Plural Ring Nitrogens In The Polycyclo Ring System Patents (Class 546/199)
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Publication number: 20110142798Abstract: 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: December 14, 2010Publication date: June 16, 2011Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Hui Cao, Lu Ying, Yat Sun Or
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Patent number: 7956069Abstract: Compounds of Formulae I, or pharmaceutically acceptable salts thereof: wherein A1, A2, G1, G2 G3, R1, R2, X, Y, Z, m, n and p 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: GrantFiled: June 8, 2007Date of Patent: June 7, 2011Assignee: AstraZeneca ABInventors: Yun-Xing Cheng, Mehrnaz Pourashraf, Miroslaw Tomaszewski
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Publication number: 20110129419Abstract: The present invention relates to the field of medical imaging, and in particular to imaging of disease states associated with the upregulation of the chemokine receptor 5 (CCR5). Imaging agents, precursors and methods are provided which are useful in imaging such disease states.Type: ApplicationFiled: December 19, 2007Publication date: June 2, 2011Applicants: GE HEALTHCARE LIMITED, HAMMERSMITH IMANET LIMITEDInventors: Anthony Eamon Storey, Julie Davis, Erik Arstad, Benedicte Guilbert, Alessandra Gaeta
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Publication number: 20110130381Abstract: Inhibitors of dihydroorotate dehydrogenase (DHODH) for the Plasmodium enzyme have been identified and characterized. The inhibitors have high specificity, submicromolar efficacy against cultured parasite strains, exhibit drug-like properties, and are not overtly cytotoxic.Type: ApplicationFiled: May 7, 2009Publication date: June 2, 2011Inventors: Cecilia Bastos, Michael L. Booker, Cassandra A. Celatka, Jon C. Clardy, Joseph Cortese, Vishal P. Patel, Renato Skerlj, Roger C. Wiegand, Dyann F. Wirth
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Publication number: 20110124637Abstract: Provided herein are sirtuin-modulating compounds of formula (II). The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders relating to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: July 2, 2009Publication date: May 26, 2011Inventors: Chi B Vu, Jeremy S. Disch, Pui Yee Ng, Charles A. Blum, Robert B. Perni
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Publication number: 20110124657Abstract: The present invention relates to compounds having pharmacological activity towards the 5-HT7 receptor; to a method for identifying them as 5-HT7 ligands, especially as agonists, by using a pharmacophore and a descriptor's profile filter; to pharmaceutical compositions comprising them; and to their use in therapy, in particular for the treatment and or prophylaxis of a disease in which 5-HT7 is involved, such as CNS disorders.Type: ApplicationFiled: July 30, 2009Publication date: May 26, 2011Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Rosalia Pascual-Ramon, H. Helmut Buschmann
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Publication number: 20110123586Abstract: Methods are provided for identifying molecules that can be used to positively and negatively manipulate quorum-sensing-mediated communication to control bacterial behavior. Small-molecule antagonists that disrupt quorum-sensing-mediated activities are identified. Methods are provided for disrupting detection of acyl-homoserine lactone autoinducer in Gram-negative bacteria by contacting the bacteria with the antagonists. Methods of inhibiting quorum sensing-mediated activity in Gram-negative bacteria are provided wherein the activity is pathogenicity, bioluminescence, siderophore production, type III secretion, or metalloprotease production.Type: ApplicationFiled: June 2, 2009Publication date: May 26, 2011Inventors: Bonnie Bassler, Lee Swem
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Publication number: 20110118278Abstract: There are provided bicyclic carbonylamino-pyrazoles of formula (I), wherein the variables are as specified in the claims, for use as medicament, in particular for the treatment of diseases due to the malfunctioning of protein kinases (PKs), such as cancer, pharmaceutical compositions comprising such carbamoyl derivatives, and their use as prodrugs of therapeutically active agents. Method of treatment and some new bicyclic carbonylamino-pyrazoles are also object of the present invention.Type: ApplicationFiled: May 14, 2009Publication date: May 19, 2011Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Maurizio Pulici, Paolo Polucci
