Having -c(=x)-, Wherein X Is Chalcogen, Attached Directly Or Indirectly To The Isoquinoline Ring System By Nonionic Bonding Patents (Class 546/146)
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Patent number: 7939666Abstract: Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers.Type: GrantFiled: May 4, 2006Date of Patent: May 10, 2011Assignee: Chroma Therapeutics Ltd.Inventors: Alan Hornsby Davidson, Sanjay Ratilal Patel, Francesca Ann Mazzei, Stephen John Davies, Alan Hastings Drummond, David Festus Moffat, Kenneth William John Baker, Alistair David Graham Donald
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Publication number: 20110105555Abstract: The invention relates to compounds having pharmacological activity towards the 5-HT6 receptor, and more particularly to some N-imidazo[2,1-b]thiazole-5-sulfonamide derivatives, 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 5-HT6 is involved.Type: ApplicationFiled: May 8, 2009Publication date: May 5, 2011Inventors: Josep Mas Prio, Antoni Torrens Jover
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Publication number: 20110105485Abstract: There is provided a series of novel ?-(N-sulfonamido)acetamide compounds of the Formula (I) wherein R, R1, R2 and R3 are defined herein, which are inhibitors of ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by anti-amyloid activity.Type: ApplicationFiled: July 21, 2010Publication date: May 5, 2011Inventors: Michael F. Parker, Katharine E. McElhone, Robert A. Mate, Joanne J. Bronson, Yonghua Gai, Carl P. Bergstrom, Lawrence R. Marcin, John E. Macor
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Publication number: 20110092481Abstract: The present invention is related to novel compounds of formula (I) having P2X7 antagonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment or prophylaxis of diseases associated with P2X7 receptor activity in animals, in particular humans.Type: ApplicationFiled: April 21, 2009Publication date: April 21, 2011Inventors: Christopher John Love, Joseph Elisabeth Leenaerts, Ludwig Paul Cooymans, Donald Alec Labsack, Bryan James Branstetter, Jason Christopher Rech, Elizabeth Ann Gleason, Jennifer Diane Venable, Danielle Wiener, Deborah Margaret Smith, James Guy Breitenbucher
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Publication number: 20110092707Abstract: Novel crystalline polymorphic forms, Forms A, B, C, D, and E of a compound of Formula I, which has been found to be a potent inhibitor of LFA-1, are disclosed. Methods of preparation and uses thereof in the treatment of LFA-1 mediated diseases are also disclosed in this invention.Type: ApplicationFiled: October 21, 2010Publication date: April 21, 2011Applicant: SARcode CorporationInventor: John Burnier
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Publication number: 20110071299Abstract: The present invention provides an efficient process for the preparation of hexahydroisoquinolines from amides. In particular, the invention provides a good yielding, one-pot process for the synthesis of hexahydroisoquinolines.Type: ApplicationFiled: September 24, 2010Publication date: March 24, 2011Applicant: Mallinckrodt Inc.Inventors: Christopher W. Grote, Frank W. Moser, Peter X. Wang, Gary L. Cantrell, David W. Berberich
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Publication number: 20110053940Abstract: The present invention relates to 3,4-substituted piperidinyl-based renin inhibitor compounds bearing at 4-position oxopyridine and having the formula (I). The invention further relates to pharmaceutical compositions containing said compounds, as well as their use in treating cardiovascular events and renal insufficiency.Type: ApplicationFiled: May 4, 2009Publication date: March 3, 2011Inventors: Austin Chih-Yu Chen, Daniel Dube, Pierre-Andre Fournier, Erich L. Grimm, Patrick Lacombe, Sebastien Laliberte, Dwight MacDonald, D. Bruce MacKay, Daniel James McKay, Tom Yao-Hsiang Wu, Louis-Charles Campeau, Jeremy Peter Scott, Nadine Bremeyer
