Plural Ring Nitrogens In The Polycyclo Ring System Patents (Class 546/199)
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Publication number: 20120065210Abstract: There are provided compounds of formula I or a pharmaceutically acceptable salt thereof, wherein X, Y, R1, R1?, R2, R2?, R3, R4, R5 are as defined herein. The compounds exhibit activity as anticancer agents.Type: ApplicationFiled: September 7, 2011Publication date: March 15, 2012Inventors: Xin-Jie Chu, Qingjie Ding, Nan Jiang, Jin-Jun Liu, Tina Morgan Ross, Zhuming Zhang
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Publication number: 20120059016Abstract: The present invention relates to piperidine and pyrazine derivatives according to formulae (Ia), (Ib) and (II) as autotaxin inhibitors and the use of such compounds for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by increased lysophosphatic acid levels and/or the activation of autotaxin, in particular of different cancers.Type: ApplicationFiled: March 3, 2010Publication date: March 8, 2012Inventors: Kai Schiemann, Melanie Schultz, Wolfgang Staehle
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Publication number: 20120053166Abstract: The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular PI3-kinase activity.Type: ApplicationFiled: March 5, 2010Publication date: March 1, 2012Inventors: Julie Nicole Hamblin, Zoe Alicia Harrison, Paul Spencer Jones, Suzanne Elaine Keeling, Joelle Le, Christopher James Lunniss, Nigel James Parr
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Publication number: 20120046275Abstract: The present invention is directed to synthetic cytoskeletal active compounds that are inhibitors of rho-associated protein kinase. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with cytoskeletal reorganization. In one embodiment of the invention, the method treats increased intraocular pressure, such as primary open-angle glaucoma. The method comprises administering to a subject a therapeutically effective amount of a cytoskeletal active compound of Formula I or Formula II, wherein said amount is effective to influence the actomyosin interactions, for example by leading to cellular relaxation and alterations in cell-substratum adhesions.Type: ApplicationFiled: October 13, 2011Publication date: February 23, 2012Inventors: John W. Lampe, Paul S. Watson, David J. Slade, Ward M. Peterson, Christopher S. Crean, Jason L. Vittitow, Jonathan Bryan DeCamp, Nicholas F. Pelz
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Publication number: 20120046303Abstract: Compounds which inhibit the activity of poly(ADP-ribose)polymerase (PARP), compositions containing the compounds and methods of treating diseases using them are disclosed.Type: ApplicationFiled: October 27, 2011Publication date: February 23, 2012Applicant: ABBOTT LABORATORIESInventors: Virajkumar B. Gandhi, Vincent L. Giranda, Jianchun Gong, Thomas D. Penning, Gui-Dong Zhu
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Patent number: 8119661Abstract: Compounds of Formula I, or pharmaceutically acceptable salts thereof: wherein R2, R3, X, m and n 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: September 8, 2008Date of Patent: February 21, 2012Assignee: AstraZeneca ABInventors: Yun-Xing Cheng, Xuehong Luo, Vijayaratnam Santhakumar, Miroslaw Jerzy Tomaszewski
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Publication number: 20120041028Abstract: Compounds of formula (I), salts and solvates are provided: Uses of the compounds for therapy, for example in the treatment of psychotic disorders and cognitive impairment, are also disclosed.Type: ApplicationFiled: October 27, 2011Publication date: February 16, 2012Inventors: David Gwyn COOPER, Ian Thomas Forbes, Vincenzo Garzya, Jian Jin, Yann Louchart, Graham Walker, Paul Adrian Wyman
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Publication number: 20120041027Abstract: Compounds of formula (I) and salts and solvates are provided: wherein Uses of the compounds for therapy, for example in the treatment of psychotic disorders and cognitive impairment, are also disclosed.Type: ApplicationFiled: October 27, 2011Publication date: February 16, 2012Inventors: David Gwyn COOPER, Ian Thomson Forbes, Vincenzo Garzya, Jian Jin, Yann Louchart, Graham Walker, Paul Adrian Wyman
