Plural Ring Nitrogens In The Polycyclo Ring System Patents (Class 546/199)
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Patent number: 8426604Abstract: 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: GrantFiled: February 16, 2011Date of Patent: April 23, 2013Assignee: Janssen Pharmaceutica NVInventors: Gilles Bignan, Micheal Gaul, Guozhang Xu, Bao-Ping Zhao
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Publication number: 20130096084Abstract: The present invention provides a compound of the Formula I: (Formular I should be inserted here) or a pharmaceutically acceptable salt, solvate or ester thereof, wherein R, R1, R2 and R3 are as defined herein. The compounds are ERK inhibitors. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same.Type: ApplicationFiled: June 22, 2011Publication date: April 18, 2013Inventors: Yongqi Deng, Liang Zhu, Gerald W. Shipps, JR., Sie-Mun Lo, Binyuan Sun, Xiaohua Huang, Corey Bienstock, Alan B. Cooper, Xiaolei Gao, Xin Yao, Hugh Y. Zhu, Joseph M. Kelly, Sobhana Babu Boga, Abdul-Basit Alhassan, Jayaram R. Tagat, Umar Faruk Mansoor, Kevin J. Wilson, Brendan M. O'Boyle, Matthew Hersh Daniels, Adam Schell, Phieng Siliphaivanh, Christian Fischer
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Publication number: 20130090342Abstract: The invention relates to new derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of one or more IGF-1R mediated disorders or diseases.Type: ApplicationFiled: June 16, 2011Publication date: April 11, 2013Applicant: NOVARTIS AGInventors: Frederic Berst, Pascal Furet, Andreas Marzinzik
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Patent number: 8415486Abstract: The present invention describes compounds, processes for their preparation, pharmaceutical compositions containing them, and their use in therapy.Type: GrantFiled: May 27, 2010Date of Patent: April 9, 2013Assignee: TetraLogic Pharmaceuticals Corp.Inventors: Stephen M. Condon, Yijun Deng, Matthew D. Alexander, Matthew G. Laporte
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Publication number: 20130085150Abstract: Compounds represented by formula I or pharmaceutically acceptable salts thereof, wherein A, B, B?, X, Y, R1, R2, R2?, R3, R3?, R4, R4?, R5, R5?m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.Type: ApplicationFiled: September 24, 2012Publication date: April 4, 2013Applicant: Vertex Pharmaceuticals IncorporatedInventors: Oswy Z. Pereira, John Maxwell, Youssef L. Bennani, Sanjoy Kumar Das, Laval Chan Chun Kong, Jagadeeswar T. Reddy, Simon Giroux, Kevin M. Cottrell, Mark A. Morris
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Publication number: 20130085161Abstract: The invention relates to new derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of one or more IGF-1R mediated disorders or diseases.Type: ApplicationFiled: June 16, 2011Publication date: April 4, 2013Applicant: NOVARTIS AGInventors: Frederic Berst, Pascal Furet, Andreas Marzinzik, Frederic Stauffer
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Patent number: 8410089Abstract: 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, A1: 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: GrantFiled: February 17, 2010Date of Patent: April 2, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Kentaro Rikimaru, Hiroshi Imoto, Masahiro Kamaura
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Publication number: 20130079339Abstract: The invention discloses compounds of formula I wherein Y is a group of formula A, B, C, D, or E: and W, Q, n, R1, R2, R3, U1-U5, J and K have the meanings given in the description. The compounds of formula I are TRPV1 antagonists and are useful as active ingredients of pharmaceutical compositions for the treatment of pain and other conditions ameliorated by the inhibition of the vanilloid receptor TRPV1.Type: ApplicationFiled: December 22, 2010Publication date: March 28, 2013Applicant: PHARMESTE S.R.L.Inventors: Mauro Napoletano, Marcello Trevisani, Maria Giovanna Pavani, Francesca Fruttarolo
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Publication number: 20130074927Abstract: The invention provides highly fluorescent materials comprising a single (n=0) or a series (n=1, 2, etc.) of benzo heterocyclic systems. The photo-stable highly luminescent chromophores are useful in various applications, including in wavelength conversion films. Wavelength conversion films have the potential to significantly enhance the solar harvesting efficiency of photovoltaic or solar cell devices.Type: ApplicationFiled: September 25, 2012Publication date: March 28, 2013Applicant: NITTO DENKO CORPORATIONInventor: NITTO DENKO CORPORATION
