The Additional Hetero Ring Contains Nitrogen As The Only Ring Hetero Atom [e.g., 2-(2-imidazolin-2-yl)-benzimidazole; 1-p-chlorophenyl-3- Pyrrolidin-1- Yl-propyl Benzimidazolone, Etc.] Patents (Class 548/306.1)
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Publication number: 20100305140Abstract: Compounds of formula I or pharmaceutically acceptable salts thereof: wherein X, A, R1, R2, R3 and R4 are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.Type: ApplicationFiled: June 11, 2007Publication date: December 2, 2010Applicant: AstraZeneca ABInventors: William Brown, Daniel Page, Sanjay Srivastava, Christopher Walpole, Zhong-Yong Wei, Hua Yang
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Publication number: 20100297038Abstract: The present invention refers to compounds with cooling properties, the compound are of formula (I), wherein R1 is selected from the list consisting of C1-C3 alkyl, —SCH3, and —NH2, and —CHR?OR? wherein R? and R? are independently selected from hydrogen, methyl and ethyl; R2 is selected from the list consisting of hydrogen, C1-C3 alkyl, and a halide; and I) A is wherein R is selected from hydrogen, —OR11 wherein R11 is selected from hydrogen, and C1-C3 alkyl; halide; —NO2; —CN; —C(O)NH2; and —C(O)OR12 wherein R12 is selected from hydrogen, and C1-C3 alkyl; and X is selected from the list consisting of —CH2—, —C(O)—, and —C(O)NHCH2—; or II) A is wherein n is 0 or 1.Type: ApplicationFiled: January 16, 2009Publication date: November 25, 2010Applicant: Givaudan S.A.Inventors: Stefan Michael Furrer, Thomas Scott McCluskey
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Publication number: 20100284970Abstract: The present invention relates to new benzimidazole modulators of H1 receptor activity and/or inhibitors of NS4B protein activity, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: April 9, 2010Publication date: November 11, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Tadimeti Rao, Chengzhi Zhang
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Publication number: 20100273831Abstract: The present invention is related to novel benzimidazole compounds of formula (I) having cannabinoid receptor agonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals, in particular humans.Type: ApplicationFiled: December 16, 2008Publication date: October 28, 2010Inventors: Henricus Jacobus Maria Gijsen, Bie Maria Pieter Verbist, Michel Surkyn
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Patent number: 7820659Abstract: The present invention discloses novel compounds of Formula I: (I) having 11?-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11?-HSD type 1 activity.Type: GrantFiled: April 19, 2007Date of Patent: October 26, 2010Assignee: Eli Lilly and CompanyInventors: Ashraf Saeed, Owen Brendan Wallace, Yanping Xu, Thomas Edward Mabry, Rebecca Lynn Rezac Guenther, Nancy June Snyder
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Publication number: 20100267698Abstract: This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula I The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABAA receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Novel processes for preparing compounds of Formula I are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABAA receptors in tissue sections.Type: ApplicationFiled: January 5, 2010Publication date: October 21, 2010Inventors: Guiying Li, Pamela Albaugh, Kevin S. Currie, Guolin Cai, Linda M. Gustavson, Kyungae Lee, Alan Hutchison, George D. Maynard, Jun Yuan, Ling Hong Xie, Manuka Ghosh, Nian Liu, George P. Luke, Scott Mitchell, Martin Patrick Allen, Spiros Liras
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Publication number: 20100261717Abstract: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein W, R1, R2, R7, R8, R9 and R10 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. Also disclosed is a method of using such compounds in the treatment of hyperproliferative diseases in mammals, and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: June 28, 2010Publication date: October 14, 2010Applicant: ARRAY BIOPHARMA INC.Inventors: Eli M. Wallace, Joseph P. Lyssikatos, Allison L. Marlow, T. Brian Hurley
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Patent number: 7807697Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands and methods for using such compounds and compositions.Type: GrantFiled: January 29, 2008Date of Patent: October 5, 2010Assignee: Abbott LaboratoriesInventors: Marlon D. Cowart, Yi-Yin Ku, Sou-Jen Chang, Dilinie P. Fernando, Timothy A. Grieme, Robert J. Altenbach