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Patent number: 8114899Abstract: Compounds corresponding to the formula (I) as defined in the disclosure, as well as methods for making such compounds, intermediates employed in such methods, pharmaceutical compositions containing the compounds of the invention, and methods of treatment using them.Type: GrantFiled: January 27, 2009Date of Patent: February 14, 2012Assignee: Sanofi-AventisInventors: Laurent DuBois, Yannick Evanno, Christian Maloizel, Mireille Sevrin
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Patent number: 8114865Abstract: 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 dysregulated protein kinase activity, like cancer formula (I).Type: GrantFiled: December 14, 2007Date of Patent: February 14, 2012Assignee: Nerviano Medical Sciences S.R.L.Inventors: Tiziano Bandiera, Andrea Lombardi Borgia, Marcella Nesi, Ettore Perrone, Roberto Bossi, Paolo Polucci
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Publication number: 20120035131Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I: wherein R1, R2, R3A, R3B, R4, R5, R6, R7, R8, and X are as defined in the detailed description of the invention. Corresponding pharmaceutical compositions, methods of treatment, and intermediates are also disclosed.Type: ApplicationFiled: October 20, 2011Publication date: February 9, 2012Inventors: Marvin J. Meyers, Graciela B. Arhancet, Xiangyang Chen, Susan Hockerman, Scott A. Long, Matthew W. Mahoney, David B. Reitz, Joseph G. Rico
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Publication number: 20120035164Abstract: The invention is directed to novel indole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula I: where R1, R2, R3, U and V are defined below and to pharmaceutically acceptable salts thereof. The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKK?) activity, such as rheumatoid arthritis, asthma, and COPD (chronic obstructive pulmonary disease). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: ApplicationFiled: October 14, 2011Publication date: February 9, 2012Inventors: Jianghe DENG, Jeffrey K. KERNS, Qi JIN, Guoliang LIN, Xichen LIN, Michael LINDENMUTH, Christopher NEIPP, Hong NIE, Sonia M. THOMAS, Katherine L. WIDDOWSON
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Publication number: 20120035214Abstract: The present invention relates to biaryl piperidine-based renin inhibitor compounds, and their use in treating cardiovascular events and renal insufficiency.Type: ApplicationFiled: April 1, 2010Publication date: February 9, 2012Applicants: Merck Canada Inc., Merck Sharp & Dohme Corp.Inventors: Daniel J. McKay, Melissa Arbour, Renee Aspiotis, Austin Chen, Pierre-Andre Fournier, Michel Gallant, Yongxin Han, Helene Juteau, Patrick Lacombe, Sebastien Laliberte, Sophie Lauzon, Carmela Molinaro, Paul O'Shea, Yeeman Ramtohul, Daniel Simard, Dwight MacDonald, Bruce Mackay, Christophe Mellon, Krista Morley, Chit Tsui, Sarah Jennifer Dolman, Greg Hughes, Jacob Janey
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Publication number: 20120035173Abstract: This invention relates to compounds, pharmaceutical compositions and methods for use in the prevention and treatment of cerebral insufficiency, including enhancement of receptor functioning in synapses in brain networks responsible for basic and higher order behaviors. These brain networks, which are involved in regulation of breathing, and cognitive abilities related to memory impairment, such as is observed in a variety of dementias, in imbalances in neuronal activity between different brain regions, as is suggested in disorders such as Parkinson's disease, schizophrenia, respiratory depression, sleep apneas, attention deficit hyperactivity disorder and affective or mood disorders, among numerous others. In a particular aspect, the invention relates to compounds useful for treatment of such conditions, and methods of using these compounds for such treatment.Type: ApplicationFiled: September 6, 2011Publication date: February 9, 2012Inventors: Leslie Street, Rudolf Mueller, Steven Lee
