopyrimidines which comprises combining A) 2-amino-pyrimidine or its derivatives with alkyloxycarbonyl isothiocyanate or aryloxycarbonyl isothiocyanate with B) hydroxyl ammonium salt and a base wherein the reaction is carried out in a polar aprotic organic solvent in the temperature range of from 40 to 150° C.Type: GrantFiled: December 22, 2004Date of Patent: August 24, 2010Assignee: Dow AgroSciences LLCInventor: Joachim Gebhardt
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Patent number: 7776864Abstract: Compounds of formula (I) a tautomer or stereoisomer thereof, or a salt thereof, wherein ring B and the pyrimidine to which it is fused, R4, R5, R6 and R7 have the meanings as given in the description and the claims, are effective inhibitors of the Pi3K/Akt pathway.Type: GrantFiled: August 14, 2008Date of Patent: August 17, 2010Assignee: Bayer Schering Pharma AGInventors: Swen Hölder, Matthias Vennemann, Gerrit Beneke, Armin Zülch, Volker Gekeler, Thomas Beckers, Astrid Zimmermann, Hemant Joshi
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Publication number: 20100197683Abstract: Provided is a novel compound represented by the following formula Wherein each symbol is as defined in the specification, or a salt thereof, which has an angiotensin II receptor antagonistic activity and a peroxisome proliferator-activated receptor ? agonistic activity, and is useful as an agent for the prophylaxis or treatment of circulatory diseases such as hypertension and the like and/or metabolic diseases such as diabetes and the like, and the like.Type: ApplicationFiled: January 29, 2010Publication date: August 5, 2010Inventors: Tsuyoshi Maekawa, Hideyuki Igawa
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Publication number: 20100196357Abstract: The present invention is a method for identifying agents which modulate microRNA activity. The invention involves contacting a cell harboring a microRNA and a microRNA binding sequence, which is operably linked to a nucleic acid molecule encoding a reporter protein, with a test agent and determining whether the test agent increases or decreases the expression of the reporter protein thereby identifying a microRNA modulator. Antagonists identified by this screening assay are provided, as are methods for using the same to inhibit microRNA activity and prevent or treat disease.Type: ApplicationFiled: January 21, 2010Publication date: August 5, 2010Inventors: Qihong Huang, Alexander Deiters, Kiranmai Gumireddy
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Publication number: 20100190762Abstract: Compounds are provided that act as potent antagonists of the CCR2 or CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2 and CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, CCR9-mediated diseases, as controls in assays for the identification of CCR2 antagonists and as controls in assays for the identification of CCR9 antagonists.Type: ApplicationFiled: April 2, 2010Publication date: July 29, 2010Applicant: CHEMOCENTRYX, INC.Inventors: Trevor T. Charvat, Cheng Hu, Anita Melikian, Aaron Novack, Andrew M.K. Pennell, Sreenivas Punna, Edward J. Sullivan, Xuefei Tan, William D. Thomas, Solomon Ungashe, Yibin Zeng
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Publication number: 20100160311Abstract: The present invention relates to azolopyrimidines of the formula I in which the substituents are defined according to the description, to processes and intermediates for preparing these compounds, to compositions comprising them and to their use for controlling phytopathogenic harmful fungi.Type: ApplicationFiled: July 5, 2007Publication date: June 24, 2010Applicant: BASF SEInventors: Jochen Dietz, Wassilios Grammenos, Bernd Müller, Jan Klaas Lohmann, Jens Renner, Sarah Ulmschneider, Marianna Vrettou