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Patent number: 7897618Abstract: Disclosed are N-aroyl cyclic amine derivatives having the formula: where the variables are as define herein, and their use as pharmaceuticals, specifically as orexin receptor antagonists.Type: GrantFiled: October 29, 2007Date of Patent: March 1, 2011Assignee: SmithKline Beecham LimitedInventors: Clive Leslie Branch, Wai Ngor Chan, Amanda Johns, Christopher Norbert Johnson, David John Nash, Riccardo Novelli, Jean-Pierre Pilleux, Roderick Alan Porter, Rachel Elizabeth Anne Stead, Geoffrey Stemp
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Patent number: 7893267Abstract: The present invention is directed to benzazole compounds that inhibit ?-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment or prevention of diseases in which BACE is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which BACE is involved.Type: GrantFiled: March 14, 2006Date of Patent: February 22, 2011Assignee: High Point Pharmaceuticals, LLCInventors: Adnan M. M. Mjalli, David Jones, Devi Reddy Gohimmukkula, Guoxiang Huang, Jeff Zhu, Mohan Rao, Robert C. Andrews, Tan Ren
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Publication number: 20110038835Abstract: Compounds useful as Rho kinase inhibitors of formula (I): wherein variable are as defined herein are provided. Methods of treatment of malconditions mediated by Rho kinase, and methods of preparation of the compounds, are also provided.Type: ApplicationFiled: December 18, 2008Publication date: February 17, 2011Applicant: The Scripps Research InstituteInventors: Yangbo Feng, Philip LoGrasso, Thomas Bannister, Thomas Schroeter, Xingang Fang, Yen ting Chen, Yan Yin, Michael P. Smolinski, Lei Yao, Bo Wang, Hampton Sessions
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Publication number: 20110039827Abstract: This invention provides compounds of formula (I): wherein R1, R2, G, m, n, p and q have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: ApplicationFiled: June 21, 2010Publication date: February 17, 2011Applicant: Millennium Pharmaceuticals, Inc.Inventors: Christopher Blackburn, Jeffrey P. Ciavarri, Kenneth M. Gigstad, He Xu
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Publication number: 20110039857Abstract: The invention relates to piperidine and pyrrolidine compounds of formula (I) wherein A, B, n and X are as described in the description; to pharmaceutically acceptable salts thereof, and to the use of such compounds use as medicaments, especially as orexin receptor antagonists.Type: ApplicationFiled: April 29, 2009Publication date: February 17, 2011Inventors: Hamed Aissaoui, Christoph Boss, Ralf Koberstein, Thierry Sifferlen, Daniel Trachsel
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Patent number: 7879848Abstract: Novel compounds exhibiting good inhibitory activity versus Dipeptidyl Peptidase-IV(DPP-IV) include those of the following formula (1) or pharmaceutically acceptable salt thereof: wherein A is a substituted or unsubstituted 1,4,5,7-tetrahydro-pyrazolo[3,4-c]pyridine, 5,6 -dihydro-8H-[1,2,4]triazolo[4,3-a]pyrazine, 4,5-dihydro-7H-isooxazolo[3,4-c]pyridine, 3,4 -dihydroisoquinoline, 5,8-dihydropyrido[3,4-d]pyrimidine, or 6,7 -dihydro[1,3]thiazolo[4,5,c]pyridine, and B is a substituted or unsubstituted piperidin-2-one, morpholin-3-one, oxazolidin-2-one, pyrrolidin-2-one, or 1,5-dihydro-pyrrol-2-one. Methods of preparing the novel inhibitory compounds of formula (1) and pharmaceutical compositions containing the same as an active agent are disclosed.Type: GrantFiled: March 30, 2006Date of Patent: February 1, 2011Assignee: LG Life Sciences, Ltd.Inventors: Chang-Seok Lee, Jong Sung Koh, Ki Dong Koo, Geun Tae Kim, Kyoung-Hee Kim, Sang Yong Hong, Sungsub Kim, Min-Jung Kim, Hyeon Joo Yim, Dongchul Lim, Hye Jin Kim, Hee Oon Han, Seong Cheol Bu, Oh Hwan Kwon, Sung Ho Kim, Gwong-Cheung Hur, Ji Young Kim, Zi-Ho Yeom, Dong-Jun Yeo
