Three Ring Nitrogens In The Bicyclo Ring System Patents (Class 546/118)
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Publication number: 20090264425Abstract: This invention relates to biaryl ether derivatives of formula (I) wherein R1, R3, R4, X, W, Y and m are defined in the description, and to compositions containing them and the uses of such derivatives. The compounds of the present invention bind to the enzyme reverse transcriptase and are modulators, especially inhibitors thereof.Type: ApplicationFiled: December 12, 2005Publication date: October 22, 2009Inventors: Lyn Howard Jones, Donald Stuart Middleton, Charles Eric Mowbray, Sandra Dora Newman, David Howard Williams
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Publication number: 20090264442Abstract: The invention relates to compounds of formula I having pharmacological activity towards the sigma receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which the sigma receptor is involved.Type: ApplicationFiled: March 1, 2007Publication date: October 22, 2009Applicant: Laboratorios Del Dr. Esteves, S.A.Inventors: Rosa Cuberes-Altisent, Joerg Holenz
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Publication number: 20090258897Abstract: Disclosed herein are substituted benzimidazole-based proton pump modulators of Formula I, processes of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: April 11, 2008Publication date: October 15, 2009Applicant: Auspex Pharmaceuticals, Inc.Inventors: Thomas G. Gant, Sepehr Sarshar
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Publication number: 20090258866Abstract: The disclosure generally relates to the novel compounds of formula I, including their salts, which are CGRP receptor antagonists. The disclosure also relates to pharmaceutical compositions and methods for using the compounds in the treatment of CGRP related disorders including migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases such as asthma, and chronic obstructive pulmonary disease (COPD).Type: ApplicationFiled: March 31, 2009Publication date: October 15, 2009Inventor: Guanglin Luo
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Publication number: 20090258856Abstract: The present invention relates to substituted imidazo-pyridinones and imidazo-pyridazinones of general formula wherein Y and R1 to R4 are defined as in claim 1, the tautomers, enantiomers, diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: ApplicationFiled: June 23, 2009Publication date: October 15, 2009Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias ECKHARDT, Norbert HAUEL, Elke LANGKOPF, Frank HIMMELSBACH, Iris KAUFFMANN-HEFNER, Mohammad TADAYYON, Michael MARK
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Patent number: 7601737Abstract: The invention relates to compounds of formula 1 and formula 10 and to compositions comprising these compounds and methods of treating gastrointestinal disorders by administering these compounds.Type: GrantFiled: December 12, 2007Date of Patent: October 13, 2009Assignee: Nycomed GmbHInventors: Bernhard Kohl, Bernd Müller, Dieter Haag, Wolfgang-Alexander Simon, Karl Zech, Michael David, Oliver Von Richter, Felix Huth
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Publication number: 20090253737Abstract: Provided are certain chemical entities, and methods of use to modulate skeletal myosin, skeletal actin, skeletal tropomyosin, skeletal troponin C, skeletal troponin I, skeletal troponin T, and skeletal muscle, including fragments and isoforms thereof, as well as the skeletal sarcomere, and methods of use in the treatment of neuromuscular disorders, conditions having muscle wasting, claudication, frailty, metabolic syndrome, muscle atrophy associated with disuse, and muscle fatigue, and other indications.Type: ApplicationFiled: February 2, 2009Publication date: October 8, 2009Inventors: Zhe YANG, Scott COLLIBEE, Alex MUCI, Jianchao WANG, Luke W. ASHCRAFT, Jeff GARDINA, Brian STOLTZ, Gustave BERGNES, Bradley P. MORGAN