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Publication number: 20100249085Abstract: This invention relates to novel heteroaryl substituted pyrazole compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients or therapeutic measures.Type: ApplicationFiled: May 8, 2008Publication date: September 30, 2010Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Stephen Boyer, Michael Härter, Philip L. Wickens, Manoj Patel, Ellalahewage Sathyajith Kumarasinghe, Ajay Kumar Bhargava, Karl-Heinz Thierauch, Hartmut Beck, Susanne Greschat, Peter Ellinghaus, Patrick Paulus, Holger Hess-Stumpp
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Publication number: 20100249132Abstract: Compounds of the formula (I), in which R1, D, E, L, Q, X and q have the meanings indicated in Claim 1, can and be employed for the treatment of tumours.Type: ApplicationFiled: September 9, 2008Publication date: September 30, 2010Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Melanie Schultz, Kai Schiemann, Gerard Botton, Andree Blaukat, Ingo Kober
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Publication number: 20100240720Abstract: The disclosure provides compounds and compositions, and methods of using these compounds and compositions, for the targeted delivery of chemotherapeutic agents.Type: ApplicationFiled: March 19, 2010Publication date: September 23, 2010Applicant: Burnham Institute for Medical ResearchInventor: Maurizio Pellecchia
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Patent number: 7799806Abstract: This invention relates to compounds of the formula wherein A, R1 to R3 are as defined in the claims and G is benzoimidazole, quinoxaline, benzotriazole, dihydro-imidazo[4,5-c]pyridinone and dihydro-isoindolone group as defined in the specification, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5 such as diabetes mellitus.Type: GrantFiled: March 24, 2008Date of Patent: September 21, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Konrad Bleicher, Andreas D. Christ, Rainer E. Martin, Peter Mohr
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Publication number: 20100233122Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: March 1, 2010Publication date: September 16, 2010Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
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Publication number: 20100234425Abstract: Compounds of Formula (I) inhibit the PARP enzyme and are useful for treating a disease or a disorder associated with PARP. Also disclosed are pharmaceutical compositions comprising compounds of Formula (I), methods of treatment comprising compounds of Formula (I), and methods of inhibiting the PARP enzyme comprising compounds of Formula (I).Type: ApplicationFiled: April 22, 2010Publication date: September 16, 2010Applicant: ABBOTT LABORATORIESInventors: Gui-Dong Zhu, Virajkumar B. Gandhi, Jianchun Gong, Thomas D. Penning, Vincent L. Giranda, Sheela Thomas
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Publication number: 20100233116Abstract: The present invention provides heterocyclic derivatives hat modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.Type: ApplicationFiled: August 13, 2007Publication date: September 16, 2010Inventors: Natalie Dales, Julia Fonarev, Jianmin Fu, Rajender Kamboj, Vishnumurthy Kodumuru, Shifeng Liu, Natalia Pokrovskaia, Vandna Raina, Shaoyi Sun, Zaihui Zhang
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Publication number: 20100215616Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: ApplicationFiled: February 8, 2010Publication date: August 26, 2010Inventors: Jeffrey Lee Romine, Denis R. St. Laurent, Makonen Belema, Lawrence B. Snyder, Lawrence G. Hamann, John F. Kadow, Jayne Kapur, Andrew C. Good, Omar D. Lopez, Rico Lavoie, John A. Bender
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Publication number: 20100216806Abstract: Compounds of formula are HDAC inhibitors. These compounds are useful for the treatment of diseases such as cancer in humans or animals.Type: ApplicationFiled: February 19, 2010Publication date: August 26, 2010Inventors: Chungen Liang, Guozhi Tang, Jason Christopher Wong, Xihan Wu, Zhenshan Zhang