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Publication number: 20110021528Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.Type: ApplicationFiled: October 1, 2010Publication date: January 27, 2011Applicant: PHARMACYCLICS, INC.Inventors: Erik J. Verner, Martin Sendzik, Chitra Baskaran, Joseph J. Buggy, James Robinson
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Patent number: 7875631Abstract: Compounds of the formula (I): where R2, R5, R6 have the meanings as given in the description, and U, V and W, respectively, may be CR2?, CR4? and CR6?, respectively (with the definitions of R2?, R4? and R6? again as in the description), or may be N, were synthesized. They were found to down-regulate or inhibit the expression or function of the IGF-1 receptor.Type: GrantFiled: March 12, 2004Date of Patent: January 25, 2011Assignee: Analytecon S.A.Inventors: Jan Gunzinger, Kurt Leander
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Publication number: 20110003795Abstract: The invention relates to substituted aromatic carboxamide and urea derivatives, to processes for the preparation thereof, to pharmaceutical compositions containing these compounds and also to the use of these compounds for preparing pharmaceutical compositions.Type: ApplicationFiled: May 6, 2010Publication date: January 6, 2011Applicant: Gruenenthal GmbHInventors: Robert FRANK, Gregor BAHRENBERG, Thomas CHRISTOPH, Klaus SCHIENE, Jean DE VRY, Nils DAMANN, Sven FRORMANN, Bernhard LESCH, Jeewoo LEE, Yong-Soo KIM, Myeong-Seop KIM
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Patent number: 7863292Abstract: The present invention relates to compounds suitable for use in mediating hypoxia inducible factor and for treating erythropoietin-associated conditions by increasing endogenous erythropoietin in vitro and in vivo.Type: GrantFiled: January 19, 2007Date of Patent: January 4, 2011Assignee: FibroGen, Inc.Inventors: Michael P. Arend, Lee A. Flippin, Volkmar Guenzler-Pukall, Wen-Bin Ho, Eric Turtle, Xiaohui Du
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Publication number: 20100331312Abstract: Amide derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the histamine H3 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of histamine H3-associated disorders, such as cognitive disorders, epilepsy, brain trauma, depression, obesity, disorders of sleep and wakefulness such as excessive daytime sleepiness, narcolepsy, shift-work sleep disorder, drowsiness as a side effect from a medication, maintenance of vigilance to aid in the completion of tasks and the like, cataplexy, hypersomnia, somnolence syndrome, jet lag, sleep apnea and the like, attention deficit hyperactivity disorder (ADHD), schizophrenia, allergies, allergic responses in the upper airway, allergic rhinitis, nasal congestion, dementia, Alzheimer's disease, pain and the like.Type: ApplicationFiled: February 18, 2009Publication date: December 30, 2010Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Vincent J. Santora, Brian J. Hofilena, Michelle Pulley, Graeme Semple, Yun Shan, Brian M. Smith
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Publication number: 20100331335Abstract: The present disclosure provides inhibitors of c-Jun N-terminal kinases (JNK) having a structure according to the following formula: or a salt or solvate thereof, wherein ring A, Ca, Cb, Z, R5, W and Cy are defined herein. The disclosure further provides pharmaceutical compositions including the compounds of the present disclosure and methods of making and using the compounds and compositions of the present disclosure, e.g., in the treatment and prevention of various disorders, such as Alzheimer's disease.Type: ApplicationFiled: February 5, 2010Publication date: December 30, 2010Inventors: Hing L. Sham, Roy K. Hom, Andrei W. Konradi, Gary D. Probst, Simeon Bowers, Anh Truong, R. Jeffrey Neitz, Jennifer Sealy, Gergely Toth
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Publication number: 20100324025Abstract: Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.Type: ApplicationFiled: September 21, 2009Publication date: December 23, 2010Applicant: University of WashingtonInventors: Niels H. Andersen, Jason Bowman, Alice L. Erwin, Eric A. Harwood, Toni Kline, Khisimuzi E. Mdluli, Simon Ng, Keith B. Pfister, Ribhi Shawar, Allan S. Wagman, Asha Yabannavar