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Patent number: 7598266Abstract: The present invention is directed to compounds represented by the following structural formula, Formula I: wherein: (a) X is selected from the group consisting of a single bond, O, S, S(O)2 and N; (b) U is an aliphatic linker; (c) Y is selected from the group consisting of C, O, S, NH and a single bond; (d) E is C(R3)(R4)A or A and wherein (i) A is selected from the group consisting of carboxyl, tetrazole, C1-C6 alkylnitrile, carboxamide, sulfonamide and acylsulfonamide; (e) B is selected from the group consisting of S, O, C, and N; (f) Z is selected from the group consisting of N and C; with the proviso that when B is C then Z is N.Type: GrantFiled: April 9, 2008Date of Patent: October 6, 2009Assignee: Eli Lilly and CompanyInventors: Scott Eugene Conner, Nathan Bryan Mantlo, Guoxin Zhu
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Publication number: 20090247507Abstract: Compounds of formula (I), are aurora kinase inhibitors: wherein X is —N—, —CH2—N—, —CH2—CH—, or —CH—; R1 is a radical of formula (IA) wherein Z is —CH2—, —NH—, -0-, —S(O)— —S—, —S(O)2 or a divalent monocyclic carbocyclic or heterocyclic radical having 3-7 ring atoms; Alk is an optionally substituted divalent C1-C6 alkylene radical; A is hydrogen or an optionally substituted monocyclic carbocyclic or heterocyclic ring having 5-7 ring atoms; r, s and t are independently 0 or 1, provided that when A is hydrogen then at least one of r and s is 1; R2 is halogen, —CN, —CF3, —OCH3, or cyclopropyl; and R3 is a radical of formula (IB) wherein Q is hydrogen or an optionally substituted phenyl or monocyclic heterocyclic ring with 5 or 6 ring atoms; Z&It;1> is —S—, —S(O)—, —S(O)2—, —O—, —SO2NH—, —NHSO2—, NHC(?O)NH, —NH(C?S)NH—, Or —N(R4)—wherein R4 is hydrogen, C1-C3 alkyl, cycloalkyl, or benzyl; and Alk&It;1> and Alk&It;2> are, independently, optionally substituted divalent C1-C3 alkylenType: ApplicationFiled: December 21, 2006Publication date: October 1, 2009Applicant: THE INSTITUTE OF CANCER RESEARCHInventors: Vassilios Bavetsias, Edward McDonald, Spyridon Linardopoulos
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Publication number: 20090247571Abstract: Provided are certain chemical entities, and methods of use to modulate skeletal myosin, skeletal actin, skeletal tropomyosin, skeletal troponin C, skeletal troponin I, skeletal troponin T, and skeletal muscle, including fragments and isoforms thereof, as well as the skeletal sarcomere, and methods of use in the treatment of obesity, sarcopenia, wasting syndrome, frailty, cachexia, muscle spasm, post-surgical and post-traumatic muscle weakness, neuromuscular disease, and other indications.Type: ApplicationFiled: January 23, 2009Publication date: October 1, 2009Inventors: Alex T. Muci, Gustave Bergnes, Bradley P. Morgan
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Publication number: 20090232844Abstract: The invention provides novel compositions comprising Imidazopyridine compounds. Also provided are methods of administering the compositions in an effective amount to enhance the immune response of a subject. Further provided are novel compositions and methods of administering the compositions in combination with (an)other agent(s).Type: ApplicationFiled: March 23, 2007Publication date: September 17, 2009Inventors: James Sutton, Nicholas Valiante
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Publication number: 20090227616Abstract: Invented are novel 1H-imidazo[4,5-c]pyridin-2-yl compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.Type: ApplicationFiled: November 9, 2006Publication date: September 10, 2009Inventors: Dirk A. Heerding, Tammy J. Clark, Jack Dale Leber, Igor Safonov, Mie Li
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Publication number: 20090227578Abstract: Objects of the present invention are the compounds of formula I their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, pharmaceutical compositions containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.Type: ApplicationFiled: July 28, 2006Publication date: September 10, 2009Inventors: Richard Engh, Hubert Hertenberger, Konrad Honold, Birgit Masjost, Petra Rueger, Wolfgang Schaefer, Stefan Scheiblich, Manfred Schwaiger