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Patent number: 7943774Abstract: Heterocyclyl-substituted thiazoles of the formula (I), in which the symbols have the meanings given in the description, and also to the agrochemically active salts thereof, and their use for controlling phytopathogenic harmful fungi, and also processes for preparing compounds of the formula (I).Type: GrantFiled: September 29, 2009Date of Patent: May 17, 2011Assignee: Bayer Cropscience AGInventors: Pierre Cristau, Nicola Rahn, Stefan Herrmann, Tomoki Tsuchiya, Ulrike Wachendorff-Neumann, Arnd Voerste, Jürgen Benting, Pierre Wasnaire, Sebastian Hoffmann
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Publication number: 20110112091Abstract: A derivative of tetrabromobenzimidazole, a process for the preparation thereof, a pharmaceutical composition, a method for using the same, a method for modulating or regulating serine/threonine kinases, and a serine/threonine kinases modulating agent. The invention relates to novel small-molecule compounds with kinase inhibitory activity, having superior properties as pharmaceutical agents, production method thereof and uses thereof. In particular, this invention relates to new derivatives of tetrabromobenzimidazole with Pim kinases inhibitory properties, which exhibits superior pharmacological actions, and can be useful for the treatment of disease conditions, especially cancers depending on Pim kinases, such as leukemias and prostate cancer.Type: ApplicationFiled: November 12, 2009Publication date: May 12, 2011Applicant: SELVITA SP. Z O.O.Inventors: Krzysztof Brzozka, Wojciech Czardybon, Adrian Zarebski, Nicolas Beuzen
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Patent number: 7939520Abstract: The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor.Type: GrantFiled: May 13, 2008Date of Patent: May 10, 2011Assignee: Wyeth LLCInventors: Simon Nicolas Haydar, Patrick Andrae
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Patent number: 7935709Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of pro-inflammatory cytokine mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein s, T, R1, R2, R3 and R4 are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use such as treatment of p38 mediated diseases by administering the compounds of Formula I or compositions including the compounds of Formula I, and intermediates and processes useful for the preparation of compounds of Formula I.Type: GrantFiled: July 16, 2007Date of Patent: May 3, 2011Assignee: Amgen Inc.Inventors: Fang-Tsao Hong, Kelvin K. C. Sham, Seifu Tadesse, Andrew Tasker
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Patent number: 7935719Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the histamine-3 receptor: wherein the variables are described in the specification.Type: GrantFiled: October 5, 2007Date of Patent: May 3, 2011Assignee: Wyeth LLCInventors: William Ronald Solvibile, Ji-In Kim, Marla Jean Williams, Jonathan Laird Gross, Albert Jean Robichaud
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Patent number: 7932250Abstract: To provide thienopyrazole derivatives inhibiting PDE 7 selectively, and therefore, enhance cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic diseases, inflammatory diseases or immunologic diseases. The compound is thienopyrazole compound represented by the following formula (I): [wherein, especially, R1 is a cyclohexyl, a cycloheptyl group or a tetrahydropyranyl group; R2 is methyl; R3 is a hydrogen atom; and R4 is a group: —CONR5R6 (in which any one of R5 and R6 is a hydrogen atom)].Type: GrantFiled: July 1, 2005Date of Patent: April 26, 2011Assignee: Daiichi Sankyo Company, LimitedInventors: Hidekazu Inoue, Hidenobu Murafuji, Yasuhiro Hayashi
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Publication number: 20110092501Abstract: The invention relates to novel pyrrolidine derivatives of formula (I): wherein R1, R2 and R3 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.Type: ApplicationFiled: September 13, 2010Publication date: April 21, 2011Applicant: PROBIODRUG AGInventors: Ulrich Heiser, Daniel Ramsbeck, Robert Sommer, Antje Meyer, Torsten Hoffmann, Livia Boehme, Hans-Ulrich Demuth
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Publication number: 20110092415Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.Type: ApplicationFiled: October 13, 2010Publication date: April 21, 2011Applicant: ABBOTT LABAORATORIESInventors: David A. DeGoey, Warren M. Kati, Charles W. Hutchins, Pamela L. Donner, Allan C. Krueger, John T. Randolph, Christopher E. Motter, Lissa T. Nelson, Sachin V. Patel, Mark A. Matulenko, Ryan G. Keddy, Tammie K. Jinkerson, Todd N. Soltwedel, Dachun Liu, John K. Pratt, Todd W. Rockway, Clarence J. Maring, Douglas K. Hutchinson, Charles A. Flentge, Rolf Wagner, Michael D. Tufano, David A. Betebenner, Michael J. Lavin, Kathy Sarris, Kevin R. Woller, Seble H. Wagaw, Jean C. Califano, Wenke Li, Daniel D. Caspi, Mary E. Bellizzi, William A. Carroll