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Publication number: 20100324046Abstract: The present invention relates to a novel class of 4-carboxybenzylamino derivatives. The 4-carboxybenzylamino compounds can be used to treat cancer. The 4-carboxybenzylamino compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: ApplicationFiled: June 24, 2008Publication date: December 23, 2010Inventors: Paul Harrington, Richard W. Heidebrecht, JR., Solomon Kattar, Thomas A. Miller, Karin M. Otte, Phieng Siliphaivanh, Paul Tempest, Kevin J. Wilson, David J. Witter
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Patent number: 7834012Abstract: The present invention relates to compounds, which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II, as well as hyperglycemia, metabolic syndrome, hyperinsulinemia, obesity, atherosclerosis, various immunomodulatory diseases, and other diseases.Type: GrantFiled: August 25, 2006Date of Patent: November 16, 2010Assignee: Abbott LaboratoriesInventors: Zhonghua Pei, Thomas von Geldern, David J. Madar, Xiaofeng Li, Fatima Basha, Hong Yong, Kenton L. Longenecker, Bradley J. Backes, Andrew S. Judd, Mathew M. Mulhern, Kent D. Stewart
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Publication number: 20100286125Abstract: Compounds having the formula wherein the symbols have the meaning described in the specification are hydroxamic acid derivatives of 4-phenyl-4-hydroxy-butyric acid and capable of inhibiting the lethal effects of infection by anthrax bacteria and are useful in the treatment of poisoning by anthrax.Type: ApplicationFiled: March 28, 2008Publication date: November 11, 2010Inventors: Alan T. Johnson, Seongjin Kim
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Publication number: 20100280024Abstract: The present invention relates to renin inhibitors of formula (I), their pharmaceutically acceptable salts and pharmaceutical compositions containing them. The present invention also relates to a process of preparing compounds of general formula (I), their tautomeric forms, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and novel intermediates involved in their synthesis.Type: ApplicationFiled: October 13, 2008Publication date: November 4, 2010Inventors: Jigar Desai, Pravin S. Thombare, Mukul R. Jain, Pankaj Ramanbhai Patel
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Publication number: 20100280066Abstract: This invention is directed to acylated amino acid amidyl pyrazoles and related compounds of Formula I. The invention is also directed to a pharmaceutical formation comprising such compound or in a pharmaceutically acceptable salt form thereof. The invention is further directed to a method for inhibiting ?-amyloid peptide release and/or synthesis, a method for inhibiting ?-secretase activity, and a method for treating neurological disorders associated with ?-amyloid peptide production. The method comprises administering to a host a pharmaceutical formulation comprising an effective amount of a compound of Formula I. The compounds of Formula I are useful in the prevention and treatment of Alzheimer's disease.Type: ApplicationFiled: July 9, 2010Publication date: November 4, 2010Inventors: Jay S. Tung, Lee H. Latimer, Jing Wu, Albert Garofalo, Michael A. Pleiss, Darren Dressen, Ashley Guinn, Scott A. Jenkins, Jennifer Sealy, John Tucker, David W.G. Wone
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Publication number: 20100280067Abstract: The present invention relates to compounds that act as acetyl-CoA carboxylase (ACC) inhibitors. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.Type: ApplicationFiled: April 30, 2010Publication date: November 4, 2010Inventors: Pakala Kumara Savithru SARMA, Vinod Parameshwaran Acharya, Srinivas Rao Kasibhatla, Vellarkad Narayana Viswanadhan, Polisetti Shekhar, Alexander Bischoff