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Patent number: 8110578Abstract: Provided herein are Heteroaryl Compounds having the following structure: wherein R1-R4 are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, neurodegenerative diseases, diabetes, obesity, neurological disorders, age-related diseases, or cardiovascular conditions, comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof.Type: GrantFiled: October 26, 2009Date of Patent: February 7, 2012Assignee: Signal Pharmaceuticals, LLCInventors: Sophie Perrin-Ninkovic, Roy L. Harris, John Sapienza, Graziella Shevlin, Patrick Papa, Branden Lee, Garrick Packard, Lida Tehrani, Jingjing Zhao, Jennifer Riggs, Jason Parnes, Deborah Mortensen, Weiming Xu, Loui Madakamutil, Kimberly Fultz, Rama K. Narla, Sabita Sankar, Jan Elsner
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Publication number: 20120028962Abstract: A compound represented by the following formula or a salt thereof, which has an GPR119 agonist action, is useful for the prophylaxis or treatment of diabetes, obesity and the like, and shows superior efficacy: wherein P: substituted 6-membered aromatic ring, Q: (substituted) 6-membered aromatic ring, CR4aR4b, NR4c, O, S, SO or SO2 {R4a-4c: H etc.}, L1: (substituted) C1-5 alkylene, L2: a bond or (substituted) C1-3 alkylene, L3-4: (substituted) C1-3 alkylene, R1: H, X, CN, (substituted) hydrocarbon, (substituted) heterocycle or (substituted) OH, or (substituted) 4- to 8-membered (heterocyclic) ring together with A1, R2: H, CN, (substituted) hydrocarbon, and R3a: —COSRA1, (substituted) 5- or 6-membered aromatic ring {RA1: (substituted) hydrocarbon or (substituted) heterocycle}.Type: ApplicationFiled: February 17, 2010Publication date: February 2, 2012Inventors: Kentaro Rikimaru, Hiroshi Imoto, Masahiro Kamaura
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Patent number: 8106191Abstract: New compounds are disclosed for multimerizing immunophilins and proteins containing immunophilin or immunophilin-related domains. The compounds are of the formula M-L-Q where M is a synthetic ligand for an FKBP protein.Type: GrantFiled: June 13, 2003Date of Patent: January 31, 2012Assignee: ARIAD Pharmaceuticals, Inc.Inventors: Dennis A. Holt, Terence P. Keenan, Tao Guo, Edgardo Laborde, Wu Yang
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Publication number: 20120022090Abstract: The present invention is concerned with novel substituted benzoxazole, benzimidazole, oxazolopyridine and imidazopyridine derivatives of Formula (I) wherein R1, R2, R3, R4, X, A1, A2, A3, A4, Y1, Y2, Y3 and Z have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.Type: ApplicationFiled: February 15, 2010Publication date: January 26, 2012Inventors: Henricu Jacobus Maria Gijsen, Francois Paul Bischoff, Wei Zhuang, Sven Franciscus Anna Van Brandt, Michel Surkyn, Mirko Zaja, Didier Jean-Claude Berthelot, Michel Anna Jozef Cleyn, Gregor James Macdonald, Daniel Oehlrich
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Publication number: 20120022253Abstract: Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.Type: ApplicationFiled: September 29, 2011Publication date: January 26, 2012Applicant: ABBOTT LABORATORIESInventors: Yujia Dai, Steven K. Davidsen, Anna M. Ericsson, Kresna Hartandi, Zhiqin Ji, Michael R. Michaelides
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Publication number: 20120015932Abstract: Indazole compounds, processes for their preparation, intermediates usable in these processes, pharmaceutical compositions containing such compounds and their use in therapy.Type: ApplicationFiled: February 24, 2010Publication date: January 19, 2012Inventors: Heather Hobbs, Simon Teanby Hodgson, Yannick Maurice LaCroix, Deborah Needham, Nigel James Parr, Panayiotis Alexandrou Procopiou, Timothy John Ritchie, Michael David Woodrow
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Publication number: 20120015959Abstract: Compounds of the formula (I), in which Het, R, X, Y, R1 and p have the meanings indicated in claim 1, are autotaxin inhibitors and can be employed for the treatment of tumours.Type: ApplicationFiled: March 3, 2010Publication date: January 19, 2012Inventors: Wolfgang Staehle, Kai Schiemann, Melanie Schultz