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Publication number: 20090221631Abstract: The invention relates to imidazopyridinones, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. By activating TLRs, it should be possible to induce or stimulate immune cells to mount an immune response. In particular, the TLR7 has been implicated in viral infections (such as HCV or HBV), cancers and tumours, and T2 Helper cell (TH2) mediated diseases, and hence TLR7 agonists are potentially useful in the treatment of such diseases. We have now found a series of imidazopyridinones which are agonists of TLR7. According, there is provided a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is 3- to 8-membered saturated heterocyclic group wherein one ring member is —O—; and R2 is phenyl or pyridinyl, each optionally substituted by C1-C6alkyl.Type: ApplicationFiled: May 15, 2009Publication date: September 3, 2009Inventors: Peter H. JONES, David Cameron Pryde, Thien Duc Tran
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Patent number: 7582652Abstract: The present invention provides kinase inhibitors of Formula I.Type: GrantFiled: January 25, 2005Date of Patent: September 1, 2009Assignee: Eli Lilly and CompanyInventors: Rosanne Bonjouklian, Chafiq Hamdouchi, Chuan Shih, Alfonso De Dios, Miriam Filadelfa del Prado, Carlos Jaramillo Aguado, Pramila Kotiyan, Mary Margaret Mader, Sheila Pleite Selgas, Concepcion Sanchez-Martinez
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Publication number: 20090215818Abstract: Invented is a method of inhibiting the activity/function of PI3 kinases using thiozolidinedione derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of thiozolidinedione derivatives.Type: ApplicationFiled: July 24, 2007Publication date: August 27, 2009Applicant: SmithKline Beecham CorporationInventors: Nicholas D. Adams, Dashyant Dhanak, Steven David Knight, Lee Schaller, Jun Tang
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Patent number: 7579359Abstract: Imidazo-containing compounds (e.g., imidazonaphthyridines, imidazopyridines, imidazoquinolines, and imidazote-trahydroquinolines) with an alkoxy substituent at the 1-position, pharmaceutical compositions containing the compounds and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.Type: GrantFiled: September 1, 2005Date of Patent: August 25, 2009Assignee: 3M Innovative Properties CompanyInventors: Larry R. Krepski, Daniel E. Duffy, John F. Gerster, Joan T. Moseman
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Patent number: 7579471Abstract: The present invention provides compounds of formula (I) wherein X, Y, R1, R2 and R3 are as defined hereinabove. The compounds of the present invention are modulators, especially antagonists, of the activity of chemokine CCR5 receptors. Modulators of the CCR5 receptor may be useful in the treatment of various inflammatory diseases and conditions, and in the treatment of infection by HIV and genetically related retroviruses.Type: GrantFiled: April 4, 2007Date of Patent: August 25, 2009Assignee: Pfizer, Inc.Inventors: Patricia Ann Basford, Peter Thomas Stephenson, Stefan Colin John Taylor, Anthony Wood
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Publication number: 20090209578Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3, R4, Het and m are as defined in the description. The compounds of the present invention are modulators, especially antagonists, of the activity of chemokine CCR5 receptors.Type: ApplicationFiled: November 27, 2006Publication date: August 20, 2009Inventors: Christopher Gordon Barber, David Clive Blakemore