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Publication number: 20100280018Abstract: A compound of formula (I), or an enantiomer or diastereoisomer thereof, or a salt, hydrate or solvate thereof: for the treatment or prophylaxis of arthritis in mammals.Type: ApplicationFiled: July 20, 2010Publication date: November 4, 2010Applicants: Laboratoires Serono S.A., Vernalis (Oxford) LimitedInventors: Gilles Pain, Stephen John Davies, Agnes Bombrun
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Publication number: 20100280005Abstract: Disclosed are compounds of Formula I, wherein the R, R1, R2, R3, X, Y, A, Q, E, and G are defined herein. These compounds bind to aspartic proteases to inhibit their activity and are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also disclosed are methods of use of the compounds of Formula I for ameliorating or treating aspartic protease related disorders in a subject in need thereof.Type: ApplicationFiled: April 4, 2008Publication date: November 4, 2010Inventors: Jonh J. Baldwin, Salvacion Cacatian, David Claremon, Lawrence W. Dillard, Patrick T. Flaherty, Bahman Ghavimi-Alagha, John Gleason, Alexey V. Ishchenko, Brian Lawhorn, Gerard McGeehan, Jaclyn R. Patterson, Simon F. Semus, Robert D. Simpson, Suresh B. Singh, Colin Tice, Tritin Tran, Zhenrong Xu, Jing Yuan, Wei Zhao
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Publication number: 20100273772Abstract: Disclosed are compounds of Formula I: pharmaceutical compositions containing compounds of Formula I, and the use of compounds of Formula I to treat diseases and disorders including schizophrenia, paranoia, depression, manic-depressive illness and anxiety wherein W1-W5, X1-X4, Y, Z1-Z5, m, n, p, and R1-R6 in Formula I are defined in the specification.Type: ApplicationFiled: April 22, 2010Publication date: October 28, 2010Applicant: Wyeth LLCInventors: Steven Victor O'Neil, Benjamin Miller Zegarelli, Dane Mark Springer, David Zenan Li
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Patent number: 7820663Abstract: The present invention is related substituted enaminones represented by a compound of Formula I that are novel allosteric modulators of ?7 nAChRs. The invention also discloses the treatment of disorders that are responsive to enhancement of acetylcholine action on ?7 nAChRs in a mammal by administering an effective amount of a compound of Formula I.Type: GrantFiled: June 15, 2006Date of Patent: October 26, 2010Assignee: The Regents of the University of CaliforniaInventors: Derk J. Hogenkamp, Timothy B. C. Johnstone, Kelvin W. Gee
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Patent number: 7820692Abstract: A kind of tetrahydro isoquinoline derivatives (I), their preparation methods, medicine compositions and medicinal uses thereof, especially their uses as ?-opioid receptor excitant in pain relieving, which belongs to the medicine chemistry. The substituents R1, R2, R3, R4 of general formula (I) are defined as the description.Type: GrantFiled: July 10, 2007Date of Patent: October 26, 2010Assignees: China Pharmaceutical University, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Yangtze River Pharmaceutical Group Co., Ltd.Inventors: Yungen Xu, Jinggen Liu, Ting Guo, Dechuan Wang, Tianjiang Sun, Hongguo Lu
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Publication number: 20100267697Abstract: The present teachings provide compounds of Formula (I) and pharmaceutically acceptable salts, hydrates, and esters thereof, wherein Ar, R1, R2, R3, p, and X are defined herein. The present teachings also provide processes for producing said compounds and their pharmaceutically acceptable salts, hydrates and esters, and methods of treating a pathological condition or disorder, or alleviating a symptom thereof, using said compounds including their pharmaceutically acceptable salts, hydrates and esters. The compounds can be useful in modulating ion channel activity including treating a variety of conditions associated with the abnormal modulation of one or more voltage-gated calcium channels.Type: ApplicationFiled: December 11, 2007Publication date: October 21, 2010Applicant: WyethInventors: Vincent P. Galullo, Robert Zelle, Danielle Soenen, Christopher Todd Baker, Paul Will, Hormoz Mazdiyasni, Jinsong Guo, Andrew Fensome, Jeffrey Curtis Kern, William Jay Moore, Edward George Melenski, Justin Kaplan