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Patent number: 7781438Abstract: A compound of formula (I) wherein R, R1, and R2, ring A and ring B are as defined in the specification, processes for their production, their uses, in particular in transplantation, and pharmaceutical compositions containing them.Type: GrantFiled: July 10, 2006Date of Patent: August 24, 2010Assignee: Novartis AGInventors: Jürgen Wagner, Maurice Van Eis, Peter Von Matt, Jean-Pierre Evenou, Walter Schuler
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Patent number: 7781596Abstract: The invention relates to novel 2-phenylbenzimidazoles of general formula (I) or (II), wherein the radicals have the meanings cited in the description, and to their tautomeric forms, possible enantiomeric and diastereomeric forms, to their prodrugs, and to possible physiologically compatible salts. The invention also relates to the production of said compounds and to their use.Type: GrantFiled: October 28, 1999Date of Patent: August 24, 2010Assignee: Abbott LaboratoriesInventors: Wilfried Lubisch, Michael Kock, Thomas Höger
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Patent number: 7763644Abstract: The present invention relates to imidazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: GrantFiled: June 11, 2007Date of Patent: July 27, 2010Assignee: UCB Pharma, S.A.Inventors: Benoît Kenda, Philippe Michel, Yannick Quesnel
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Publication number: 20100179147Abstract: Benzimidazole compounds of formula (I): wherein R1, R2, R3, R4, R5, X, Y, Z1, and Z2 are defined herein. Also disclosed is a method for treating cancer with benzimidazole compounds.Type: ApplicationFiled: December 10, 2009Publication date: July 15, 2010Inventors: Chih-Shiang Chang, Jih-Hwa Guh, Che-Ming Teng, Shiow-Lin Pan, Wei-Ling Chang, Ju-Fang Liu, Kai-Wei Chang, Sheng-Chu Kuo
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Publication number: 20100173898Abstract: The present invention discloses and claims a series of substituted N-phenyl-pyrrolidinylmethylpyrrolidine amides of formula (I). Wherein R, R1, R2, R3 and R4 are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted pyrrolidinylmethylpyrrolidine amides and intermediates therefor.Type: ApplicationFiled: March 15, 2010Publication date: July 8, 2010Applicant: SANOFI-AVENTISInventors: Werngard CZECHTIZKY, Zhongli GAO, William J. HURST, Lothar SCHWINK, Siegfried STENGELIN
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Publication number: 20100168088Abstract: The present invention relates to a compound of formula I wherein Ar1, Ar2, R1, R2, R3, n, o, and p are as described herein or to a pharmaceutically active salt, to all stereoisomeric forms, including individual diastereoisomers and enantiomers as well as to racemic and non-racemic mixtures thereof. Compounds of the invention are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).Type: ApplicationFiled: October 2, 2009Publication date: July 1, 2010Inventors: Caterina Bissantz, Philippe Jablonski, Henner Knust, Matthias Nettekoven, Angélique Patiny-Adam, Hasane Ratni, Claus Riemer
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Patent number: 7737166Abstract: A 1,6-?-glucan synthetase inhibitor is provided, having potent growth inhibition and having excellent safety. A compound is provided, capable of expressing in a wide spectral range and specifically or selectively, an antifungal effect based on its functional mechanism of 1,6-?-glucan synthesis inhibition. Also provided is a drug, a salt or hydrate thereof, especially an antifungal that contains the compound.Type: GrantFiled: August 16, 2006Date of Patent: June 15, 2010Assignee: Daiichi Sankyo Company, LimitedInventors: Katsuhiro Kawakami, Kazuo Kanai, Takao Horiuchi, Hiroshi Takeshita, Syozo Kobayashi, Yuichi Sugimoto, Issei Achiwa, Junichi Kuroyanagi
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Publication number: 20100136136Abstract: This invention relates to the field of protein tyrosine kinases and inhibitors thereof. In particular, the invention relates to inhibitors of JAK-2, pharmaceutical compositions of the compounds for inhibiting JAK-2, methods of inhibiting JAK-2 in a cell, comprising contacting a cell in which inhibition of JAK-2 is desired with a compound or pharmaceutical composition comprising a compound according to the invention. The also comprises methods of treating a disease or condition that involves JAK-2 comprising administering to a patient a pharmaceutical composition comprising a compound according to the invention.Type: ApplicationFiled: September 28, 2007Publication date: June 3, 2010Applicant: EXELIXIS, INC.Inventors: Adam Antoni Galan, Jeff Chen, Hongwang Du, Timothy Forsyth, Tai Phat Huynh, Henry William Beecroft Johnson, Patrick Kearney, James W. Leahy, Matthew Sangyup Lee, Grace Mann, Brian Hugh Ridgway, Craig Stacy Takeuchi, Peiwen Zhou
