Oxygen Bonded Directly To The Diazine Ring Patents (Class 544/123)
-
Publication number: 20110070193Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.Type: ApplicationFiled: March 17, 2010Publication date: March 24, 2011Applicant: Abbott LaboratoriesInventors: Rolf Wagner, Warren M. Kati, Dachun Liu, Yaya Liu, Kenton L. Longenecker, Clarence J. Maring, John K. Pratt, Todd W. Rockway, Kent D. Stewart, Michael D. Tufano
-
Publication number: 20110071153Abstract: Compounds of the formula I, in which R1, R2, R3?, R3, R4 and D 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: April 24, 2009Publication date: March 24, 2011Applicant: Merck Patent GesellschaftInventors: Dieter Dorsch, Oliver Schadt, Frank Stieber, Andree Blaukat
-
Publication number: 20110053931Abstract: Compounds of Formula (I), and stereoisomers, geometric isomers, tautomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof, are useful for inhibiting receptor tyrosine kinases and for treating hyperproliferative disorders mediated thereby. Methods of using compounds of Formula (I), and stereoisomers, geometric isomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Type: ApplicationFiled: June 8, 2007Publication date: March 3, 2011Inventors: John Gaudino, Steven Armen Boyd, Allison L. Marlow, Tomas Kaplan, Kin Chiu Fong, Jeongbeob Seo, Hongqi Tian, James Blake, Kevin Koch
-
Publication number: 20110034435Abstract: A compound of formula (A); wherein ring A is an aromatic ring or a heteroaromatic ring; R1 is independently halogen, cyano, etc., each of X1, X2 and X3 is CR2 or nitrogen, R2 is independently hydrogens, etc., n is 0, 1, 2, 3 or 4; -D-Y is —O—CH2COOH, etc, and G is a substituted amino, a substituted heterocyclic group, etc, or a pharmaceutical acceptable salt thereof, has activities of opening BK channels.Type: ApplicationFiled: April 8, 2009Publication date: February 10, 2011Applicant: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Yasuyuki Tsuzuki, Miki Hirai
-
Publication number: 20110034433Abstract: The present invention relates to novel 4-(4-cyano-2-thioaryl)dihydropyrimidin-2-one 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 9, 2008Publication date: February 10, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Franz Von Nussbaum, Dagmar Karthaus, Sonja Anlauf, Martina Delbeck, Volkhart Min-Jian Li, Daniel Meibom, Klemens Lustig, Jens Schamberger
-
Publication number: 20110021773Abstract: A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: which is used for preventive and/or therapeutic treatment of a disease caused by abnormal activity of tau protein kinase 1 such as a neurodegenerative diseases (e.g. Alzheimer disease).Type: ApplicationFiled: September 12, 2008Publication date: January 27, 2011Applicants: MITSUBISHI TANABE PHARMA CORPORATION, SANOFI-AVENTISInventors: Kenji Fukunaga, Kazutoshi Watanabe, Pascal Barneoud, Jesus Benavides, Jeremy Pratt
-
Publication number: 20110003988Abstract: A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: which is used for preventive and/or therapeutic treatment of a disease caused by abnormal activity of tau protein kinase 1 such as a neurodegenerative diseases (e.g. Alzheimer disease).Type: ApplicationFiled: September 12, 2008Publication date: January 6, 2011Applicant: SANOFI-AVENTISInventors: Daiki Sakai, Kazutoshi Watanabe
-
Publication number: 20110003798Abstract: The invention provides a novel class of 2,7-naphthyridin derivatives; pharmaceutical compositions comprising such compounds and methods of using such compounds to treat o prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly Syk, ZAP70, KDR, FMS, FLT*, c-Kit, RET, TrkA, TrkB, TrkC-GR-1R, Alk, c-FMS or combinations thereof.Type: ApplicationFiled: January 27, 2009Publication date: January 6, 2011Applicant: IRM LLCInventors: Barun Okram, Tetsuo Uno, Qiang Ding, Yahua Liu, Yunho Jin, Qihui Jin, Xu Wu, Jianwei Che, S. Frank Yan, Xueshi Hao
-
Publication number: 20100324045Abstract: This invention relates to novel compounds of the Formula (I), (Ia), (Ib), (Ic), (Id), (Ie), (If), (Ig), (Ih)1 (Ij), (Ik), (Il1-3). (Im1-3), (In1-3), (Io1-2), (Ip1-6), (Iq1-6), (Ir1-6) and (Is1-2), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.Type: ApplicationFiled: November 7, 2008Publication date: December 23, 2010Inventors: David A. Claremon, Linghang Zhuang, Colin M. Tice, Yuanjie Ye, Wei He, Suresh B. Singh, Zhenrong Xu, Salvacion Cacatian, Wei Zhao