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Publication number: 20100267696Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-thiophene compounds that, inter alia, inhibit 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11?-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11?-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.Type: ApplicationFiled: December 11, 2008Publication date: October 21, 2010Applicant: THE UNIVERSITY OF EDINBURGHInventors: Scott Peter Webster, Jonathan Robert Seckl, Brian Robert Walker, Peter Ward, Thomas David Pallin, Hazel Joan Dyke, Trevor Robert Perrior
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Publication number: 20100261705Abstract: The present invention provides a carbostyril compound represented by General Formula (1) or a salt thereof, wherein A is a direct bond, a lower alkylene group, or a lower alkylidene group; X is an oxygen atom or a sulfur atom; R4 and R5 each represent a hydrogen atom; the bond between the 3 and 4 positions of the carbostyril skeleton is a single bond or a double bond; R1 is a hydrogen atom, etc; R2 is a hydrogen atom, etc; and R3 is a hydrogen atom, etc. The carbostyril compound or salt thereof of the present invention induces the production of TFF, and thus is usable for the treatment and/or prevention of disorders such as alimentary tract diseases, oral diseases, upper respiratory tract diseases, respiratory tract diseases, eye diseases, cancers, and wounds.Type: ApplicationFiled: November 3, 2009Publication date: October 14, 2010Inventors: Takeshi Kuroda, Takahito Yamauchi, Tomoichi Shinohara, Kunio Oshima, Chiharu Kitajima, Hitoshi Nagao, Tae Fukushima, Takahiro Tomoyasu, Hironobu Ishiyama, Ohta Kazuhide, Masaaki Takano, Takumi Sumida
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Publication number: 20100261687Abstract: Object of the present invention are novel substituted compounds of the formula 1, wherein A, R1, R2, R3 and R4 are defined as in the description. Another object of the present invention is to provide antagonists of CCR3, more particularly to provide pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of at least one of the compounds of the present invention or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: March 19, 2010Publication date: October 14, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Marc GRUNDL, Horst DOLLINGER, Riccardo GIOVANNINI, Christoph HOENKE, Matthias HOFFMANN, Jan KRIEGL, Domnic MARTYRES, Georg RAST, Peter SEITHER
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Publication number: 20100261725Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: August 26, 2009Publication date: October 14, 2010Applicant: CALCIMEDICA, INC.Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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Publication number: 20100256182Abstract: The invention relates to novel 1,2,3,4-tetrahydroisoquinoline derivatives of formula (I) wherein R1, R2, R3 and X are as defined in the claims, and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and methods of treatment comprising administration of said compounds to a mammal.Type: ApplicationFiled: June 15, 2010Publication date: October 7, 2010Inventors: Hamed Aissaoui, Martine Clozel, Walter Fischli, Ralf Koberstein, Thomas Weller