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Publication number: 20120004196Abstract: 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: May 4, 2011Publication date: January 5, 2012Applicant: 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, Yi Gao, 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, 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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Publication number: 20110319393Abstract: This invention is directed to compounds and salts that are generally useful as anthelmintic agents or as intermediates in processes for making anthelmintic agents. This invention also is directed to processes for making the compounds and salts, pharmaceutical compositions and kits comprising the compounds and salts, uses of the compounds and salts to make medicaments, and treatments comprising the administration of the compounds and salts to animals in need of the treatments.Type: ApplicationFiled: March 17, 2010Publication date: December 29, 2011Inventors: Christophe Pierre Alain Chassaing, Thorsten Meyer
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Publication number: 20110313153Abstract: The invention relates generally to the treatment of diseases of the respiratory system such as asthma and chronic obstructive pulmonary disease. More particularly, the present invention relates to methods of treating and preventing asthmatic airway inflammation. The treatment involves the administration of a 5-HT4 receptor antagonist to the subject in need thereof; more in particular the administration of aroylated 4-aminomethylpiperidine derivatives as defined herein. Other aspects of the invention are directed to compositions for treating or preventing respiratory disorders, including pharmaceutical compositions.Type: ApplicationFiled: January 28, 2010Publication date: December 22, 2011Inventors: Ann Meulemans, Leen Thielemans, Joris De Maeyer, Jan Schuurkes
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Publication number: 20110311485Abstract: The present disclosure relates to 1, 2, 4 oxadiazole derivatives of formula (I) as well as pharmaceutical compositions comprising them, and their use in therapy as agonists of the S1P1 receptors.Type: ApplicationFiled: December 15, 2009Publication date: December 22, 2011Applicant: ALMIRALL S.A.Inventors: Victor Giulio Matassa, Nuria Aguilar Izquierdo, Marta Mir Cepeda, Marta Carrascal Riera, Silvia Fonquerna Pou, Aranzazu Cardus Figueras, Julio Cesar Castro Palomino Laria, Montserrat Erra Sola
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Publication number: 20110312949Abstract: The use of substituted amides for modulating the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11?HSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.Type: ApplicationFiled: August 30, 2011Publication date: December 22, 2011Applicant: HIGH POINT PHARMACEUTICALS, LLCInventors: John Paul Kilburn, Henrik Sune Andersen, Gita Camilla Tejlgaard Kampen, Soren Ebdrup
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Publication number: 20110306599Abstract: Provided is an agent for the treatment or prophylaxis of inflammatory diseases, allergic diseases, autoimmune diseases, transplant rejection or the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein each symbol is as described in the specification.Type: ApplicationFiled: November 24, 2010Publication date: December 15, 2011Applicant: JAPAN TOBACCO INC.Inventors: Teruhiko INOUE, Tetsudo KAYA, Shinichi KIKUCHI, Koji MATSUMURA, Ritsuki MASUO, Motoya SUZUKI, Michihide MAEKAWA
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Publication number: 20110306611Abstract: 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: August 3, 2009Publication date: December 15, 2011Applicant: Paratek Pharmaceuticals, Inc.Inventors: Michael N. Alekshun, Victor Amoo, Oak K. Kim, Atul K. Verma
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Publication number: 20110306638Abstract: The invention relates to a benzisoxazolyl piperidine derivative having the following general formula, a salt or a hydrate thereof, wherein R, X, Y, R? and T are defined as in the specification. Such compounds have serotonin system modulating effects such as antagonizing effect on 5-HT2A and inhibitory effect on 5-HT reuptake. The compounds have good analgesic and sedative activities with mild toxic and side effects. The invention also relates to a composition comprising said derivative and the use thereof.Type: ApplicationFiled: December 22, 2009Publication date: December 15, 2011Applicant: NHWA PHARMA. CORPORATIONInventors: Jianqi Li, Guan Wang, Guisen Zhang, Na Lv, Guangjun Jiao, Shicheng Liu, Shixia Zhou