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Publication number: 20090209540Abstract: Disclosed are biaryl benzoimidazole derivatives. They have an inhibitory effect on calcium influx in HEK cells, thereby showing a powerful antagonistic effect on a vanilloid receptor, and further have an analgesic effect, thereby being useful for preventing or treating pain, acute pain, chronic pain, neuropathic pain, postoperative pain, migraine, arthralgia, neuropathies, nerve injury, diabetic neuropathy, neurological illness, neurodermatitis, stroke, bladder hypersensitivity, irritable bowel syndrome, a respiratory disorder such as cough, asthma, and chronic obstructive pulmonary disease, burning, psoriasis, itching, vomiting, irritation of the skin, eyes, and mucous membranes, gastric-duodenal ulcers, inflammatory intestinal diseases, and inflammatory diseases.Type: ApplicationFiled: July 11, 2007Publication date: August 20, 2009Applicant: DAEWOONG PHARMACEUTICAL CO., LTD.Inventors: Ji Duck Kim, Hong-Chul Yoon, In Woo Kim, Hyae Jung Hyun
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Publication number: 20090208456Abstract: The present invention relates to pharmaceutical compositions for the treatment of prevention of viral infections comprising as an active principle at least one imidazo[4,5-c]pyrimidine having the general formula (A), wherein the substituents are described in the specification. The invention also relates to processes for the preparation of compounds according to the invention having above mentioned general formula, their pharmaceutically acceptable formulations and their use as a medicine or to treat or prevent viral infections.Type: ApplicationFiled: July 26, 2005Publication date: August 20, 2009Applicants: Gilead Sciences, Inc., K.U. Leuven Research & Development, Gerhard PuerstingerInventors: Gerhard Puerstinger, Choung U. Kim, Johan Neyts, David A. Oare
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Publication number: 20090203730Abstract: Disclosed are compounds of Formula I, pharmaceutical compositions comprising Formula I and methods of treating bacterial infections. The disclosed compounds are inhibitors of PPAT (phosphopantetheine adenyl transferase), and are useful in the treatment and prevention of diseases caused by bacteria, particularly bacteria dependent on PPAT, for example, species such Escherichia coli, Helicobacter pylori, Staphyloccocus aureus, and the like.Type: ApplicationFiled: November 26, 2008Publication date: August 13, 2009Applicant: MAXTHERA INC.Inventor: Roger FRECHETTE
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Publication number: 20090203912Abstract: The present invention relates to a process for the regioselective synthesis of compounds of the formula I, wherein R0; R1; R2; R3; R4; R5; A1; A2; A3; A4, Q and J have the meanings indicated in the claims. The present invention provides a direct palladium catalyzed, regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides useful for the production of pharmaceuticals, diagnostic agents, liquid crystals, polymers, herbicides, fungicidals, nematicidals, parasiticides, insecticides, acaricides and arthropodicides.Type: ApplicationFiled: January 14, 2009Publication date: August 13, 2009Applicant: SANOFI-AVENTISInventors: Jorge ALONSO, Andreas LINDENSCHMIDT, Marc NAZARE, Nis HALLAND, Omar RKYEK, Matthias URMANN
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Publication number: 20090197910Abstract: The present invention relates to a pharmaceutical composition for the treatment or prevention of viral infections comprising as an active principle at least one benzimidazole conjugates derivative having the general formula (I). The invention also relates to processes for the preparation of compounds according to the invention having above mentioned general formula and their use as a medicine or to treat or prevent viral infections.Type: ApplicationFiled: May 7, 2007Publication date: August 6, 2009Applicants: KATHOLIEKE UNIVERSITEIT LEUVEN, NATIONAL TSING HUA UNIVERSITYInventors: Johan Neyts, Asish R. Das, Shih Ching Hung, Jih Ru Hwu, Raghunath Singha
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Publication number: 20090197889Abstract: This invention provides for compounds, compositions, and methods that involve anti-proliferative and anti-neoplastic activity in cancer cells. In particular, a series of benzimidazole, purine, imidazopyridine, and imidazopyrizine compounds having selected substitution patterns are disclosed, and the activity of various subject compounds is demonstrated.Type: ApplicationFiled: January 30, 2009Publication date: August 6, 2009Applicant: SPELMAN COLLEGEInventor: Leyte L. Winfield