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Publication number: 20100130738Abstract: It is to provide a novel pyrazolone derivative represented by the following general formula (1), which is useful as a pharmaceutical and has a phosphodiesterase inhibitory action: wherein R1,R2: C1-6 alkyl; R3,R4: H, X, C1-6 alkoxy; Z:O, S; A:AA, BB, wherein AA represents wherein BB represents wherein R5: H, C1-6 alkyl; R6,R7: C1-6 alkyl.Type: ApplicationFiled: June 18, 2008Publication date: May 27, 2010Inventors: Yasushi Kohno, Koji Ochiai, Satoshi Takita, Tetsuya Kishi
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Publication number: 20100119475Abstract: Compounds of general formula (I): wherein R1, R2, R3, R4, X and Y are as defined herein are inhibitors of glutaminyl cyclase and are therefore useful in treating conditions that can be treated by modulation of glutaminyl cyclase activity.Type: ApplicationFiled: September 4, 2009Publication date: May 13, 2010Applicant: PROBIODRUG AGInventors: Ulrich Heiser, Robert Sommer, Ulf-Torsten Gaertner, Antje Hamann, Michael Almstetter, Michael Thormann, Andreas Treml, Hans-Ulrich Demuth, Torsten Hoffman
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Patent number: 7714009Abstract: There is provided a CRF receptor antagonist comprising a compound of the formula (I): wherein, ring A is a 5-membered ring represented by the formula (A?): wherein X is a carbon and X1 is an oxygen, a sulfur or —NR5—, or formula (A?): wherein X is a nitrogen and R6 is an optionally substituted hydrocarbyl, R1 is an amino substituted by two optionally substituted hydrocarbyl groups, R2 is an phenyl, Y1 is CR3a or a nitrogen, Y2 is CR3b or a nitrogen and Y3 is CR3c or a nitrogen, provided that one or less of Y1, Y2, and Y3 is nitrogen, W is a bond, —(CH2)n-, and Z is a bond, —NR4—, etc.; or a salt thereof or a prodrug thereof.Type: GrantFiled: October 27, 2004Date of Patent: May 11, 2010Assignee: Takeda Pharmaceutical Company LimitedInventors: Albert Charles Gyorkos, Christopher Peter Corrette, Suk Young Cho, Timothy Mark Turner, Scott Alan Pratt, Kazuyoshi Aso, Masakuni Kori, Michiyo Gyoten
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Publication number: 20100087427Abstract: Novel 3-mono-, 3,4-di- and 3,4,4,-tri-substituted pyrrolidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on inappropriate activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on inappropriate activity of renin; the use of a compound of that class in the treatment of a disease that depends on inappropriate activity of renin; pharmaceutical formulations comprising a said substituted pyrrolidine compound, and/or a method of treatment comprising administering a said substituted pyrrolidine compound, a method for the manufacture of said substituted pyrrolidine compounds, and novel intermediates and partial steps for their synthesis are described. The substituted pyrrolidine compounds are especially of the formula I wherein the substituents are as described in the specification.Type: ApplicationFiled: December 21, 2005Publication date: April 8, 2010Inventors: Werner Breitenstein, Sylvain Cottens, Claus Ehrhardt, Edgar Jacoby, Edwige L. Lorthiolis, Juergen K. Maibaum, Nils Ostermann, Holger Sellner, Oliver Simic
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Publication number: 20100081643Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.Type: ApplicationFiled: September 21, 2009Publication date: April 1, 2010Inventors: BRETT C. BOOKSER, Qun Dang, Tony S. Gibson, Hongjian Jiang, De Michael Chung, Jianming Bao, Jinlong Jiang, Andy Kassick, Ahmet Kekec, Ping Lan, Huagang Lu, Gergely M. Makara, F. Anthony Romero, Iyassu Sebhat, David Wilson, Dariusz Wodka
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Publication number: 20100069353Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3 and R4 are as defined herein, compositions and uses thereof for treating human immunodeficiency virus (HIV) infection. In particular, the present invention provides novel inhibitors of HIV replication, pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HIV infection.Type: ApplicationFiled: December 3, 2007Publication date: March 18, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Christiane Yoakim, Patrick Deroy, Martin Duplessis, Alexandre Gagnon, Sylvie Goulet, Oliver Huecke, Christopher Lemke, Simon Surprenant