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Patent number: 8399681Abstract: 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: GrantFiled: August 3, 2012Date of Patent: March 19, 2013Assignee: Janssen Pharmaceutica NVInventors: Gilles Bignan, Micheal Gaul, Guozhang Xu, Bao-Ping Zhao
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Patent number: 8399683Abstract: The present invention describes compounds, processes for their preparation, pharmaceutical compositions containing them, and their use in therapy.Type: GrantFiled: September 16, 2009Date of Patent: March 19, 2013Assignee: TetraLogic PharmaceuticalsInventors: Stephen M. Condon, Matthew G. Laporte
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Publication number: 20130059852Abstract: Some embodiments of this invention include methods for treating disease and methods for administering a compound of Formula (I). In some aspects of the invention, diseases can be treated by administration of compositions comprising a compound of Formula (I). Pharmaceutical compositions of some embodiments of the present invention comprise a compound of Formula (I).Type: ApplicationFiled: April 8, 2011Publication date: March 7, 2013Applicant: UNIVERSITY OF LOUISVILLE RESEARCH FOUNDATION, INC.Inventors: John O. Trent, Jason B. Meier, Kelby B. Napier
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Patent number: 8389511Abstract: The present invention relates to a compound of the following formula (I) or a pharmaceutically acceptable salt thereof, being useful as a renin inhibitor. [wherein R1a is halogen, etc.; R1m is H, etc.; G1 is —N(R1b)—, etc.; G2 is —CO—, etc.; G3 is —C(R1c)(R1d)—, etc.; G4 is oxygen, etc.; R1b is optionally substituted C1-6 alkyl, etc.; R1c and R1d are independently the same or different, H, etc.; R3 is H, optionally substituted C1-6 alkyl, etc.; R3a, R3b, R3c and R3d are independently the same or different, and a group: -A-B (said A is single bond, etc., and said B is H, etc.), etc.; and n is 1, etc.Type: GrantFiled: December 19, 2008Date of Patent: March 5, 2013Assignee: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Hiroyuki Nakahira, Yohei Ikuma, Nobuhisa Fukuda, Kozo Yoshida, Hidenori Kimura, Satoshi Suetsugu, Akira Fusano, Kiyoto Sawamura, Junya Ikeda, Yoshio Nakai
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Publication number: 20130053382Abstract: The instant invention provides for compounds that inhibit PDK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting PDK1 activity by administering the compound to a patient in need of treatment of cancer.Type: ApplicationFiled: April 28, 2011Publication date: February 28, 2013Inventors: Sunil Paliwal, Matthew Paul Rainka, Ang Li, May Xiaowu Jiang, Hon-chung Tsui, Ronald J. Doll
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Publication number: 20130045986Abstract: The present invention relates to novel compounds of formula (A) and (B) as modulators of GPR-119, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of GPR-119 mediated diseases or disorders with them.Type: ApplicationFiled: June 8, 2012Publication date: February 21, 2013Applicant: Rhizen Pharmaceuticals SAInventors: Dhanapalan NAGARATHNAM, Swaroop Kumar V.S. Vakkalanka, Srikant Viswanadha, Gayatri S. Merikapudi
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Patent number: 8378096Abstract: This invention is directed to a hexahydro-cycloheptapyrazole cannabinoid modulator compound of formula (I): and a method for use in treating, ameliorating or preventing a cannabinoid receptor mediated syndrome, disorder or disease.Type: GrantFiled: April 7, 2009Date of Patent: February 19, 2013Assignee: Janssen Pharmaceutica N.V.Inventors: Fina Liotta, Mingde Xia, Huajun Lu, Meng Pan, Michael P. Wachter
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Publication number: 20130035342Abstract: The present invention relates to a compound of formula (I): Wherein R1 is a substituted or unsubstituted aromatic hetero- or homocyclic or a substituted or unsubstituted alicyclic hetero- or homocyclic group; R2 is an alkyl group with 1 to 18 carbon atoms or a substituted or unsubstituted cycloalkyl or aryl group; R3 is a substituted or unsubstituted aromatic hetero- or homocyclic or a substituted or unsubstituted alicyclic hetero- or homocyclic group; L is a single bond, an alkyl group having 1 to 6 carbon atoms, NHCO, O, S, NHCONH or NHCOO; X, Y and Z are independently 0, N, NH, S or CH; W is a single bond or an alkyl group having from 1 to 6 carbon atoms; or a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate of said compound or salt.Type: ApplicationFiled: December 16, 2010Publication date: February 7, 2013Applicant: NEUROPORE THERAPIES, INC.Inventors: Eliezer Masliah, Edward M. Rockenstein, Wolfgang Wrasidlo, Igor Flint Tsigelny