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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: 20090181957Abstract: This invention relates to compounds of the formula (I): or pharmaceutically acceptable salts thereof, wherein: A, B, R1, R2 and R3 are each as described herein, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by CB2 receptor binding activity such as, but not limited to, inflammatory pain, nociceptive pain, neuropathic pain, fibromyalgia, chronic low back pain, visceral pain, acute cerebral ischemia, pain, chronic pain, acute pain, post herpetic neuralgia, neuropathies, neuralgia, diabetic neuropathy, HIV-related neuropathy, nerve injury, rheumatoid arthritic pain, osteoarthritic pain, back pain, cancer pain, dental pain, fibromyalgia, neuritis, sciatica, inflammation, neurodegenerative disease, cough, broncho constriction, irritable bowel syndrome (IBS), inflammatory bowel disease (IBD), colitis, cerebrovascular ischemia, emesis such as cancer chemotherapy-induced emesis, rheumatoid arthritis, asthma, Crohn's disease, ulcerative colitis, asthmaType: ApplicationFiled: March 2, 2006Publication date: July 16, 2009Inventors: Kazuo Ando, Makoto Kawai, Tsutomu Masuda, Hirofumi Omura
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Publication number: 20090176986Abstract: An efficient syntheses for the preparation of the intermediate 2-oxo-1-(4-piperidinyl)-2,3-dihydro-1H-imidazo[4,5-b]pyridine dihydrochloride, and other salt forms of 2-oxo-1-(4-piperidinyl)-2,3-dihydro-1H-imidazo[4,5-b]pyridine.Type: ApplicationFiled: April 6, 2007Publication date: July 9, 2009Inventors: Mark McLaughlin, Michael Palucki, Karen Marcantonio
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Publication number: 20090176778Abstract: Provided are certain chemical entities, pharmaceutical compositions, and methods of treatment of a member of the flaviviradae family of viruses such as hepacivirus (Hepatitis C or HCV).Type: ApplicationFiled: August 8, 2008Publication date: July 9, 2009Inventors: Franz Ulrich Schmitz, Vincent W-F Tai, Roopa Rai, Christopher Don Roberts, Ali Dehghani Mohammad Abadi, Subramanian Baskaran, Irina Slobodov, Jack Maung, Martin Leon Neitzel
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Publication number: 20090176769Abstract: The present invention relates to CGRP receptor antagonists, pharmaceutical compositions thereof, and methods therewith for treating CGRP receptor-mediated diseases and conditions.Type: ApplicationFiled: December 13, 2007Publication date: July 9, 2009Inventors: Corey Anderson, Andreas Termin, Sara Hadida-Ruah, Pramod Joshi, Sanghee Yoo, Daniele Bergeron, Hayley Binch, Jon Come, Jingrong Cao, Suganthi Nanthakumar, Elaine Krueger, John Maxwell, Arnaud Le Tiran, Yusheng Liao
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Publication number: 20090170847Abstract: The inventive imidazopyridine derivative can be used in a pharmaceutical composition for preventing or treating diseases such as diabetes, obesity, dementia, cancer, and inflammation, since it can efficiently inhibit the activities of several protein kinases including glycogen synthase kinase-3 (GSK-3), aurora kinase, extracellular signal-regulated kinase (ERK), protein kinase B (AKT), and the likes, to control signal transductions thereof.Type: ApplicationFiled: January 23, 2007Publication date: July 2, 2009Inventors: Seung Chul Lee, Jin Seok Choi, Jung Hoon Oh, Boonsaeng Park, Yong Eun Kim, Jun Hee Lee, Dongkyu Shin, Cheol Min Kim, Young-Lan Hyun, Cheol Soon Lee, Joong-Myung Cho, Seonggu Ro