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Publication number: 20100256113Abstract: As a result of extensive studies on NAD(P)H oxidase inhibitors, the present inventors found that a quinolone derivative having, at the 2-position, an alkyl group substituted with a heteroatom or the like has an excellent NAD(P)H oxidase inhibitory activity, and accomplished the present invention. The compound of the present invention has a reactive oxygen species production inhibitory activity based on the NAD(P)H oxidase inhibitory activity, and therefore can be used as an agent for preventing and/or treating diabetes, impaired glucose tolerance, hyperlipidemia, fatty liver, diabetic complications and the like.Type: ApplicationFiled: September 25, 2008Publication date: October 7, 2010Applicant: Astellas Pharma Inc.Inventors: Kenichi Onda, Kenichiro Imamura, Fumie Sato, Hiroyuki Moritomo, Yasuharu Urano, Yuki Sawada, Naoki Ishibashi, Keita Nakanishi, Kazuhiro Yokoyama, Shigetada Furukawa, Kazuhiro Momose
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Publication number: 20100256144Abstract: The present invention relates to the crystal structure of the serine protease kallikrein 7 and to the use of this crystal structure in drug discovery. The present invention also relates to compounds binding specifically to this active site of kallikrein 7.Type: ApplicationFiled: June 26, 2008Publication date: October 7, 2010Inventors: Stefanie Flohr, Stefan Andreas Randl, Nils Ostermann, Ulrich Hassiepen, Frederic Berst, Ursula Bodendorf, Bernd Gerhartz, Adreas Marzinzik, Claus Ehrhardt, Josef Gottfried Meingassner
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Publication number: 20100256101Abstract: The invention relates to novel compounds having the general formula (I), and which compounds are useful to manufacture a medicament to treat a disorder or disease characterized by bronchoconstriction, e.g. COPD and asthma, and vasoconstriction, e.g. hypertension.Type: ApplicationFiled: July 10, 2008Publication date: October 7, 2010Inventors: Maria Dalence, Martin Johansson, Viveca Thornqvist Oltner, Jörgen Toftered, David Wensbo
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Patent number: 7807672Abstract: Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substituents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.Type: GrantFiled: February 13, 2007Date of Patent: October 5, 2010Assignee: Schering CorporationInventors: Yongqi Deng, Gerald W. Shipps, Jr., Alan Cooper, Yang Nan, Tong Wang, M. Arshad Siddiqui, Hugh Zhu, Robert Sun, Joseph M. Kelly, Ronald Doll, Jagdish Desai, James J-S Wang, Youhao Dong, Vincent Madison, Li Xiao, Alan Hruza, Neng-Yang Shih
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Patent number: 7803799Abstract: This invention relates to selenophene compounds of formula (I) shown below. Each variable in formula (I) is defined in the specification. These compounds can be used to treat cannabinoid-receptor mediated disorders.Type: GrantFiled: July 3, 2007Date of Patent: September 28, 2010Assignee: National Health Research InstitutesInventors: Kak-Shan Shia, Jing-Po Tsao, Chia-Liang Tai, Wan-Ping Hsieh, Ming-Shiu Hung, Jen-Shin Song, Yu-Sheng Chao
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Publication number: 20100234219Abstract: Disclosed are compounds of Formula (1), including all geometric and stereoisomers, N-oxides, and salts thereof, Formula (1): wherein A1, A2, A3, A4, A5 and A6 are independently, selected from the group consisting of CR3 and N; provided that at most 3 of A1, A2, A3; A4, A5 and A6 is N; B1, B2 and B3 are independently selected from the group consisting of CR2. and N; each R3 is independently H, halogen, C1-C6 alkyl, C1-C6 haloalkyl, C3-C6 cycloalkyl, C3-C6 halocycloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 haloalkylthio, C1-C6 alkylsulfinyl, C1-C6 haloalkylsulfinyl, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfo?yl, C1-C6 alkylamino, C2-G6 dialkylamino, —CN or —NO2; and R1, R2, R4, R5, W and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula (1) and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.Type: ApplicationFiled: December 28, 2006Publication date: September 16, 2010Inventors: George Philip Lahm, Wesley Lawrence Shoop, Ming Xu
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Patent number: 7790745Abstract: A compound of formula I wherein X, R1, R2a, R3a, R3b, R4a, R4b, R4c and R5 are defined herein.Type: GrantFiled: October 18, 2006Date of Patent: September 7, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Wu Yang, Yufeng Wang, Ellen K. Kick