-
Publication number: 20100311754Abstract: Naphthalene-based compounds having linked heterocyclic and aromatic rings capable of inhibiting P38, methods for inhibiting P38 in vivo or in vitro, diagnostics for determining activity in the treatment of P38 and/or cytokine-associated conditions and methods for treating conditions associated with P38 activity or cytokine activity; more particularly naphthalene-based compounds of Formula (I) having a morpholine heterocyclic ring, and methods of use thereof.Type: ApplicationFiled: August 11, 2010Publication date: December 9, 2010Applicant: ARQULE, INC.Inventors: Mark A. Ashwell, Yanbin Liu, Syed Ali, Jason Hill, Woj Wrona
-
Patent number: 7829560Abstract: 1,4 disubstituted napthylenes, of formula (I), are disclosed. These compounds may be useful in treating cell-proliferative diseases.Type: GrantFiled: July 8, 2005Date of Patent: November 9, 2010Assignee: Arqule, Inc.Inventors: Mark A. Ashwell, Yanbin Liu, Syed Ali, Jason Hill, Woj Wrona
-
Publication number: 20100280030Abstract: Compounds of the formula (I), in which R1, R2, R3, R3?, R4, R4?, E, E?, E? and E?? 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: May 8, 2008Publication date: November 4, 2010Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Oliver Schadt, Dieter Dorsch, Frank Stieber, Andree Blaukat
-
Patent number: 7820660Abstract: N-substituted 5-hydroxypyrimidin-6-one-4-carboxamides of formula: are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R1, R2, R3 and R4 are defined herein. These compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.Type: GrantFiled: June 20, 2008Date of Patent: October 26, 2010Assignee: Instituto di Ricerche di Biologia Molecolare P. Angeletti S.p.A.Inventors: Benedetta Crescenzi, Cristina Gardelli, Ester Muraglia, Emanuela Nizi, Federica Orvieto, Paola Pace, Giovanna Pescatore, Alessia Petrocchi, Marco Poma, Michael Rowley, Rita Scarpelli, Vincenzo Summa
-
Publication number: 20100249405Abstract: The present invention relates to novel IAP inhibitor compounds of formula I:Type: ApplicationFiled: December 7, 2007Publication date: September 30, 2010Inventors: Zhuoliang Chen, Run-Ming David Wang, Ming Chen, Christopher Sean Straub, Leigh Zawel
-
Patent number: 7795271Abstract: Disclosed are compounds Formula I and pharmaceutically acceptable salts thereof, wherein R1, R2, R4, and R5 are defined herein. These compounds are useful for treating diseases and conditions caused or exacerbated by unregulated p38 MAP Kinase and/or TNF activity. Pharmaceutical compositions containing the compounds, methods of preparing the compounds and methods of treatment using the compounds are also disclosed.Type: GrantFiled: May 4, 2009Date of Patent: September 14, 2010Assignee: Pharmacia CorporationInventor: Richard C. Durley
-
Publication number: 20100210637Abstract: Provided are compounds of a formula (I) and their pharmaceutically-acceptable salts: wherein X1, X2 and X3 each independently represent N or CH; W represents the following formula (II): or the following formula (III): Y represents a group of a formula (IV): The compounds have a histamine-H3 receptor antagonistic or inverse-agonistic activity and are useful for remedy and/or prevention of obesity, diabetes, hormone secretion disorders, sleep disorders, etc.Type: ApplicationFiled: August 13, 2009Publication date: August 19, 2010Inventors: Norikazu Ohtake, Akira Naya, Yuji Haga, Makoto Jitsuoka, Takuya Suga, Ryo Yoshimoto, Shigeru Tokita, Akio Kanatani
-