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Publication number: 20100055071Abstract: Disclosed are compounds, stereoisomers, tautomers, pharmaceutically acceptable salts, or prodrugs thereof of having Formula (I), their preparation, use, and compositions thereof for treating an infection mediated at least in part by a virus in the Flaviviridae family of viruses, wherein A, L1, V, W, T, Z, R, Y1, and p are as defined herein.Type: ApplicationFiled: November 20, 2007Publication date: March 4, 2010Inventors: Martin Robert Leivers, Franz Ulrich Schmitz, Christopher Don Roberts, Ali Dehghani Mohammad Abadi
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Publication number: 20100029736Abstract: The present invention is directed to 2-substituted proline bis-amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin 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 orexin receptors are involved.Type: ApplicationFiled: July 13, 2007Publication date: February 4, 2010Applicant: MERCK & CO., INC.Inventors: Christopher D. Cox, David B. Whitman, Michael J. Breslin
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Publication number: 20100028299Abstract: Briefly described, embodiments of this disclosure include compounds, pharmaceutical compositions, methods of treating a host infected with a virus from the Flaviviridae family of viruses, methods of inhibiting HCV replication in a host, methods of inhibiting the binding of NS4B polypeptide to the 3?UTR of HCV negative strand RNA in a host, methods of treating liver fibrosis in a host, and the like.Type: ApplicationFiled: March 18, 2009Publication date: February 4, 2010Inventors: Shirit Einav, Jeffrey S. Glenn, Wenjin Yang, Hadas Dvory-Sobol, Ingrid C. Choong, Robert McDowell
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Publication number: 20100029643Abstract: The invention relates to chemical compounds of formula (I), (Ia) and (Ib) or pharmaceutically acceptable salts thereof, which possess Edg-1 antagonistic activity and are accordingly useful for their anti-cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an anti-cancer effect in a warm-blooded animal, such as man.Type: ApplicationFiled: November 8, 2007Publication date: February 4, 2010Applicant: ASTRAZENECA ABInventors: Gurmit Grewal, Edward Hennessy, Victor Kamhi, Danyang Li, Paul Lyne, Vibha Oza, Jamal Carlos Saeh, Qibin Su, Bin Yang
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Publication number: 20090326029Abstract: The present invention provides benzimidazole thiophene compounds pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.Type: ApplicationFiled: May 31, 2007Publication date: December 31, 2009Inventors: Kevin Wayne Kuntz, Holly Kathleen Emerson, Mui Cheung, Jennifer Gabriel Badiang
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Publication number: 20090318445Abstract: The invention relates to novel compounds that are inhibitors of peptidyl deformylase (PDF). The compounds are useful as antimicrobials and antibiotics. The compounds of the invention display selective inhibition of peptidyl deformylase versus other metalloproteinases such as MMPs. Methods of preparation and uses of the compounds are also disclosed.Type: ApplicationFiled: December 28, 2006Publication date: December 24, 2009Applicants: NORVARTIS AG, NOVARTIS PHARMA GMBHInventors: Arkadius Pichota, Jeyaraj Duraiswamy, Zheng Yin, Thomas Hugo Keller, Mark Schreiber
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Publication number: 20090312383Abstract: There is provided a CRF receptor antagonist comprising a compound of the formula (I): wherein R1 is an optionally substituted hydrocarbyl, an optionally substituted C-linked heterocyclic group, an optionally substituted N-linked heteroaryl group, a cyano or an acyl; R2 is an optionally substituted cyclic hydrocarbyl or an optionally substituted heterocyclic group; X is oxygen, sulfur or —NR3— (wherein R3 is a hydrogen, an optionally substituted hydrocarbyl or an acyl); Y1, Y2 and Y3 are each an optionally substituted carbon or a nitrogen, provided that one or less of Y1, Y2 and Y3 is nitrogen; and Z is a bond, —CO—, oxygen, sulfur, —SO—, —SO2—, —NR4—, —NR4-alk-, —CONR4— or —NR4CO— (wherein alk is an optionally substituted C1-4 alkylene and R4 is a hydrogen, an optionally substituted hydrocarbyl or an acyl); or a salt thereof or a prodrug thereof.Type: ApplicationFiled: April 26, 2006Publication date: December 17, 2009Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Kazuyoshi Aso, Michiyo Mochizuki, Albert Charles Gyorkos, Christopher Peter Corrette, Suk Young Cho, Scott Alan Pratt, Christopher Stephen Siedem