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Publication number: 20100145045Abstract: Process for the protection of fish and invertebrates and all their stages of development against mycoses caused by fungi of the genera Saprolegnia, Aphanomyces, Achlyaflagellata and other species important in aquacultures by use of abovementioned, selected fungicides. This use leads to an inhibition or destruction of pathogenic fungi. The composition, comprising at least one fungicide selected from the abovementioned group for use in fish farming and keeping is suitable for the prophylaxis and therapy of diseases of fish in aquaculture, in breeding ponds, breeding tanks, aquariums, natural stretches of game fish waters, ponds, and marine fish farms. Addition to the water and feed and direct application are the associated use forms. The addition of the composition according to the invention to the water decreases fungal infections of spawn and fish.Type: ApplicationFiled: April 10, 2008Publication date: June 10, 2010Applicant: Bayer CropScience AGInventors: Isolde Häuser-Hahn, Klaus Stenzel, Ulrike Wachendorff-Neumann
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Publication number: 20100144744Abstract: Novel compounds are provided which are 1 1-beta-hydroxysteroid dehydrogenase type I inhibitors. 1 1-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 1 1-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: W-L-Z or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein W, L are defined herein and Z is selected from the following bicyclic heteroaryl groups: (a), (b), (c), (d).Type: ApplicationFiled: April 16, 2008Publication date: June 10, 2010Inventors: Jun Li, James J. Li, Stephen P. O'Connor, Haixia Wang, Lawrence J. Kennedy, Jeffrey A. Robl, Lawrence G. Hamann
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Publication number: 20100113441Abstract: The invention relates to substituted imidazopyrimidines and triazolopyrimidines, to methods for the production thereof, and to the use of same for producing medicaments for the treatment and/or prophylaxis of diseases, especially haematological diseases, preferably leucopenia and neutropenia.Type: ApplicationFiled: March 4, 2008Publication date: May 6, 2010Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Stephan Siegel, Andreas Wilmen, Susanne Röhrig, Niels Svenstrup, Mark Jean Gnoth, Stefan Heitmeier, Ulrich Rester, Dmitry Zubov, Jochen Strayle, Michael Sperzel
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Publication number: 20100105903Abstract: The present invention relates to a process for preparing ?-ketonitriles of the general formula I in which R1 is, inter alia, C1-C12-alkyl, C2-C12-alkenyl, C2-C12-alkinyl, C3-C8-cycloalkyl, C3-C8-cycloalkyl-C1-C4-alkyl, phenyl-C1-C4-alkyl, phenoxy-C1-C4-alkyl or benzyloxy-C1-C4-alkyl; R2 is, inter alia, hydrogen, C1-C12-alkyl, C2-C12-alkenyl, C2-C12-alkinyl, C3-C8-cycloalkyl, C3-C8-cycloalkyl-C1-C4-alkyl, phenyl, phenyl-C1-C4-alkyl, phenoxy-C1-C4-alkyl or benzyloxy-C1-C4-alkyl, which comprises reacting a nitrile of the formula II in which R1 has one of the meanings given above with a carboxylic ester of the formula III in which R2 has one of the meanings given above and R3 is C1-C12-alkyl, C1-C4-alkoxy-C1-C4-alkyl, C3-C8-cycloalkyl, C3-C8-cycloalkyl-C1-C4-alkyl, phenyl-C1-C4-alkyl, phenoxy-C1-C4-alkyl or benzyloxy-C1-C4-alkyl, where the reaction is carried out in the presence of a potassium alkoxide and at least 80% of the nitrile of the formula II are added to the reaction under reactionType: ApplicationFiled: February 29, 2008Publication date: April 29, 2010Applicant: BASF SEInventors: Uwe Josef Vogelbacher, Peter Otto, Michael Rack
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Publication number: 20100105704Abstract: The present invention relates to novel {7-(3?,4?-dialkoxyphenyl)-[1,2,4]-triazolo[1,5-a]pyrimidine compounds or pharmaceutically acceptable salts thereof, a process for preparing the same, and pharmaceutical compositions for treating or preventing inflammatory diseases including asthma and chronic obstructive pulmonary disease, arthritis, atopic dermatitis, cancers including leukemia, and degenerative brain diseases including Alzheimer's disease, depression and memory impairment, which comprises the same as an active ingredient.Type: ApplicationFiled: March 7, 2008Publication date: April 29, 2010Applicant: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGYInventors: Dong Ju Jeon, Zaesung No, Jong Hwan Song, Gehyeong Lee, Ikyon Kim, Chang Min Park, Hyae Gyeong Cheon, Young Sik Cho, Jin Sook Song, Myung Ae Bae, Sung-eun Yoo