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Publication number: 20090170812Abstract: Substituted benzoimidazole compounds useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. Methods of making and using substituted benzoimidazole compounds, as well as pharmaceutical preparations thereof, in, e.g., reducing antibiotic resistance and inhibiting biofilms.Type: ApplicationFiled: June 25, 2007Publication date: July 2, 2009Applicant: Paratek Pharmaceuticals, Inc.Inventors: Michael N. Alekshun, Victoria Bartlett, Lynne Garrity-Ryan, Mark Grier, Oak K. Kim, Atul K. Verma
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Publication number: 20090163539Abstract: This invention relates to optically active substances of tenatoprazole, (+) and (?) -5-methoxy-2-{(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]sulfinyl}-1H-imidazo[4,5-b]pyridine. The compound and pharmaceutical compositions thereof are useful for anti-ulcer agent.Type: ApplicationFiled: January 26, 2009Publication date: June 25, 2009Applicant: MITSUBISHI PHARMA CORPORATIONInventors: Setsuo YAMASHITA, Kengo EBINA
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Publication number: 20090156607Abstract: The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: May 31, 2006Publication date: June 18, 2009Applicant: UCB, S.A.Inventors: Benoit Kenda, Yannick Quesnel, Ali Ates, Philippe Michel, Laurent Turet, Joel Mercier
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Patent number: 7547779Abstract: Novel inhibitors of Rho-kinases are disclosed.Type: GrantFiled: October 6, 2004Date of Patent: June 16, 2009Assignee: Glaxo Group LimitedInventors: Dennis Lee, Robert A. Stavenger, Krista B. Goodman, Mark A. Hilfiker, Haifeng Cui, Andrew Q. Viet, Joseph P. Marino
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Publication number: 20090124625Abstract: The present invention relates to novel compounds of formula (I) wherein W, n, X and W? are defined in the description; invention compounds are modulators of metabotropic glutamate receptors—subtype 5 (“mGluR5”) which are useful for the treatment of central nervous system disorders as well as other disorders modulated by mGluR5 receptors.Type: ApplicationFiled: June 17, 2005Publication date: May 14, 2009Applicant: Addex Pharmaceuticals SAInventors: Anne-Sophie Bessis, Christelle Bolea, Beatrice Bonnet, Mark Epping-Jordan, Nicolas Poirier, Sonia-Maria Poli, Jean-Philippe Rocher, Yves Thollon
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Patent number: 7531660Abstract: The present invention discloses the compound of Formula I and pharmaceutically acceptable salts and solvates thereof. The invention also relates to pharmaceutical compositions comprising the Compound of Formula I and its use in treating obesity, metabolic syndrome, diabetes, hepatic lipidosis or nonalcoholic fatty liver disease. The invention also relates to the use of a combination of the Compound of Formula I with additional therapeutic agents for treating obesity, metabolic syndrome, diabetes, hepatic lipidosis or nonalcoholic fatty liver disease.Type: GrantFiled: August 10, 2007Date of Patent: May 12, 2009Assignee: Schering CorporationInventors: Manuel de Lera Ruiz, Robert G. Aslanian, Michael Y. Berlin, Kevin D. McCormick, Chander S. Celly
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Patent number: 7528252Abstract: Compounds of formula (I) wherein: X is CH or CH—R2; R1 is C1-C6 linear or branched alkyl or C1-C6 linear or branched alkenyl; R2 is hydrogen, C1-C6 linear or branched alkyl or C1-C6 linear or branched alkenyl, C6-C14 aryl or C6-C14 aryl(C1-C6) linear or branched alkyl or C6-C14 aryl(C1-C6) linear or branched alkenyl, with the aryl group optionally substituted by one or more substituents, either the same or different, selected from the group consisting of halogen, hydroxy, C1-C6 alkoxy linear or branched or C1-C6 alkenyloxy linear or branched, amino, optionally mono- or disubstituted with C1-C6 linear or branched alkyl; R3 is NH2, or NHR4; R4 is C1-C6 alkyl or C1-C6 hydroxyalkyl, C1-C3 alkoxyalkyl, amino(C1-C6)alkyl, where the amino group is optionally substituted with one or two C1-C3 linear or branched alkyl groups, or with one or two C2-C3 alkenyl groups C6-C14 aryl or C6-C14 aryl(C1-C6)alkyl, with the aryl group optionally substituted by one or more substituents, either the same or different, selecteType: GrantFiled: May 4, 2007Date of Patent: May 5, 2009Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Tarzia Giorgio, Piersanti Giovanni, Giorgi Luca, Minetti Patrizia, Di Cesare Maria Assunta, Gallo Grazia, Giorgi Fabrizio