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Patent number: 7629340Abstract: Disclosed are compounds having Formula (I) and the compositions and methods relating to these compounds, for treating or preventing a viral infection mediated at least in part by a virus in the Flaviviridae family of viruses, wherein A, R2, m, R, V, W, T, Z, R1, Y, and p are disclosed herein.Type: GrantFiled: December 12, 2006Date of Patent: December 8, 2009Assignee: SmithKline Beecham CorporationInventors: Franz Ulrich Schmitz, Christopher Don Roberts, Ali Dehghani Mohammad Abadi, Ronald Conrad Griffith, Martin Robert Leivers
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Publication number: 20090286791Abstract: The present invention provides compounds represented by the formula (Ia): the formula (Ib): the formula (Ic): and the formula (Id): wherein each symbol is as defined in the specification. According to the present invention, these compounds have a DGAT inhibitory activity and are useful for the prophylaxis, treatment or improvement of diseases or pathologies caused by high expression or high activation of DGAT.Type: ApplicationFiled: July 20, 2007Publication date: November 19, 2009Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Shuji Kitamura, Thomas Daniel Aicher, Steve Gonzales, Yvan Le Huerou, Scott Alan Pratt, Tim Turner, Yoshihisa Nakada
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Publication number: 20090286261Abstract: An exemplary embodiment may be directed to a fluorescence polarization assay that screens compounds or agents for their affinity to hematopoietic prostaglandin D synthase (H-PGDS) based on their ability to displace a fluorophore-containing detection analyte bound to an enzyme comprising the primary amino acid sequence of H-PGDS. Another exemplary embodiment utilizes an enzyme having a maltose binding protein amino-acid sequence fused with an N-terminus of the enzyme.Type: ApplicationFiled: May 13, 2009Publication date: November 19, 2009Applicant: CAYMAN CHEMICAL COMPANYInventors: Kirk W. Maxey, Jeffrey K. Johnson, Karie L. McGowan, Nisha Palackal, Gregory W. Endres
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Publication number: 20090281310Abstract: The present invention relates to a process for preparing a compound of formula (6a): wherein Ar1 represents an imidazolyl group which may be substituted with 1 to 3 substituents shown below; Ar2 represents a pyridinyl group, a pyrimidinyl group or a phenyl group which may be substituted with 1 to 3 substituents; and R11 represents a group selected from certain substituents.Type: ApplicationFiled: July 2, 2009Publication date: November 12, 2009Inventors: Teiji KIMURA, Koki KAWANO, Eriko DOI, Noritaka KITAZAWA, Kogyoku SHIN, Takehiko MIYAGAWA, Toshihiko KANEKO, Koichi ITO, Mamoru TAKAISHI, Takeo SASAKI, Hiroaki HAGIWARA
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Publication number: 20090270613Abstract: Benzoimidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H4 receptor, and in treating conditions such as inflammation, H4 receptor-mediated conditions, and related conditions.Type: ApplicationFiled: August 26, 2008Publication date: October 29, 2009Inventors: James P. Edwards, Michael D. Hack, David E. Kindrachuk, Jennifer D. Venable
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Publication number: 20090264646Abstract: Benzoimidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H4 receptor, and in treating conditions such as inflammation, H4 receptor-mediated conditions, and related conditions.Type: ApplicationFiled: August 26, 2008Publication date: October 22, 2009Inventors: James P. Edwards, Michael D. Hack, David E. Kindrachuk, Jennifer D. Venable