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Patent number: 7928105Abstract: Disclosed are compounds of the following formula: in which R1, R2, R5, R6, R7, R31, u, and X are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.Type: GrantFiled: January 21, 2010Date of Patent: April 19, 2011Assignee: Takeda Pharmaceutical Company LimitedInventors: Anthony R. Gangloff, Andrew John Jennings, Benjamin Jones, Andre A. Kiryanov
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Patent number: 7928129Abstract: New carboxyphenyl-glycylboronic acid transition-state analog inhibitors, representative of a class of compounds effective against class C ?-lactamase AmpC. The new compounds improve inhibition by over two-orders of magnitude compared to analogous glycylboronic acids, with Ki values as low as 1 nM.Type: GrantFiled: September 18, 2007Date of Patent: April 19, 2011Assignees: Northwestern University, University of ModenaInventors: Brian K. Shoichet, Fabrio Prati
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Publication number: 20110086853Abstract: Compounds of formula I or pharmaceutically acceptable salts thereof: wherein 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: October 8, 2009Publication date: April 14, 2011Inventors: William Brown, Ziping Liu, Daniel Page, Zena Qadoumi, Sanjay Srivastava, Maxime Tremblay, Christopher Walpole, Zhong-yong Wei, Hua Yang
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Publication number: 20110082143Abstract: Bicyclic heteroaryl compounds of formula (I) shown below are disclosed. Each variable in formula (I) is defined in the specification. Also disclosed is treatment of cancer with these compounds.Type: ApplicationFiled: October 1, 2010Publication date: April 7, 2011Applicant: National Taiwan UniversityInventors: Chung-Ming Sun, Min-Liang Kuo
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Substituted benzimidazole compounds with dual NOS inhibitory activity and mu opioid agonist activity
Patent number: 7919510Abstract: The present invention relates to benzimidazole compounds having dual nitric oxide synthase (NOS) inhibitory activity and agonist activity at the mu-opioid receptor, to pharmaceutical and diagnostic compositions containing them, and to their medical use, particularly as compounds for the treatment or prevention of chronic pain, acute pain, migraine, and neuropathic pain.Type: GrantFiled: May 18, 2006Date of Patent: April 5, 2011Assignee: NeurAxon, IncInventors: Paul Renton, Shawn Maddaford, Suman Rakhit, John Andrews -
Publication number: 20110077236Abstract: The present invention relates to new substituted carboxylic acid amides of general formula wherein A, B and R1 to R5 are defined as in claim 1, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.Type: ApplicationFiled: December 2, 2010Publication date: March 31, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Henning PRIEPKE, Kai GERLACH, Roland PFAU, Norbert HAUEL, Iris KAUFFMANN-HEFNER, Georg DAHMANN, Herbert NAR, Sandra HANDSCHUH, Wolfgang WIENEN, Annette SCHULER-METZ
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Publication number: 20110076292Abstract: Benzoxazepin compounds of Formula I, including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z1 is CR1 or N; Z2 is CR2 or N; Z3 is CR3 or N; Z4 is CR4 or N; and B is a pyrazolyl, imidazolyl, or triazolyl ring fused to the benzoxepin ring, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I 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: September 27, 2010Publication date: March 31, 2011Inventors: Nicole Blaquiere, Steven Do, Danette Dudley, Adrian Folkes, Robert Heald, Timothy Heffron, Mark Jones, Aleksandr Kolesnikov, Chudi Ndubaku, Alan G. Olivero, Stephen Price, Steven Staben, Lan Wang
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Publication number: 20110071130Abstract: The invention relates to 2-aminobenzimidazoles useful in treating disorders that are mediated by A2a receptor function, including neurodegenerative diseases including Parkinson's disease and inflammation.Type: ApplicationFiled: May 7, 2007Publication date: March 24, 2011Applicant: Pharmacopeia, Inc.Inventors: Andrew G. Cole, Brian F. McGuinness, Guizhen Dong, Ian Henderson