Publication number: 20100209488Abstract: The invention provides compositions, e.g., small molecules, that disrupt the activity of protein kinases, including constitutively activated protein kinases, such as kinases constitutively activated through mutations, and kinases in their native inactivated state, and methods for making and using them. In one aspect, compositions of the invention bind a protein kinase in its inactive conformation involving the conserved asparagine-phenylalanine-glycine residue motif, or “Asp-Phe-Gly” or “DFG” motif, of the activation loop in the allosteric binding site. The small molecule protein kinase inhibitors of the invention comprise or are derivatives or analogs of oxadiazoles, thiadiazoles, oxazoles, thiazoles, arylamides, quinolones, pyrazoles, pyrazolones, imides, pyrolles, imidazoles and/or triazoles.Type: ApplicationFiled: July 15, 2008Publication date: August 19, 2010Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Wolfgang Wrasidlo, Eric Murphy, David Cheresh
-
Publication number: 20100135954Abstract: A compound having Formula I or II (Formula I) or (Formula II), or a pharmaceutically acceptable salt thereof, wherein X, Z, R1, R2, R11 and R12 are as defined in the specification; pharmaceutical compositions thereof; and methods of use thereof.Type: ApplicationFiled: April 25, 2008Publication date: June 3, 2010Applicant: EXELIXIS, INC.Inventors: Amy L. Tsuhako, Naing Aay, S. David Brown, Wai Ki Vicky Chan, Hongwang Du, Ping Huang, Brian Kane, Patrick Kearney, Moon Hwan Kim, Elena S. Koltun, Michael Pack, Wei Xu, Peiwen Zhou
-
Publication number: 20100130490Abstract: Benzoxazole and benzothiazole compounds and their oxides, esters, prodrugs, solvates, and pharmaceutically acceptable salts thereof are disclosed. Compositions of the compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier, and uses of the compounds, either alone or in combination with at least one additional therapeutic agent are also disclosed. The embodiments are useful for inhibiting cellular proliferation, inhibiting the growth and/or metathesis of tumors, treating or preventing cancer, treating or preventing degenerating bone diseases such as rheumatoid arthritis, and/or inhibiting molecules such as CSF 1R.Type: ApplicationFiled: May 20, 2008Publication date: May 27, 2010Inventors: Simon C. Ng, Keith B. Pfister, Martin Sendzik, James Sutton, Allan S. Wagman, Marion Wiesmann
-
Publication number: 20100113775Abstract: A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof: wherein each R1 represents hydrogen atom or the like; X represents oxygen atom or the like; A represents a C3-C7 cycloalkyl group, a C6-C10 aryl group or a heterocyclic group; R6 represents a halogen atom or the like; s represents 0 or an integer of 1 to 5; Q represents a pyridine ring which may be substituted or pyrimidine ring; and R2 represents hydrogen atom or the like, which is used for preventive and/or therapeutic treatment of a disease caused by abnormal activity of tau protein kinase 1 such as a neurodegenerative diseases (e.g. Alzheimer disease).Type: ApplicationFiled: December 26, 2007Publication date: May 6, 2010Applicants: MITSUBISHI TANABE PHARMA CORPORATION, SANOFI-AVENTISInventors: Kazutoshi Watanabe, Toshiyuki Kohara, Kenji Fukunaga, Fumiaki Uehara
-
Publication number: 20100113444Abstract: The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I), (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.Type: ApplicationFiled: June 22, 2007Publication date: May 6, 2010Inventors: Kevin J. Duffy, Duke M. Fitch, Jian Jin, Ronggang Liu, Antony N. Shaw, Kenneth Wiggall
-
Publication number: 20100093998Abstract: A novel adenine compound represented by the formula (1): wherein A represents an (un)substituted aromatic carbocycle or (un)substituted aromatic heterocycle; L1 and L2 each independently represents straighted or branched alkylene, etc.; R1 represents halogen, (un)substituted alkyl, (un)substituted alkenyl, (un)substituted alkynyl, (un)substituted cycloalkyl, (un)substituted aryl, or (un)substituted heteroaryl; R2 and R3 each independently represents hydrogen, or (un)substituted alkyl, (un)substituted alkenyl, (un)substituted alkynyl, (un)substituted cycloalkyl, (un)substituted saturated heterocycle, (un)substituted aryl, or (un)substituted heteroaryl, or R2 combines together with L2 or R3 to form (un)substituted 4- to 8-membered nitrogen-containing saturated heterocycle; X is oxygen, sulfur, SO, SO2, NR7, NR7CO wherein R7 is hydrogen or alkyl, or a single bond; provided that X is a single bond when R1 is halogen, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: March 19, 2008Publication date: April 15, 2010Applicants: Dainippon Sumitomo Pharma Co., Ltd., AstraZeneca AktiebolagInventors: Yoshiaki Isobe, Tomoaki Nakamura