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Patent number: 8367704Abstract: 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: GrantFiled: February 12, 2009Date of Patent: February 5, 2013Assignee: Yuhan CorporationInventors: Chun-Ho Lee, Ja-Heouk Khoo, Kyoung-Chan Kwon, Hyun Ju
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Publication number: 20130029964Abstract: An object of the present invention is to provide a novel low molecular weight compound exhibiting an osteogenesis-promoting action. This object is achieved by a compound having the general formula (I) or a pharmacologically acceptable salt thereof. In the general formula (I), R1 and R2 represent hydrogen atoms, and the like; R3 represents a hydrogen atom, and the like; X, Y, and Z represent nitrogen atoms, and the like; A represents a phenylene group, and the like; n represents 1 or 2, and the like; and V and W represent oxygen atoms, and the like.Type: ApplicationFiled: August 27, 2012Publication date: January 31, 2013Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Kazumasa Aoki, Satoshi Matsui, Kenji Yoshikawa, Hiroki Shimizu, Junko Sasaki, Katsuyoshi Nakajima, Osamu Kanno, Kiyoshi Oizumi
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Publication number: 20130029995Abstract: Substituted bicyclic aromatic carboxamide and urea compounds as vanilloid receptor ligands, pharmaceutical compositions containing these compounds, and a method of using these compounds in the treatment and/or inhibition of pain and further diseases and/or disorders mediated at least in part via the vanilloid receptor 1 (VR1/TRPV1).Type: ApplicationFiled: July 25, 2012Publication date: January 31, 2013Applicant: Gruenenthal GmbHInventors: Robert FRANK, Thomas CHRISTOPH, Bernhard LESCH, Jeewoo LEE
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Patent number: 8357690Abstract: Provided herein are methods of treating a proliferative disease in a subject, comprising administering to the subject a therapeutically effective amount of AC220 and a nucleoside analog, a topoisomerase inhibitor or an anthracycline, or a combination thereof.Type: GrantFiled: March 23, 2010Date of Patent: January 22, 2013Assignee: Ambit Biosciences CorporationInventors: Robert C. Armstrong, Barbara A. Belli
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Publication number: 20130017149Abstract: Condensed tricyclic compounds having a condensed structure containing one phenyl and one pyrazole ring linked with each other by a central ring comprising from five to eight atoms, having affinity for the CB1 and/or CB2 receptors, with central nervous system and/or peripheral activity, of formula (I): wherein the various substituents are as defined in the description. The compounds show affinity for the CB1 and/or CB2 cannabinoidergic receptors.Type: ApplicationFiled: September 14, 2012Publication date: January 17, 2013Applicant: NEUROSCIENZE PHARMANESS S.C. A.R.L.Inventors: Paolo LAZZARI, Giovanni Loriga, Ilaria Manca, Gerard Aime Pinna, Luca Pani
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Patent number: 8354399Abstract: 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: GrantFiled: December 15, 2009Date of Patent: January 15, 2013Assignee: 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: 20130012543Abstract: 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: September 13, 2012Publication date: January 10, 2013Inventors: 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: 20130012507Abstract: Compounds represented by formula (Ia) or (Ib) and wherein R and R1 are as defined in the description, and pharmaceutically acceptable salts thereof, are disclosed; the said compounds are useful in the treatment of cell cycle proliferative disorders, e.g. cancer, associated with an altered cell cycle dependent kinase activity.Type: ApplicationFiled: September 13, 2012Publication date: January 10, 2013Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Maria Gabriella Brasca, Raffaella Amici, Daniele Fancelli, Marcella Nesi, Paolo Orsini, Fabrizio Orzi, Patrick Roussel, Anna Vulpetti, Paolo Pevarello
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Patent number: 8344148Abstract: The present invention provides a novel intermediate for manufacturing a 2,3-dihydroimidazo[2,1-b]oxazole compound with a high yield and a high purity, and a manufacturing method of the intermediate. The present invention provides an epoxy compound represented by the general formula (2): wherein, R1 represents hydrogen or a lower alkyl group; and R2 represents a piperidyl group represented by the general formula (A1): (wherein, R3 represents a phenoxy group having a halogen-substituted lower alkoxy group substituted on a phenyl group, and the like) and the like; and n represents an integer of 1 to 6, a manufacturing method of the epoxy compound, and a manufacturing method of an oxazole compound using the epoxy compound.Type: GrantFiled: May 7, 2008Date of Patent: January 1, 2013Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Hidetsugu Tsubouchi, Yoshikazu Haraguchi, Satoshi Hayakawa, Naoto Utsumi, Shinichi Taira, Yoshihisa Tanada, Nobuhisa Fujita, Koichi Shinhama, Kimiyoshi Annaka, Takuya Furuta