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Publication number: 20090258868Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.Type: ApplicationFiled: December 10, 2008Publication date: October 15, 2009Inventors: Zhaoning Zhu, Brian A. McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey Strickland, Elizabeth M. Smith, Andrew Stamford, William J. Greenlee, Robert Mazzola, John Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X.H. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter, Michelle L. Morris, Huizhong Gu, Gang Qian, Dawit Tadesse
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Patent number: 7601745Abstract: The present invention relates to compounds of the general formula (III) or pharmaceutically acceptable salts thereof with an acid or a base, or pharmaceutically acceptable prodrugs or a stereoisomer thereof, wherein R3 is H, —C(O)NRaRb, halogen, alkyl, haloalkyl, aryl, heteroaryl, OH, SH, NR4?OR5?, NH2, amine, alkylamine, alkoxy, cycloalkyl, heterocycloalkyl, hydroxyalkyl, or haloalkyloxy; R4 is H, halogen, alkyl, —C(NR7)NR7R8, —(CH2)paryl, —(CH2)pNR7R8, —C(O)NR7R8, —N?CR7R8, —NR7C(O)R8, cycloalkyl, heterocycloalkyl, haloalkyl, hydroxyalkyl, hyodroxyalkylamino, alkylamino, heteroaryl, or aryl; R5 is halogen, alkyl, —C(NR7)NR7R8, —(CH2)paryl, —(CH2)pNR7R8, —C(O)NR7R8, —N?CR7R8, —NR7C(O)R8, cycloalkyl, heterocycloalkyl, haloalkyl, hydroxyalkyl, hydroxyalkylamino, alkylamino, heteroaryl, or aryl.Type: GrantFiled: March 15, 2006Date of Patent: October 13, 2009Assignee: 4SC AGInventors: Johann Leban, Harald Schmitt, Kristina Wolf, Stefano Pegoraro, Andreas Wuzik
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Patent number: 7569688Abstract: Provided is a pharmaceutical composition containing a propane-1,3-dione derivative as the active ingredient, particularly a GnRH receptor antagonist. Also, provided is a propane-1,3-dione derivative having a GnRH antagonistic effect.Type: GrantFiled: June 20, 2005Date of Patent: August 4, 2009Assignee: Astellas Pharma Inc.Inventors: Masaaki Hirano, Eiji Kawaminami, Akira Toyoshima, Hiroyuki Moritomo, Norio Seki, Ryutaro Wakayama, Minoru Okada, Toshiyuki Kusayama
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Publication number: 20090192169Abstract: Compounds of Formula I: wherein A, B, D, L, R1, R2, R3, R4, m, and n are as defined for Formula I in the description. The invention also relates to processes for the preparation of the compounds and to new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and to the use of the compounds in therapy.Type: ApplicationFiled: March 29, 2007Publication date: July 30, 2009Inventors: Ian Egle, Methvin Isaac, Rebecca Urbanek, Frances M. McLaren, Sally B. Walsh, Gary B. Steelman, Dean G. Brown, David Nugiel, Deborah W. Chen, Abdelmalik Slassi, Fupeng Ma
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Patent number: 7557136Abstract: The present invention relates to novel pyrrolidine derivatives of Formula (I), its geometrical isomers, its optically active forms as enantiomers, diastercomers, mixtures of these and its racemate forms, as well as salts thereof, wherein: R1is selected from the group comprising or consisting of H and C1-C6-alkyl; R2 is selected from the group comprising or consisting of hydrogen, C1-C6-alkyl, C1-C6 alkyl aryl, heteroaryl, C1-C6 alkyl heteroaryl, C2-C6-alkenyl, C2-C6-alkenyl aryl, C2-C6 alkenyl heteroaryl, C2-C6-alkynyl, C2-C6-alkynyl aryl, C2C6-alkynyl heteroaryl, C3-C8 cycloalkyl, heterocycloalkyl, CI-C6-alkyl cycloallcyl, CI-C6-alkyl heterocycloalkyl, CIC6 alkyl carboxy, acyl, C1-C6-alkyl acyl, C1-C6-alkyl acyloxy, C1-C6-alkyl alkoxy, alkoxycarbonyl, C1-C6-alkyl alkoxycarbonyl, aminocarbonyl, C1-C6-alkyl aminocarbonyl, C1-C6-alkyl acylarnino, C1-C6-alkyl ureido, amino, C1-C6-alkyl amino, sulfonyloxy, C1-C6 alkyl sulfonyloxy, sulfonyl, C1-C6-alkyl sulfonyl, sulfinyl, C1-C6-alkyl sulfinyl, C1-C6alkyl sulfanylType: GrantFiled: February 16, 2004Date of Patent: July 7, 2009Assignee: Laboratoires Serono SAInventors: Matthias Schwarz, Catherine Jorand-Lebrun, Delphine Valognes
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Patent number: 7557221Abstract: This invention relates to compounds of formula I: or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, and R6 are described in this application. These compounds inhibit the enzymes MEK 1 and MEK2, protein kinases that are components of the MAP kinase signal transduction pathway and as such the compounds will have anti-hyperproliferative cellular activity.Type: GrantFiled: August 6, 2008Date of Patent: July 7, 2009Assignee: Hoffman-La Roche Inc.Inventors: Shaoqing Chen, Nicholas J. S. Huby, Norman Kong, John Anthony Moliterni, Omar Jose Morales