-
Patent number: 7696204Abstract: Pyrimidines of formula (I): wherein R1 to R4, X and Y are defined in the specification are inhibitors of P13K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behavior associated with P13 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.Type: GrantFiled: October 11, 2006Date of Patent: April 13, 2010Assignees: Ludwig Institute for Cancer Research, Cancer Research Technology Limited, The Institute of Cancer Research: Royal Cancer Hospital, Astellas Pharma, Inc., F. Hoffmann-La Roche AGInventors: Edward McDonald, Jonathan M Large, Stephen J Shuttleworth
-
Publication number: 20100075944Abstract: A compound represented by the following formula, or a salt thereof or a hydrate of the foregoing, has excellent hepatocyte growth factor receptor (HGFR) inhibitory activity, and exhibits anti-tumor activity, angiogenesis inhibitory activity, and cancer metastasis inhibitory activity. R1 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; R2 and R3 represent hydrogen; R4, R5, R6, and R7 may be the same or different and each represents hydrogen, halogen, C1-6 alkyl or the like; R8 represents hydrogen or the like; R9 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; n represents an integer of 1 or 2; X represents —CH?, nitrogen or the like.Type: ApplicationFiled: September 14, 2009Publication date: March 25, 2010Inventors: Tomohiro MATSUSHIMA, Keiko Takahashi, Setsuo Funasaka, Hiroshi Obaishi, Shuji Shirotori
-
Publication number: 20100056512Abstract: Pyrimidine compounds of the following formula: wherein R1, R2, R3, R4, R5, X, Q1, Q2, and Q3 are defined herein. Also disclosed is a method of treating cancer with one of these compounds.Type: ApplicationFiled: August 29, 2008Publication date: March 4, 2010Applicant: Hutchison MediPharma Enterprises LimitedInventors: Wei-Guo Su, Hong Jia, Rick B. Ye, Yang Sai
-
Publication number: 20100056526Abstract: A compound represented by the formula (I): wherein R1 is an oxo group, ?N—R or the like; a group represented by the formula: is a group represented by the formula: R2 is a group represented by the formula: or a salt thereof. The compound of the present invention is useful as a drug for the prophylaxis or treatment of circulatory diseases, metabolic diseases and/or central nervous system diseases.Type: ApplicationFiled: November 21, 2007Publication date: March 4, 2010Inventors: Takanobu Kuroita, Hiroki Sakamoto, Hideyuki Igawa, Minoru Sasaki, Kouhei Asano, Tsuyoshi Maekawa
-
Publication number: 20100048547Abstract: Phosphatidylinositol (PI) 3-kinase inhibitor compounds, their pharmaceutically acceptable salts, and prodrugs thereof; compositions of the new compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of diseases characterized by the abnormal activity of growth factors, protein serine/threonine kinases, and phospholipid kinases, including proliferative diseases, inflammatory and obstructive airways diseases, allergic conditions, autoimmune and cardiovascular diseases.Type: ApplicationFiled: February 6, 2008Publication date: February 25, 2010Inventors: Gordana Atallah, Sarah Bartulis, Matthew Burger, Hanne Merritt, Simon Ng, Zhi-Jie Ni, Sabina Pecchi, Keith B. Pfister, Aaron Smith, Charles Voliva, Allan Wagman, Yanchen Zhang
-
Patent number: 7655649Abstract: The present invention is directed to compounds which contain substituted pyridazines and pyrimidines moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.Type: GrantFiled: April 5, 2005Date of Patent: February 2, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Mark T. Bilodeau, Peter C. Chua, Nicholas D. P. Cosford, Jacob M. Hoffman, Johnny Yasuo Nagasawa
-
Publication number: 20100022537Abstract: This invention relates to novel heterocyclic derivatives, processes for their preparation, and their use in medicaments, especially for the treatment of chronic obstructive pulmonary diseases, acute coronary syndrome, acute myocardial infarction and heart failure development.Type: ApplicationFiled: July 27, 2009Publication date: January 28, 2010Applicant: Bayer Healthcare AGInventors: Heike Gielen-Haertwig, Volkhart Min-Jian Li, Ulrich Rosentreter, Karl-Heinz Schlemmer, Swen Allerheiligen, Leila Telan, Lars Bärfacker, Jörg Keldenieh, Mary F. Fitzgerald, Kevin Nash, Barbara Albrecht, Dirk Meurer