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Publication number: 20110301192Abstract: The present invention provides compounds that inhibit cyclin kinase inhibitor p21, such as compounds of formula I. The present invention also provides compositions including compounds of Formula I and a pharmaceutically acceptable excipient. In addition, the present invention provides methods of inhibiting cyclin kinase inhibitor p21 and of treating cancer.Type: ApplicationFiled: September 29, 2009Publication date: December 8, 2011Applicant: The regents of the University of CaliforniaInventors: Robert Weiss, See-Hyoung Park, Kit S. Lam, Ruiwu Liu
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Publication number: 20110300072Abstract: Use of benzimidazole-derived compounds of formula (I) according to the following structure, wherein x is a heteroatom selected from N, S, O, P, SO, SO2 and SO3, preferably from N, S and SO3 and most preferably from N and SO3; n may be 0 or 1, R1 is a group selected from formula (II) and formula (III) and R2 is a group selected from H and formula (IV) since the aforesaid serves for the production of a formulation used as a specific marker in the case of neurodegenerative diseases and tau pathologies.Type: ApplicationFiled: July 22, 2009Publication date: December 8, 2011Applicant: SERVICIOS CIENTIFICOS NEUROINNOVATION LTDA.Inventors: Ricardo Maccioni Baraona, Leonel Rojo, Rodrigo Kuljis Azocar
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Publication number: 20110301146Abstract: GSK-3beta inhibitors comprising 7-Hydroxy-benzoimidazole-4-yl-methanone Derivatives are provided. For example, the inhibitors have following general formula (I).Type: ApplicationFiled: September 29, 2009Publication date: December 8, 2011Applicant: ONCOTHERAPY SCIENCE, INC.Inventors: Yo Matsuo, Ryuji Ohsawa, Shoji Hisada
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Patent number: 8071622Abstract: The present invention is concerned with novel indol-2-yl-carbonyl-piperidin-benzoimidazolon and indol-2-yl-carbonyl-piperidin-benzoxazolon derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases. In particular, the present invention concerns compounds of formula (I) wherein R1 to R11, X and Y are as defined in the specification.Type: GrantFiled: November 29, 2007Date of Patent: December 6, 2011Assignee: Hoffman-La Roche Inc.Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
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Patent number: 8071623Abstract: The present invention relates to compounds of formula I: and pharmaceutically acceptable salts, stereoisomers or tautomers thereof which are inhibitors of poly (ADP-ribose) polymerase (PARP) and thus useful for the treatment of cancer, inflammatory diseases, reperfusion injuries, ischemic conditions, stroke, renal failure, cardiovascular diseases, vascular diseases other than cardiovascular diseases, diabetes, neurodegenerative diseases, retroviral infection, retinal damage or skin senescence and UV-induced skin damage, and as chemo- and/or radiosensitizers for cancer treatment.Type: GrantFiled: January 8, 2008Date of Patent: December 6, 2011Assignee: Instituto di Ricerche di Biologia Molecolare P. Angeletti SpAInventors: Philip Jones, Jesus Maria Ontoria Ontoria, Rita Scarpelli, Carsten Schultz-Fademrecht
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Patent number: 8071779Abstract: The present invention is directed to synthetic cytoskeletal active compounds that are inhibitors of rho-associated protein kinase. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with cytoskeletal reorganization. In one embodiment of the invention, the method treats increased intraocular pressure, such as primary open-angle glaucoma. The method comprises administering to a subject a therapeutically effective amount of a cytoskeletal active compound of Formula I or Formula II, wherein said amount is effective to influence the actomyosin interactions, for example by leading to cellular relaxation and alterations in cell-substratum adhesions.Type: GrantFiled: December 17, 2007Date of Patent: December 6, 2011Assignee: Inspire Pharmaceuticals, Inc.Inventors: John W. Lampe, Paul S. Watson, David J. Slade, Ward M. Peterson, Christopher S. Crean, Jason L. Vittitow, Jonathan Bryan DeCamp, Nicholas F. Pelz