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Publication number: 20120322826Abstract: This invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof with 5-HT4 agonistic activities, which is useful in the treatment of dementia. This invention also relates to a pharmaceutical composition for the treatment of dementia which comprises a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof. Further this invention relates to a method for the treatment of dementia in an animal subject including a mammalian subject, which comprises administering to the animal subject including a mammalian subject a compound of the formula (I) or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: February 14, 2011Publication date: December 20, 2012Applicant: RQUALIA PHAMRA INC.Inventors: Hiroyuki Ohshiro, Akiyoshi Fujiuchi, Yukinori Take
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Publication number: 20120316202Abstract: Compounds of the general formula And their use in the treatment of psychotic disorders and cognitive impairment are disclosed.Type: ApplicationFiled: August 14, 2012Publication date: December 13, 2012Inventors: David Gwyn COOPER, Ian Thomson Forbes, Vincenzo Garzya, Jian Jin, Yann Louchart, Graham Walker, Paul Adrian Wyman
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Publication number: 20120316201Abstract: The invention relates to novel benzimidazole and imidazopyridine derivatives having the general Formula (I), which have a good affinity with certain subtypes of melanocortin receptors, particularly MC4 receptors. The derivatives are particularly suitable for the treatment of pathological states and diseases involving one or more melanocortin receptors. The invention also relates to pharmaceutical compositions containing said the compounds having the general Formula (I).Type: ApplicationFiled: June 8, 2012Publication date: December 13, 2012Applicant: IPSEN PHARMA S.A.S.Inventors: Lÿdie POITOUT, Valerie Brault, Carole Sackur, Pierre Roubert, Pascale Plas
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Patent number: 8329705Abstract: The present invention relates to substituted [1,2,4]triazolo-[4,3-a]pyrazine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted [1,2,4]triazolo-[4,3-a]pyrazine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: GrantFiled: December 29, 2010Date of Patent: December 11, 2012Assignee: ArQule, Inc.Inventor: Neil Westlund
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Publication number: 20120309789Abstract: Compounds of general formula and their use in the treatment of psychotic disorders and cognitive impairment, are disclosed.Type: ApplicationFiled: August 14, 2012Publication date: December 6, 2012Inventors: David Gwyn COOPER, Ian Thomas FORBES, Vicenzo GARZYA, Jian JIN, Yann LOUCHART, Graham WALKER, Paul Adrian WYMAN
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Publication number: 20120309736Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.Type: ApplicationFiled: February 21, 2011Publication date: December 6, 2012Inventors: Jinlong Jiang, Andrew J. Kassick, Ahmet Kekec, Iyassu K. Sebhat
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Publication number: 20120309738Abstract: This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), to pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, M, W, R1, R2, R3, R4, R6, R2, R7, R8, R9, Ra, Rb have meanings given in the description.Type: ApplicationFiled: December 8, 2011Publication date: December 6, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Henning Priepke, Raimund Kuelzer, Juergen Mack, Roland Pfau, Dirk Stenkamp, Benjamin Pelcman, Robert Roenn, Dimitrijs Lubriks, Edgars Suna
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Patent number: 8318773Abstract: Provided herein are isoindoline compounds, pharmaceutical compositions comprising one or more of such compounds, and methods of their use for treating, preventing, or managing various diseases.Type: GrantFiled: June 11, 2012Date of Patent: November 27, 2012Assignee: Celgene CorporationInventors: George W. Muller, Alexander L. Ruchelman
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Patent number: 8314253Abstract: 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: GrantFiled: October 21, 2009Date of Patent: November 20, 2012Assignee: Actelion Pharmaceuticals Ltd.Inventors: Kurt Hilpert, Francis Hubler, Dorte Renneberg