-
Publication number: 20100022538Abstract: This present disclosure is related to the field of 5-fluoro pyrimidines and their derivatives and to the use of these compounds as fungicides.Type: ApplicationFiled: August 7, 2009Publication date: January 28, 2010Applicant: Dow AgroSciences LLCInventors: Timothy A. Boebel, Kristy Bryan, Carla J.R. Klittich, Beth Lorsbach, Timothy P. Martin, W. John Owen, Mark A. Pobanz, Michael T. Sullenberger, Jeffery D. Webster, Chenglin Yao
-
Publication number: 20100016252Abstract: Disclosed are Mannich base N-oxides of drugs containing acidic N—H groups. Pharmaceutical compositions comprising a therapeutically effective amount of Mannich base N-oxides, or a N-oxide rearrangement product, pharmaceutically acceptable salt or prodrug thereof, are also disclosed. Further, disclosed are methods of using the compounds, alone or in combination with one or more other active agents or treatments.Type: ApplicationFiled: September 21, 2009Publication date: January 21, 2010Applicant: State of Oregon Acting By and Through The Oregon State Board of Higher Education On Behalf of The UInventors: John F.W. Keana, Paul Westberg, John Curd, Alshad S. Lalani
-
Publication number: 20100016319Abstract: This invention relates to a pharmaceutical comprising as an effective ingredient an arylmethylene urea exemplified by the following formula: or a pharmaceutically acceptable salt thereof. The arylmethylene urea and the pharmaceutically acceptable salts thereof are useful for therapy or prophylaxis of inflammatory bowel disease and overactive bladder.Type: ApplicationFiled: November 29, 2006Publication date: January 21, 2010Applicant: TORAY INDUSTRIES, INC. a corporation of JapanInventors: Michihiro Ohno, Hideki Inoue, Shinnosuke Hayashi, Mie Kaino, Sunao Hara, Satoru Yoshikawa
-
Publication number: 20100010003Abstract: The invention relates to new pyrimidine compounds of formula (1) wherein the variables have the meaning as indicated in the claims; in free form and in salt form; and optionally the enantiomers and geometrical isomers thereof. The compounds of formula (1) are useful in the control of parasites, in particular ectoparasites, in and on warmblooded animals.Type: ApplicationFiled: July 17, 2007Publication date: January 14, 2010Inventors: Noelle Gauvry, Francois Pautrat, Jacques Bouvier, Jorg Fruchtel, Beatrice Bapst, Sandra Schorderet Weber
-
Publication number: 20090306076Abstract: The present invention is directed to morpholine carboxamide compounds which are antagonists of prokineticin receptors, in particular antagonists of prokineticin 2 receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which prokineticin receptors are involved. 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 prokineticin receptors are involved.Type: ApplicationFiled: December 4, 2006Publication date: December 10, 2009Inventors: Wayne J. Thompson, Jeffrey Y. Melamed
-
Patent number: 7625930Abstract: This invention relates to a group of novel chelating agents, novel chelates, biomolecules labeled with said chelates or chelating agents as well as solid supports conjugated with said chelates, chelating agents or labeled biomolecules. Especially the invention relates to novel chelating agents useful in solid phase synthesis of oligonucleotides or oligopeptides and the oligonucleotides and oligopeptides so obtained.Type: GrantFiled: December 6, 2004Date of Patent: December 1, 2009Assignee: Walloc OyInventors: Jari Hovinen, Veli-Matti Mukkala, Harri Hakala, Jari Peuralahti
-
Publication number: 20090247523Abstract: The present invention relates to the use of carboxamide 4-[(4-pyridyl)amino]-pyrimidines as inhibitors of HCV replication as well as their use in pharmaceutical compositions aimed to treat or combat HCV infections.Type: ApplicationFiled: October 4, 2007Publication date: October 1, 2009Inventors: Pierre Jean-Marie Bernard Raboisson, Oliver Lenz, Tse-I Lin, Kenneth Simmen
-