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Patent number: 7790742Abstract: The present invention relates to substituted 4-phenyltetrahydroisoquinoline compounds of the structure of formula I and pharmaceutical compositions comprising them wherein the R groups are herein defined. These are excellent inhibitors of the sodium-hydrogen exchanger (NHE), in particular of the sodium-hydrogen exchanger of subtype 3 (NHE3). As such these compounds are useful in the treatment of various disorders of the renal and respiratory systems such as acute or chronic renal failure, pulmonary complications, biliary function disorders, respiratory disorders such as snoring or sleep apneas and cardiovascular/central nervous system disorders such as stroke.Type: GrantFiled: March 1, 2007Date of Patent: September 7, 2010Assignee: Sanofi-Aventis Deutschland GmbHInventors: Hans-Jochen Lang, Uwe Heinelt, Klaus Wirth, Thomas Licher, Armin Hofmeister
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Publication number: 20100222324Abstract: Substituted indole compounds corresponding to the formula I: In which R8, R9a, R9b, R10, R11, R200, R210, A, D, T, q, s and t have defined meanings, processes for the preparation thereof, pharmaceutical compositions containing such compounds and the use of substituted indole compounds for the treatment or inhibition of pain and other conditions which are at least partly mediated by Bradykinin 1 receptors (B1R).Type: ApplicationFiled: February 3, 2010Publication date: September 2, 2010Applicant: Gruenenthal GmbHInventors: Stefan Schunk, Melanie Reich, Michael Engels, Tieno Germann, Ruth Jostock, Sabine Hees
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Publication number: 20100222299Abstract: The present invention involves tetrahydroisoquinoline compounds and their use in the inhibition and/or prevention of tumor growth.Type: ApplicationFiled: March 27, 2008Publication date: September 2, 2010Applicant: Sterix LimitedInventors: Fabrice Jourdan, Meriel Kimberley, Matthew Leese, Barry Victor Lloyd Potter, Atul Purohit, Michael John Reed
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Patent number: 7786137Abstract: Bicyclic derivatives having formula (I) and a composition thereof are useful as ion channel antagonists:Type: GrantFiled: May 8, 2006Date of Patent: August 31, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Aarti S. Kawatkar, Tara M. Whitney, Timothy D. Neubert, Nicole Zimmermann, Andreas Termin, Esther Martinborough
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Publication number: 20100217003Abstract: Provided are 7-hydroxy-6-methoxy-1,2,3,4-tetrahydroisoquinoline derivatives and synthesis methods thereof. The compounds significantly inhibit the production of nitrogen monoxide (NO) and superoxide in an activated microglial cell and expressions of TNF-?, IL-1? inducive NO synthase and cyclooxygenase-2 genes. They also prevent NF-kB shift to a nucleus, decrease reactive oxygen species (ROS), inhibit expression of GTP cyclohydrolase I gene and over-production of tetrahydrobiopterin (BH4), and protect dopaminergic neurons from injury due to activated microglial cells. Consequently, the compounds are effective in treating inflammatory and neurodegenerative diseases.Type: ApplicationFiled: December 10, 2007Publication date: August 26, 2010Inventors: On-You Hwang, Dae-Yoon Chi, Hyo-Jin Son, Jai-Woong Seo
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Publication number: 20100197664Abstract: Disclosed are compounds of the formula I wherein A, Y, R1, R2, R3, R4 and R5 are defined, suitable for treating diseases and symptoms of diseases caused at least to some extent by stimulation of bradykinin-B1 receptors, the preparation thereof and the use thereof.Type: ApplicationFiled: July 23, 2008Publication date: August 5, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Iris Kauffmann-Hefner, Angelo Ceci, Henri Doods, Norbert Hauel, Ingo Konetzki, Annette Schuler-Metz, Rainer Walter