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Publication number: 20110065682Abstract: The present invention relates to novel heterocyclic compounds of Formulae I-III; as disclosed herein or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosed are pharmaceutical compositions comprising said compounds, and methods for using said compounds for treating or preventing a thromboembolic disorder.Type: ApplicationFiled: May 18, 2009Publication date: March 17, 2011Inventors: Martin C. Clasby, William J. Greenlee, Yan Xia, Tin-Yau Chan, Mariappan V. Chelliah, Samuel Chackalamannil, Haiyan Pu,, Keith A. Eagen, Henry Vaccaro, Brian A. McKittrick,, Liyuan Wang, Xiaobang Gao
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Patent number: 7906532Abstract: This invention relates to compounds of the formula (I): or pharmaceutically acceptable salts thereof, wherein: R1, R2, R3, A and m are each as described herein and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by 5-HT4 agonistic activity such as, but not limited to, gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageral disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders, cardiac failure, heart arrhythmia, diabetes and apnea syndrome.Type: GrantFiled: July 14, 2006Date of Patent: March 15, 2011Assignee: Pfizer Inc.Inventors: Asako Ishibashi, Tomoki Kato, Kiyoshi Kawamura, Sachiko Mihara, Mikio Morita
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Patent number: 7906655Abstract: 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: GrantFiled: August 5, 2009Date of Patent: March 15, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Makonen Belema, Andrew C. Good, Jason Goodrich, Ramesh Kakarla, Guo Li, Omar D. Lopez, Van N. Nguyen, Jayne Kapur, Yuping Qiu, Jeffrey Lee Romine, Denis R. St. Laurent, Michael Serrano-Wu, Lawrence B. Snyder, Fukang Yang
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Publication number: 20110059959Abstract: The present invention is directed to novel multicyclic molecules that mediate enzymatic activity. In particular, the compounds may be effective in the treatment of diseases or disease states related to the activity of PARP, VEGFR2, and MLK3 enzymes, including, for example, neurodegenerative diseases, inflammation, ischemia, and cancer.Type: ApplicationFiled: November 18, 2010Publication date: March 10, 2011Applicant: CEPHALON, INC.Inventors: Sankar Chatterjee, James L. Diebold, Derek Dunn, Robert L. Hudkins, Reddeppareddy Dandu, Gregory J. Wells, Allison L. Zulli
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Patent number: 7897634Abstract: This invention relates to compounds of the formulas (1), (2) and (3) having pharmacological activity, to compositions containing these compounds, and to methods of treatment employing the compounds and compositions.Type: GrantFiled: January 30, 2007Date of Patent: March 1, 2011Assignee: Athersys, Inc.Inventors: Youssef L. Bennani, Michael G. Campbell, David Dastrup, Emile Porter Huck
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Publication number: 20110046132Abstract: The present invention is directed to benzoimidazole compounds of the formula (1) and enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions modulated by prolyl hydroxylase activity.Type: ApplicationFiled: April 28, 2009Publication date: February 24, 2011Inventors: Frances Meredith Hocutt, Barry Eastman Leonard, JR., Hillary M. Peltier, Victor K. Phuong, Michael H. Rabinowitz, Mark D. Rosen, Kyle T. Tarantino, Hariharan Venkatesan, Lucy Xiumin Zhao
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Publication number: 20110044940Abstract: The present invention relates to novel Heterocyclic Ether or Thioether Derivatives, compositions comprising the Heterocyclic Ether or Thioether Derivatives, and methods for using the Heterocyclic Ether or Thioether Derivatives for treating or preventing a proliferative disorder, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral infection, a fungal infection, or a disorder related to the activity of a protein kinase.Type: ApplicationFiled: October 27, 2008Publication date: February 24, 2011Inventors: Gerald W. Shipps, JR., Matthew Richards, Cliff C. Cheng, Xiaohua Huang
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Patent number: 7893049Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R6 are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.Type: GrantFiled: April 5, 2007Date of Patent: February 22, 2011Assignee: Boehringer Ingelheim International GmbHInventors: Darryl McConnell, Bodo Betzemeier, Thomas Gerstberger, Maria Impagnatiello, Steffen Steurer, Lars van der Veen, Ulrike Weyer-Czernilofsky
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Publication number: 20110039857Abstract: The invention relates to piperidine and pyrrolidine compounds of formula (I) wherein A, B, n and X are as described in the description; to pharmaceutically acceptable salts thereof, and to the use of such compounds use as medicaments, especially as orexin receptor antagonists.Type: ApplicationFiled: April 29, 2009Publication date: February 17, 2011Inventors: Hamed Aissaoui, Christoph Boss, Ralf Koberstein, Thierry Sifferlen, Daniel Trachsel