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Patent number: 8314097Abstract: The present invention provides a compound of formula I: Said compound is inhibitor of aldosterone synthase and aromatase, and thus can be employed for the treatment of a disorder or disease mediated by aldosterone synthase or aromatase. Accordingly, the compound of formula I can be used in treatment of hypokalemia, hypertension, congestive heart failure, atrial fibrillation, renal failure, in particular, chronic renal failure, restenosis, atherosclerosis, syndrome X, obesity, nephropathy, post-myocardial infarction, coronary heart diseases, inflammation, increased formation of collagen, fibrosis such as cardiac or myocardiac fibrosis and remodeling following hypertension and endothelial dysfunction, gynecomastia, osteoporosis, prostate cancer, endometriosis, uterine fibroids, dysfunctional uterine bleeding, endometrial hyperplasia, polycystic ovarian disease, infertility, fibrocystic breast disease, breast cancer and fibrocystic mastopathy.Type: GrantFiled: August 23, 2006Date of Patent: November 20, 2012Assignee: Novartis AGInventors: Gary Michael Ksander, Erik Meredith, Lauren G. Monovich, Julien Papillon, Fariborz Firooznia, Qi-Ying Hu
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Publication number: 20120283259Abstract: Novel heterocyclic derivatives 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: July 12, 2012Publication date: November 8, 2012Applicant: PROBIODRUG AGInventors: Ulrich Heiser, Ulf-Torsten Gaertner, Hans-Ulrich Demuth
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Publication number: 20120276050Abstract: Clemizole and clemizole analog compounds, and pharmaceutical compositions of the same, are useful in methods of treating a host infected with a virus from the Flaviviridae family of viruses, methods of inhibiting HCV replication in a host, methods of inhibiting the binding of NS4B polypeptide to the 3?UTR of HCV negative strand RNA in a host, and methods of treating liver fibrosis in a host.Type: ApplicationFiled: March 16, 2010Publication date: November 1, 2012Inventors: Ingrid C. Choong, David Cory, Jeffrey S. Glenn, Wenjin Yang
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Publication number: 20120277215Abstract: The present invention provides a compound of formula I: Said compound is inhibitor of aldosterone synthase and aromatase, and thus can be employed for the treatment of a disorder or disease mediated by aldosterone synthase or aromatase. Accordingly, the compound of formula I can be used in treatment of hypokalemia, hypertension, congestive heart failure, atrial fibrillation, renal failure, in particular, chronic renal failure, restenosis, atherosclerosis, syndrome X, obesity, nephropathy, post-myocardial infarction, coronary heart diseases, inflammation, increased formation of collagen, fibrosis such as cardiac or myocardiac fibrosis and remodeling following hypertension and endothelial dysfunction, gynecomastia, osteoporosis, prostate cancer, endometriosis, uterine fibroids, dysfunctional uterine bleeding, endometrial hyperplasia, polycystic ovarian disease, infertility, fibrocystic breast disease, breast cancer and fibrocystic mastopathy.Type: ApplicationFiled: July 2, 2012Publication date: November 1, 2012Inventors: Gary Michael Ksander, Erik Meredith, Lauren G. Monovich, Julien Papillon, Fariborz Firooznia, Qi-Ying Hu
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Publication number: 20120277190Abstract: Compounds of formula (I) wherein A, R1, R2, and R3 are defined in the specification, and which are useful as therapeutic compounds particularly for treating disorders or conditions associated with inflammation, pain, bladder overactivity, urinary incontinence, and other disorders caused by or exacerbated by TRPV1.Type: ApplicationFiled: July 9, 2012Publication date: November 1, 2012Inventors: Arthur R. Gomtsyan, Erol K. Bayburt, John R. Koenig, Kennan C. Marsh, Robert G. Schmidt, JR., Chih-Hung Lee, Weili Wang, Jerome F. Daanen, Brian S. Brown
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Publication number: 20120277248Abstract: Substituted pyrrolo-pyrazole 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 dysregulated protein kinase activity, like cancer.Type: ApplicationFiled: June 13, 2012Publication date: November 1, 2012Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Michele CARUSO, Italo BERIA, Maria Gabriella BRASCA, Ron FERGUSON, Helena POSTERI