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Patent number: 7528251Abstract: The present invention concerns enantioselective preparation of sulphoxide derivatives or their salts. The method consist in performing an enantioselective oxidation of a sulphur of general formula (I) A —CH2—SB, wherein: A is a diversely substituted pyridinyl ring and B is a heterocyclic radical comprising an imidazo-pyridinyl ring, using an oxidizing agent in the presence of a titanium (IV)-based catalyst and a chiral ligand consisting of a cyclic beta or gamma-amino-alcohol, in an organic solvent, followed, if required, by salt formation with a base. The invention is useful for preparing sulphoxides useful in therapeutics.Type: GrantFiled: October 5, 2005Date of Patent: May 5, 2009Assignee: Sidem Pharma SAInventors: Avraham Cohen, Suzy Charbit, François Schutze, Frédéric Martinet, Patricia Gizecki
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Patent number: 7528149Abstract: This invention concerns compounds of formula (I) prodrugs, addition salts, or stereochemically isomeric forms thereof for use as, inter alia, respiratory syncytial virus replication inhibitors; their preparation, compositions containing them and methods of their use in treating respiratory syncytial viral infections.Type: GrantFiled: January 22, 2007Date of Patent: May 5, 2009Assignee: Janssen Pharmaceutica N.V.Inventors: Frans Eduard Janssens, Kathleen Petrus Marie-José Meersman, François Maria Sommen, Koenraads Jozef Lodewijk Marcell Andries
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Patent number: 7524847Abstract: The objective of this invention is to provide novel compounds that show excellent DPPIV-inhibiting activity. The present invention provides compounds represented by the general formula (I), salts thereof, or hydrates thereof, [wherein, T1 stands for a monocyclic or bicyclic 4 to 12-membered heterocycle having 1 or 2 nitrogen atoms in the ring, which may have substituents; in formula (I), the following formula represents a double bond or a single bond; X3 denotes an oxygen atom or a sulfur atom; X1 denotes a C2-6 alkyl group which may have substituents; Z1 denotes a nitrogen atom or the formula —CR3=; Z2 and Z3 each independently denote a nitrogen atom, the formula —CR1=, a carbonyl group, or the formula —NR2—; R1, R2, R3, and X2 each independently denote a C1-6 alkyl group which may have substituents, and such].Type: GrantFiled: December 2, 2003Date of Patent: April 28, 2009Assignee: Eisai R&D Management Co., Ltd.Inventors: Kazunobu Kira, Richard Clark, Seiji Yoshikawa, Taisuke Uehara
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Publication number: 20090105295Abstract: Imidazo ring compounds (e.g., imidazoquinolines, 6,7,8,9-tetrahydroimidazoquinolines, imidazonaphthyridines, and imidazopyridines) with a hydroxylamine substituent at the 2-position, pharmaceutical compositions containing the compounds, intermediates, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.Type: ApplicationFiled: November 12, 2004Publication date: April 23, 2009Applicant: Coley Pharmaceutical Group, Inc.Inventors: Tushar A. Kshirsagar, Gregory D. Lundquist, JR., David T. Amos, Joseph F. Dellaria, JR., Bernhard M. Zimmermann, Philip D. Heppner
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Patent number: 7521459Abstract: The invention relates to a method and composition for treating aged or photo-damaged skin. In one embodiment, the invention includes using a composition comprising about 1% to about 2% of 1-isobutyl-1H-imidazo [4,5,-C] quinolin-4-amine in a topical preparation or cream. In further embodiments, the method includes identifying topical compositions that can diagnose or identify precancerous region of the skin, as well as methods for treating aged or photo-damaged skin by applying a Toll-like receptor activator, such as 1-isobutyl-1H-imidazo [4,5,-C] quinolin-4-amine.Type: GrantFiled: July 28, 2003Date of Patent: April 21, 2009Assignee: Metabeauty Inc.Inventors: Leslie Baumann, Esperanza Welsh