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Patent number: 7879850Abstract: The present invention provides compounds of the following structure; A-Q-B—C-D that are useful for treating conditions or disorders associated with DGAT1 activity in animals, particularly humans.Type: GrantFiled: September 26, 2008Date of Patent: February 1, 2011Assignee: Novartis AGInventors: Young-Shin Kwak, Gary Mark Coppola
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Publication number: 20110009636Abstract: The present invention relates to a process for preparing 2-methyl-2?-phenylpropionic acid derivatives showing antihistamine activity in more simplified way, intermediate compounds and their preparation processes used therefor. According to the present invention, pharmaceutically useful 2-methyl-2?-phenylpropionic acid derivatives can be prepared with high yield and purity on industrial scale.Type: ApplicationFiled: February 12, 2009Publication date: January 13, 2011Inventors: Chun-Ho Lee, Ja-Heouk Khoo, Kyoung-Chan Kwon, Hyun Ju
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Publication number: 20110009389Abstract: There is provided an imidazole derivative useful as a thrombosis treating agent, which is represented by the formula (I): wherein R represents an optionally substituted cyclic hydrocarbon group or an optionally substituted heterocyclic group, W represents a bond or an optionally substituted divalent linear hydrocarbon group, X represents an optionally substituted divalent hydrocarbon group, Y represents —CO—, —S(O)—, —S(O)2— or a bond, ring A represents an optionally substituted pyrrolidine ring, an optionally substituted piperidine ring or an optionally substituted perhydroazepine ring, Z1 and Z3 independently represent a bond or an optionally substituted divalent linear hydrocarbon group, Z2 represents —N(R1)—, —O—, —S(O)—, —S(O)2—, —CO—, —CH(R1)— or a bond, ring B represents an optionally substituted imidazole ring, wherein a substituent which the optionally substituted imidazole ring represented by ring B may have may be taken together with R1 to form an optionally substituted ring, and a represents 0Type: ApplicationFiled: September 10, 2010Publication date: January 13, 2011Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Keiji KUBO, Takanobu KUROITA, Yasuhiro IMAEDA, Masaki KAWAMURA
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Publication number: 20110009622Abstract: [Problem] To provide compounds useful as preventives or remedies for circular system disorders, nervous system disorders, metabolic disorders, reproduction system disorders, digestive system disorders, neoplasm, infectious diseases, etc., or as herbicides. [Means for Solution] A long-chain fatty acyl elongase inhibitor comprising, as the active ingredient thereof, a compound or a pharmaceutically-active salt thereof of a formula (I): [wherein W represents a hydrogen atom, a C1-6 alkyl, etc.; X represents an aryl, a heteroaryl, etc.; n indicates 0 or 1; Z represents a hydrogen atom, a C1-6 alkyl, etc.; A1, A2, A3 and A4 each independently represent CH or N].Type: ApplicationFiled: April 17, 2009Publication date: January 13, 2011Inventors: Makoto Jitsuoka, Tsuyoshi Nagase, Nagaaki Sato, Daisuke Tsukahara
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Publication number: 20110003797Abstract: The present invention is directed to hexahydrocyclopentyl[f]imidazole carboxamides and derivatives thereof as selective glucocorticoid receptor ligands useful for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: February 16, 2009Publication date: January 6, 2011Inventors: William P. Dankulich, Danielle M. McMaster, Robert S. Meissner, Helen J. Mitchell
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Publication number: 20110003994Abstract: The present invention relates to a novel cycloalkane derivative which exhibits an excellent psychotropic action and has less side effect.Type: ApplicationFiled: June 30, 2010Publication date: January 6, 2011Inventor: Megumi MARUYAMA
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Patent number: 7863310Abstract: The present invention provides kinase inhibitors of Formula I:Type: GrantFiled: January 21, 2005Date of Patent: January 4, 2011Assignee: Eli Lilly and CompanyInventors: Rosanne Bonjouklian, Robert Dean Dally, Alfonso de Dios, Mirian Filadelfa del Prado Catalina, Carmen Dominguez-Fernandez, Carlos Jaramillo Aguado, Beatriz Lopez de Uralde-Garmendia, Timothy Alan Shepherd