Publication number: 20090239864Abstract: A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof: wherein R1 represents a C1-C12 alkyl; R2 represents a hydrogen atom or the like; R3 represents a halogen or the like; q represents an integer of 1 to 7; R4 represents a halogen or the like; p represents 0 or an integer of 1 to 5; R5 represents a C6-C10 aryl, a heterocycle or the like; and X represents oxygen, NH, or the like, which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).Type: ApplicationFiled: September 29, 2005Publication date: September 24, 2009Applicants: MITSUBISHI PHARMA CORPORATION, SANOFI-AVENTISInventors: Kazutoshi Watanabe, Kenji Fukunaga, Toshiyuki Kohara, Fumiaki Uehara, Shinsuke Hiki, Satoshi Yokoshima
-
Patent number: 7589090Abstract: Compounds and methods for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist, the compounds being of formula (I): wherein R1, R2, R3 and R4 are as defined herein.Type: GrantFiled: February 27, 2008Date of Patent: September 15, 2009Assignee: Roche Palo Alto LLCInventors: Michael Patrick Dillon, Alam Jahangir
-
Publication number: 20090221584Abstract: Compounds, compositions and methods are provided that are useful in the treatment or prevention of a condition or disorder mediated by PPAR? or PPAR?. In particular, the compounds of the invention modulate the function of PPAR? or PPAR?. The subject methods are particularly useful in the treatment and/or prevention of diabetes, obesity, hypercholesterolemia, rheumatoid arthritis and atherosclerosis.Type: ApplicationFiled: November 12, 2008Publication date: September 3, 2009Inventors: Philippe Bergeron, Christopher N. Farthing, Stuart D. Jones, John W. Liebeschuetz, Sarah E. Lively, Lawrence R. McGee, Sharon McKendry, David Sheppard, Stephen C. Young
-
Publication number: 20090221579Abstract: This invention relates to novel compounds having the structural formula Ia or formula Ib: Ia Ib and their pharmaceutically acceptable salts, tautomers or in vivo hydrolysable precursors, compositions and methods of use thereof. These novel compounds provide a treatment or prophylaxis of A? related pathologies such as cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.Type: ApplicationFiled: October 14, 2005Publication date: September 3, 2009Inventors: Jeffrey Scott Albert, Don Andisik, James Arnold, Dean Brown, Owen Callaghan, James Campbell, Robin Arthur Ellis Carr, Gianni Chessari, Miles Stuart Congreve, Phil Edwards, James R. Empfield, Martyn Frederickson, Gerard M. Koether, Jennifer Krumrine, Russ Mauger, Christopher William Murray, Sahil Patel, Mark Sylvester, Scott Throner
-
Publication number: 20090203647Abstract: This present disclosure is related to the field of 5-fluoro pyrimidines and their derivatives and to the use of these compounds as fungicides.Type: ApplicationFiled: January 22, 2009Publication date: August 13, 2009Applicant: DOW AGROSCIENCES LLCInventors: Zoltan L. Benko, Timothy Boebel, Nneka T. Breaux, Kristy Bryan, George E. Davis, Jeffrey B. Epp, Beth Lorsbach, Timothy P. Martin, Kevin G. Meyer, Bassam S. Nader, W. J. Owen, Mark A. Pobanz, James M. Ruiz, Frisby D. Smith, Michael T. Sullenberger, Jeffery D. Webster, Chenglin Yao, David H. Young
-
Publication number: 20090176784Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.Type: ApplicationFiled: September 17, 2008Publication date: July 9, 2009Applicant: ABBOTT LABORATORIESInventors: Pamela L. Donner, John T. Randolph, Allan C. Krueger, David A. Betebenner, Douglas K. Hutchinson, Dachun Liu, Yaya Liu, Kenton L. Longenecker, Clarence J. Maring, John K. Pratt, Todd W. Rockway, Kent D. Stewart, Rolf Wagner, Shuang Chen, Yi Gao, John E. Hengeveld, Rodger F. Henry, Xiaochun Lou, Geoff G.Z. Zhang
-