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Publication number: 20110294780Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacType: ApplicationFiled: May 24, 2011Publication date: December 1, 2011Inventors: Gilles Bignan, Wing Cheung, Micheal Gaul, Hui Huang, Xun Li, Raymond Patch, Sharmila Patel, Mark Player, Guozhang Xu, Bao-Ping Zhao, Jian Liu
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Publication number: 20110294777Abstract: Substituted bicyclic beta-lactams of Formula I: (I), are ?-lactamase inhibitors, wherein a, X, R1 and R2 are defined herein. The compounds and pharmaceutically acceptable salts thereof are useful in the treatment of bacterial infections in combination with ?-lactam antibiotics. In particular, the compounds can be employed with a ?-lactam antibiotics (e.g., imipenem, piperacillin, or ceftazidime) against microorganisms resistant to ?-lactam antibiotics due to the presence of the ?-lactamases.Type: ApplicationFiled: January 15, 2009Publication date: December 1, 2011Inventors: Timothy A. Blizzard, Helen Chen, Candido Gude, Jeffrey D. Hermes, Jason Imbriglio, Seongkon Kim, Jane Y. Wu, Sookhee Ha, Christopher J. Mortko, Ian Mangion, Nelo Rivera, Rebecca T. Ruck, Michael Shevlin
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Publication number: 20110295013Abstract: Provision of an industrial method of producing a 1-(4-piperidinyl)benzimidazolone derivative in a high yield at a low cost. A production method of 1-(4-piperidinyl)benzimidazolone derivative (1) or a salt thereof according to the following steps. [step 1] a step of subjecting a piperidone compound (2) and an aniline compound (3) to a reductive amination reaction to give to a compound (4) [step 2] a step of reacting the compound (4) with di-t-alkyl dicarbonate or N,N?-disuccinimidyl carbonate to give the 1-(4-piperidinyl)benzimidazolone derivative (1) wherein R1 is optionally substituted alkyl or an optionally substituted cyclic group, and R2 is optionally substituted alkyl, optionally substituted alkenyl or optionally substituted aryl.Type: ApplicationFiled: February 3, 2010Publication date: December 1, 2011Inventors: Hiroshi Iwamura, Yoshihiro Tarao
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Publication number: 20110294808Abstract: Disclosed indazoles compounds that are useful as antagonists of CCR1 activity and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: July 18, 2011Publication date: December 1, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Daniel KUZMICH, Can MAO, Alan David SWINAMER, David Smith THOMSON
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Patent number: 8067613Abstract: Compounds which inhibit the activity of poly(ADP-ribose)polymerase (PARP), compositions containing the compounds and methods of treating diseases using them are disclosed.Type: GrantFiled: July 15, 2008Date of Patent: November 29, 2011Assignee: Abbott LaboratoriesInventors: Virajkumar B. Gandhi, Vincent L. Giranda, Jianchun Gong, Thomas D Penning, Gui-Dong Zhu
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Patent number: 8067603Abstract: The invention relates to a group of novel 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 imidazolone 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 22, 2004Date of Patent: November 29, 2011Assignee: Solvay Pharmaceuticals B.V.Inventors: Jacobus A. J. Den Hartog, Gustaaf J. M. Van Scharrenburg, Herman H. Van Stuivenberg, Tinka Tuinstra, Jan-Willem Terpstra
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Publication number: 20110281843Abstract: 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: December 15, 2009Publication date: November 17, 2011Applicant: NERVIANO MEDICAL SCIENCES S.r.l.Inventors: Maria Menichincheri, Jay Aaron Bertrand, Chiara Marchionni, Marcella Nesi, Paolo Orsini, Achille Panzeri