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Publication number: 20100087452Abstract: To provide a novel pesticide. The present invention provides a pesticide containing a pyridyl-triazolopyrimidine derivative represented by the formula (I) or its salt as an active ingredient: wherein R1 is substitutable alkyl, substitutable cycloalkyl, substitutable alkenyl, substitutable alkynyl, halogen, cyano, aryl, a heterocyclic group which may be substituted by alkyl, OR2, S(O)n#191R3? or NR4R5; R2 is hydrogen, alkyl, alkenyl, alkynyl, haloalkyl, alkoxyalkyl, acetyl or aryl; R3 is alkyl or acetyl; R4 is hydrogen or alkyl; R5 is hydrogen, alkyl or the like; X is alkyl, alkenyl, alkynyl, halogen, haloalkyl, cyano, nitro or the like; m is an integer of from 1 to 4; and n is an integer of from 0 to 2.Type: ApplicationFiled: February 7, 2008Publication date: April 8, 2010Applicant: ISHIHARA SANGYO KAISHA, LTDInventors: Takahiro Haga, Hirohiko Kimura, Masayuki Morita, Tsuyoshi Ueda, Toshihiko Ueki, Kazuhisa Kiriyama, Kotaro Yoshida, Taku Hamamoto
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Publication number: 20100087640Abstract: The present invention relates to a process for preparing aryl-substituted fused pyrimidines of the general formula (I) in which L1 to L5 are H, halogen, CN, NO2, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy etc.; Y1 to Y3 are C—RY or N; RY is H or optionally substituted C1-C4-alkyl or two adjacent RY together form a ring; X is OH, Cl or Br; which comprises (i) the reaction of a 2-phenylmalonate with a compound (III) or a tautomer thereof, in the presence of a suitable base, where the alcohol, released during the reaction, of the formula R—OH is continuously removed from the reaction mixture under reduced pressure; giving a compound of the formula (I) or a salt thereof in which X is OH, and, if X in the compounds of the general formula (I) is chlorine or bromine, (ii) the reaction of the compounds of the formula (I) obtained in step (i) or the salts with a halogenating agent.Type: ApplicationFiled: January 10, 2008Publication date: April 8, 2010Applicant: BASF SEInventors: Bernd Wolf, Volker Maywald, Michael Keil, Manuel Budich, Michael Rack, Manfred Ehresmann
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Publication number: 20100069407Abstract: The present invention relates to compounds of formula (I) and the use of these compounds as pharmaceuticals, e.g. in preventing or treating a CXCR2 receptor mediated condition or disease.Type: ApplicationFiled: November 21, 2007Publication date: March 18, 2010Inventors: Neil John Press, David Porter, Carsten Spanka
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Publication number: 20100069395Abstract: Compounds of formula wherein the residues have various meanings, their pharmaceutical use, pharmaceutical compositions comprising such compounds and methods for preparation and use for the treatment of protein kinase modulation responsive disorders.Type: ApplicationFiled: October 29, 2007Publication date: March 18, 2010Inventors: Patricia Imbach, Pascal Furet
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Patent number: 7678793Abstract: Corticotropin releasing factor (CRF) antagonists of formula I or II: and their use in treating anxiety, depression, and other psychiatric, neurological disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress.Type: GrantFiled: June 29, 2006Date of Patent: March 16, 2010Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Liqi He, Paul Gilligan, Robert Chorvat, Argyrios Georgios Arvanitis
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Publication number: 20100056371Abstract: Azolopyrimidines of the formula I in which the symbols are each defined as specified in the description are suitable for controlling phytopathogenic harmful fungi.Type: ApplicationFiled: January 7, 2008Publication date: March 4, 2010Applicant: BASF SEInventors: Jochen Dietz, Wassilios Grammenos, Bernd Müller, Jan Klaas Lohmann, Jens Renner, Sarah Ulmschneider, Marianna Vrettou