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Publication number: 20090099172Abstract: The present invention relates to 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives having the general Formula I to pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S related diseases such as atherosclerosis, obesity, inflammation and immune disorders, such as rheumatoid arthritis, psoriasis, cancer, and chronic pain, such as neuropathic pain.Type: ApplicationFiled: July 15, 2008Publication date: April 16, 2009Inventors: Jiaqiang Cai, Zoran Rankovic, Philip Stephen Jones, David Jonathan Bennett, Xavier Fradera
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Publication number: 20090092854Abstract: The present invention relates to organic light emitting devices (OLEDs), and more specifically to phosphorescent organic materials used in such devices. More specifically, the present invention relates to emissive phosphorescent material which comprise at least one tridentate ligand bound to a metal center, wherein at least one of the bonds to the tridentate ligand is a carbon-metal bond.Type: ApplicationFiled: October 4, 2007Publication date: April 9, 2009Inventors: Robert W. Walters, Jui-Yi Tsai, Peter Borden Mackenzie, Scott Beers
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Publication number: 20090088570Abstract: An organic electroluminescent device, which has, between a pair of electrodes, at least one organic layer including a light-emitting layer, in which the organic layer contains a specific tetraphenylene compound, and in which the light-emitting layer contains a phosphorescent material; and a specific tetraphenylene compound that can be used in the device.Type: ApplicationFiled: November 20, 2008Publication date: April 2, 2009Applicant: FUJIFILM CORPORATIONInventors: Jun OGASAWARA, Tatsuya Igarashi, Satoshi Sano
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Publication number: 20090088569Abstract: The present invention relates to 2-amino-imidazo[4,5-d]pyridazin-4-ones and 2-amino-imidazo[4,5-c]pyridin-4-ones of general formula wherein R1 to R4 and X are defined as in claims 1 to 6, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: ApplicationFiled: December 5, 2008Publication date: April 2, 2009Inventors: Matthias ECKHARDT, Frank HIMMELSBACH, Elke LANGKOPF, Norbert HAUEL, Mohammad TADAYYON, Leo THOMAS
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Patent number: 7511058Abstract: Disclosed are compounds of the Formula III and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9 R10, and W are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.Type: GrantFiled: April 24, 2006Date of Patent: March 31, 2009Assignee: Array BioPharma Inc.Inventors: T. Brian Hurley, Eli M. Wallace, Joseph P. Lyssikatos, James Blake
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Patent number: 7507746Abstract: This invention relates to optically active substances of tenatoprazole, (+) and (?)-5-methoxy-2-{(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]sulfinyl}-1H-imidazo[4,5-b]pyridine. The compound and pharmaceutical compositions thereof are useful for anti-ulcer agent.Type: GrantFiled: February 23, 2004Date of Patent: March 24, 2009Assignee: Mitsubishi Pharma CorporationInventors: Setsuo Yamashita, Kengo Ebina
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Publication number: 20090076070Abstract: [Problems] To provide a useful compound as an active ingredient for a preventing and/or treating agent for rejection in the transplantation of an organ, bone marrow, or a tissue, an autoimmune disease, or the like, which has an excellent S1P1 agonist activity.Type: ApplicationFiled: October 2, 2008Publication date: March 19, 2009Applicant: Astellas Pharma Inc.Inventors: Hironori HARADA, Kazuyuki Hattori, Kazuya Fujita, Masataka Morita, Sunao Imada, Yoshito Abe, Hiromichi Itani, Tatsuaki Morokata, Hideo Tsutsumi