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Publication number: 20110281868Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A1, A2, A3 and L are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as aurora and KDR.Type: ApplicationFiled: May 12, 2011Publication date: November 17, 2011Applicant: ABBOTT LABORATORIESInventors: Michael R. Michaelides, James H. Holms, Douglas H. Steinman
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Publication number: 20110281840Abstract: This invention relates to compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein X, R1, R2, R3, R4, R5, R6, R7, k, m, n, p, q, r and s 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 activity.Type: ApplicationFiled: January 22, 2010Publication date: November 17, 2011Inventors: Kazuo Ando, Yasuhiro Iwata
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Publication number: 20110282066Abstract: [Object] A screening method for a compound which is useful as an agent for treating 17?HSD type 5-related diseases and/or an agent for treating 17?HSD type 5-related cancer such as prostate cancer is provided. [Means for Solution] The present invention has been completed by establishing a screening method for a compound which is useful for treating 17?HSD type 5-related diseases, by manifesting a tumor by transplanting tumor cells to, for example, an immunodeficient mouse, topically administering a steroid which is a biosynthetic substance for a hormone into the tumor, and measuring the level of a hormone produced in the tumor.Type: ApplicationFiled: January 26, 2010Publication date: November 17, 2011Inventors: Takashi Furutani, Kentaro Enjo, Aya Kikuchi, Sadao Kuromitsu, Yukitaka Ideyama, Tomoyuki Suzuki, Ryoko Kurihara
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Publication number: 20110275612Abstract: Disclosed is a compound of formula (I). Wherein R1, R2Ar and Cy are as defined herein, or a pharmaceutically acceptable salt thereof. Also disclosed are pharmaceutical compositions of the compound of formula (I), methods of making the compounds of formula I, and methods of using the compounds of formula (I) to treat a disorder associated with activation of CCR10.Type: ApplicationFiled: May 14, 2009Publication date: November 10, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Derek Cogan, Alexander Heim-Riether, Wang Mao, Craig Andrew Miller, Philip Dean Ramsden, Lana Louise Smith Keenan, Roger John Snow, Jiang-Ping Wu, Yu Yang
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Patent number: 8053431Abstract: The use of substituted amides for modulating the activity of 11-hydroxysteroid dehydrogenase type 1 (11HSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11HSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.Type: GrantFiled: November 1, 2006Date of Patent: November 8, 2011Assignee: High Point Pharmaceuticals, LLCInventors: John Paul Kilburn, Henrik Sune Andersen, Gita Camilla Tejlgaard Kampen, Soren Ebdrup
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Publication number: 20110269742Abstract: Disclosed are Serotonin 5-HT2B receptor inhibitors of the formula I. Also disclosed are methods of making and methods of using these compounds.Type: ApplicationFiled: December 14, 2009Publication date: November 3, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Derek Cogan, Neil Moss, Christopher Ronald Sarko, Samantha Jayne Bamford, Pui Leng Loke, Spencer Charles R. Napier, Heather Tye, Mark Whittaker
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Publication number: 20110263648Abstract: The invention relates to compounds of formula (I) wherein R1, R2, R3, R4, A, B, W and n are as defined in the description, and to pharmaceutically acceptable salts of such compounds. These compounds are useful as calcium channel blockers.Type: ApplicationFiled: October 21, 2009Publication date: October 27, 2011Inventors: Kurt Hilpert, Francis Hubler, Dorte Renneberg
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Publication number: 20110263566Abstract: 7-Hydroxy-benzoimidazole-4-yl-methanone Derivatives, which are useful for PBK inhibitors, are provided.Type: ApplicationFiled: July 30, 2009Publication date: October 27, 2011Inventors: Yo Matsuo, Yingfu Li, Joel Walker, Feryan Ahmed, Ryuji Ohsawa, Shoji Hisada