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Publication number: 20120277229Abstract: In one aspect, the invention relates to substituted 3-(1H-benzo[d]imidazol-2-yl)-1H-indazole analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the PDK1 kinase; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions for treating disorders associated with dysfunction of the PDK1 kinase. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: March 31, 2012Publication date: November 1, 2012Inventors: David J. Bearss, Hariprasad Vankayalapati, Venkataswamy Sorna, Steven L. Warner, Sunil Sharma
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Patent number: 8299096Abstract: This invention is directed to methods of preventing or treating diseases or conditions of the lungs associated with excessive cell proliferation, remodeling, inflammation, vasoconstriction, bronchoconstriction, airway hyperreactivity and edema.Type: GrantFiled: June 26, 2009Date of Patent: October 30, 2012Assignee: Inspire Pharmaceuticals, Inc.Inventors: Tomas Navratil, Ward M. Peterson, John W. Lampe, Emilee H. Fulcher, Scott D. Sorensen
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Patent number: 8299243Abstract: 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: GrantFiled: September 29, 2011Date of Patent: October 30, 2012Assignee: AbbVie Inc.Inventors: Yujia Dai, Steven K. Davidsen, Anna M. Ericsson, Kresna Hartandi, Zhiqin Ji, Michael R. Michaelides
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Patent number: 8299070Abstract: 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: GrantFiled: November 24, 2010Date of Patent: October 30, 2012Assignee: Japan Tobacco Inc.Inventors: Teruhiko Inoue, Tetsudo Kaya, Shinichi Kikuchi, Koji Matsumura, Ritsuki Masuo, Motoya Suzuki, Michihide Maekawa
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Patent number: 8293738Abstract: 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: GrantFiled: May 12, 2011Date of Patent: October 23, 2012Assignee: Abbott LaboratoriesInventors: Michael R. Michaelides, James H. Holms, Douglas H. Steinman
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Publication number: 20120264737Abstract: Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by disregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders.Type: ApplicationFiled: March 8, 2012Publication date: October 18, 2012Applicant: 3-V BIOSCIENCES, INC.Inventors: Johan D. Oslob, Robert S. McDowell, Russell Johnson, Hanbiao Yang, Marc Evanchik, Cristiana A. Zaharia, Haiying Cai, Lily W. Hu
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Publication number: 20120264733Abstract: Compounds represented by the formulas wherein each symbol is as defined in the specification, and a prodrug thereof have a superior renin inhibitory activity, and are useful as agents for the prophylaxis or treatment of hypertension, various organ damages attributable to hypertension and the like.Type: ApplicationFiled: April 13, 2012Publication date: October 18, 2012Inventors: Takanobu KUROITA, Yasuhiro Imaeda, Kouichi Iwanaga, Naohiro Taya, Hidekazu Tokuhara, Yoshiyuki Fukase
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Patent number: 8288412Abstract: Compounds of formula (I) and salts are provided: wherein R5 is selected from halogen, C1-6alkyl, C1-6alkyl substituted with one or more fluorine atoms, C1-6 alkoxy, C1-6 alkoxy substituted with one or more fluorine atoms, and cyano; R6 is selected from halogen, C1-6alkyl, C1-6alkyl substituted with one or more fluorine atoms, C3-6cycloalkyl, C3-6cycloalkyl substituted with one or more fluorine atoms, C1-6 alkoxy, C1-6 alkoxy substituted with one or more fluorine atoms, and cyano; and Q is hydrogen or C1-6alkyl. The compounds are M1 agonists and are useful for therapy, for example in the treatment of psychotic disorders and cognitive impairment.Type: GrantFiled: September 27, 2006Date of Patent: October 16, 2012Assignee: Glaxo Group LimitedInventors: Brian Budzik, David Gwyn Cooper, Ian Thomson Forbes, Vincenzo Garzya, Jian Jin, Dongchuan Shi, Paul William Smith, Graham Walker
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Patent number: 8288413Abstract: Compounds of formula (I) and salts are provided: wherein R6 is selected from hydrogen, halogen, C1-6alkyl, C1-6alkyl substituted with one or more fluorine atoms, C3-6cycloalkyl, C3-6cycloalkyl substituted with one or more fluorine atoms, C1-6 alkoxy, C1-6 alkoxy substituted with one or more fluorine atoms, and cyano, and Q is hydrogen or C1-6alkyl. The compounds are M1 agonists and are useful for therapy, for example in the treatment of psychotic disorders and cognitive impairment.Type: GrantFiled: September 27, 2006Date of Patent: October 16, 2012Assignee: Glaxo Group LimitedInventors: Brian Budzik, David Gwyn Cooper, Ian Thomson Forbes, Jian Jin, Dongchuan Shi, Paul William Smith, Graham Walker