Publication number: 20090156804Abstract: The present invention relates to a production method of an optically active morpholine compound represented by the formula 10, which includes the following steps: wherein each symbol is as defined in the specification. The present invention also relates to a production method of an compound represented by the formula 55, which includes the following steps: wherein each symbol is as defined in the specification. According to the production method of the present invention, an optically active 2-aryl-substituted morpholine compound and 3-oxo-3-(pyrimidin-4-yl)propionate, which are important as starting materials for synthesizing 2-(2-arylmorpholin-4-yl)-1-methyl-1H-[4,4?]bipyrimidinyl-6-one having a tau protein kinase 1 inhibitory activity and useful as a therapeutic drug for Alzheimer's disease and the like, can be produced in a high yield by an industrially advantageous method.Type: ApplicationFiled: July 21, 2006Publication date: June 18, 2009Applicants: MITSUBISHI TANABE PHARMA CORPORATION, SANOFI-AVENTISInventors: Masahiro Okuyama, Fumiaki Uehara, Hiroshi Iwamura, Kazutoshi Watanabe
-
Publication number: 20090156592Abstract: Disclosed are compounds of Formulae 1, 1A, 1B and 1C including all geometric and stereoisomers, N-oxides, and salts thereof, wherein R1, R2, R4a1, R4a2, A, Aa, G, M, W, Z1, Z3, X, J, J1 and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.Type: ApplicationFiled: July 27, 2007Publication date: June 18, 2009Applicant: E.I. DU PONT DE NEMOURS AND COMPANYInventors: Robert James Pasteris, Mary Ann Hanagan, Rafael Shapiro
-
Publication number: 20090143384Abstract: The invention concerns pyrimidine derivatives of Formula (I) wherein each of Qa, G1, G2, q, R3, r, R4, X1 and Qb have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the production of an anti-proliferative effect in a warm-blooded animal such as man.Type: ApplicationFiled: July 7, 2005Publication date: June 4, 2009Applicant: ASTRAZENECA UK LIMITEDInventor: Martin Pass
-
Publication number: 20090137557Abstract: Novel calcilytic compounds, pharmaceutical compositions, methods of synthesis and methods of using them are provided.Type: ApplicationFiled: November 21, 2006Publication date: May 28, 2009Inventors: Thomas Wen Fu Ku, Hong Lin, Juan I. Luengo, Robert W. Marquis Jr., Joshi M. Ramanjulu, Robert Trout, Dennis S. Yamashita
-
Publication number: 20090131437Abstract: The invention relates to compounds of the formula (I), their use as kinase inhibitors, new pharmaceutical formulations comprising said compounds, said compounds for use in the diagnostic or therapeutic treatment of warm-blooded animals, especially humans, their use in the treatment of diseases or for the manufacture of pharmaceutical formulations useful in the treatment of diseases that respond to modulation of kinase activity, methods of treatment comprising administration of said compounds to a warm-blooded animal, especially a human, and processes for the manufacture of said compounds.Type: ApplicationFiled: January 3, 2006Publication date: May 21, 2009Applicants: CORIUM INTERNATIONAL, INC., A.V. TOPCHIEV INSTITUTE OF PETROCHEMICAL SYNTHESISInventors: Pascal Furet, Georg Martiny-Baron, Clive McCarthy, Vittorio Rasetti, Andrea Vaupel
-
Publication number: 20090124596Abstract: The present invention provides a compound of a formula (I): wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a PDE4 mediated disease state.Type: ApplicationFiled: January 10, 2008Publication date: May 14, 2009Inventors: Roger Victor Bonnert, Frank Burkamp, Rhona Jane Cox, Simon De Sousa, Mark Dickinson, Simon Fraser Hunt, Premji Meghani, Austen Pimm, Hitesh Jayantilal Sanganee
-
Publication number: 20090082351Abstract: The present invention relates to 2,5-disubstituted-4-pyrimidinyl-substituted-phenyl-amidine derivatives of formula (I) in which the substituents are as in the description, notably to 2,5-dialkyl-4-pyrimidinyl-substituted-phenyl-amidine derivatives, their process of preparation, their use as fungicide or insecticide active agents, particularly in the form of fungicide or insecticide compositions, and methods for the control of phytopathogenic fungi or damaging insects, notably of plants, using these compounds or compositions.Type: ApplicationFiled: September 12, 2006Publication date: March 26, 2009Applicant: Bayer CropScience AGInventor: Klaus Kunz
-
Publication number: 20090075939Abstract: The invention is related to compounds of Formula (I): or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.Type: ApplicationFiled: June 26, 2008Publication date: March 19, 2009Inventors: Gong-Xin He, Choung U. Kim, Michael L. Mitchell, Lianhong Xu