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Patent number: 7851630Abstract: The invention relates to a group of hydronopol substituted benzimidazolone and quinazolinone derivatives which are agonists on human ORL1 (nociceptin) receptors. The invention also relates to the preparation of these compounds, to pharmaceutical compositions containing a pharmacologically active amount of at least one of these novel benzimidazolone and quinazolinone derivatives as an active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of disorders in which ORL1 receptors are involved. The invention relates to compounds of the general formula (1) wherein the symbols have the meanings as given in the description.Type: GrantFiled: September 29, 2004Date of Patent: December 14, 2010Assignee: Solvay Pharmaceuticals B.V.Inventors: Jacobus A. J. Den Hartog, Samuel David, Daniel Jasserand, Gustaaf J. M. Van Scharrenburg, Herman H. Van Stuivenberg, Tinka Tuinstra
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Publication number: 20100311709Abstract: The present invention is directed to 2-[1-phenyl-5-hydroxy or methoxy-4alpha-methyl-hexahydrocyclopenta[f]indazol-5-yl]ethyl phenyl derivatives of formula I (I) as glucocorticoid receptor ligands useful for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: October 23, 2007Publication date: December 9, 2010Inventors: Christopher J. Bungard, Jesse J. Manikowski, James J. Perkins, Robert Meissner
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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: 20100298377Abstract: This disclosure relates to compounds of formula (I): wherein R1, R2, R3, R4, E, and n1 are as defined in the disclosure, to compositions containing them, to processes for preparing them, and the use thereof.Type: ApplicationFiled: December 11, 2009Publication date: November 25, 2010Applicant: SANOFI-AVENTISInventors: Michel ALETRU, Dominique DAMOUR, Patrick MOUGENOT, Frederico NARDI, Patrick NEMECEK, Christophe PHILIPPO, Catherine MONSEAU, Claudie NAMANE
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Publication number: 20100298378Abstract: The invention relates to aryl-substituted polycyclic amines of formula I, especially bicyclic amines, and to the physiologically tolerated salts and physiologically functional derivatives thereof; where the symbols and radicals are explained in the description, as well as to pharmaceutical compositions containing them and to methods of treatment using them.Type: ApplicationFiled: July 29, 2010Publication date: November 25, 2010Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBHInventors: Lothar SCHWINK, Siegfried STENGELIN, Matthias GOSSEL, Gerhard HESSLER, Petra LENNIG
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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: 20100298380Abstract: This invention relates to novel N-aryl-N-piperidin-4-ylmethyl amide derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy, and to pharmaceutical compositions comprising the compounds of the invention.Type: ApplicationFiled: July 31, 2008Publication date: November 25, 2010Applicant: NeuroSearch A/SInventors: Dan Peters, John Paul Redrobe, Gordon Munro, Elsebet Østergaard Nielsen
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Publication number: 20100292266Abstract: Certain oxazolyl piperidine compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity. Thus, the compounds may be administered to treat, e.g., anxiety, pain, inflammation, sleep disorders, eating disorders, or movement disorders (such as multiple sclerosis).Type: ApplicationFiled: May 25, 2007Publication date: November 18, 2010Inventors: Richard Apodaca, James Guy Breitenbucher, Alison L. Chambers, Mark Seierstad, Wei Xiao
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Publication number: 20100292214Abstract: The Invention relates to compounds having an antiparasitic activity, and to their use as a drug, in particular as a drug for the prevention and/or treatment of parasitic diseases caused by apicomplexans. The invention also relates to pharmaceutical compositions containing those compounds.Type: ApplicationFiled: June 2, 2008Publication date: November 18, 2010Applicants: commissariat a l'Energie Atomique, Centre National De La Recherche ScientifiqueInventors: Michael Deligny, Nadia Saidani, Anne-Laure Bonneau, Cyrille Botte, Helene Hardre, Bernard Rousseau, Henri Vial, Corinne Mercier, Roman Lopez, Eric Marechal
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Publication number: 20100292207Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.Type: ApplicationFiled: July 8, 2008Publication date: November 18, 2010Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni