The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 548/253)
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Publication number: 20110130398Abstract: There are provided compounds of the formula wherein X, Y and R1 to R8 are described herein along with the enantiomers, pharmaceutically acceptable salts and esters thereof. The compounds are useful as anticancer agents.Type: ApplicationFiled: November 4, 2010Publication date: June 2, 2011Inventors: David Joseph Bartkovitz, Xin-Jie Chu, Qingjie Ding, Bradford James Graves, Nan Jiang, Jing Zhang, Zhuming Zhang
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Publication number: 20110118322Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.Type: ApplicationFiled: October 15, 2010Publication date: May 19, 2011Inventors: David Robert Bolin, Yimin Qian, Kshitij Chhabilbhai Thakkar, Lin Yi, Weiya Yun
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Patent number: 7943648Abstract: The present invention provides pharmaceutically acceptable salts of imidazole-5-carboxylic acid derivatives, methods for preparing same and pharmaceutical compositions comprising same. The salts obtained by the present invention can be easily dissolved in common solvents, such as water and methanol. The bioavailability thereof is good in animal body. Thereby it is applicable to be developed as a normal preparation for treating hypertension.Type: GrantFiled: June 5, 2009Date of Patent: May 17, 2011Assignee: Shanghai Allist Pharmaceutical Inc.Inventors: Jianghui Guo, Dong An
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Patent number: 7943780Abstract: The invention relates to process for the preparation of Candesartan cilexetil. More particularly, it relates to the preparation of pure candesartan cilexetil by the deprotection of Trityl candesartan cilexetil with inorganic acids.Type: GrantFiled: February 14, 2007Date of Patent: May 17, 2011Assignee: Matrix Laboratories Ltd.Inventors: Seeta Ramajaneyulu Gorantla, Mohan Bandari, Nageswara Rao Karusala
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Patent number: 7943778Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.Type: GrantFiled: April 20, 2009Date of Patent: May 17, 2011Assignee: Reata Pharmaceuticals, Inc.Inventors: Xin Jiang, Xiaofeng Liu, Jack Greiner, Stephen S. Szucs, Melean Visnick
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Patent number: 7943779Abstract: The present invention relates to an improved process for the manufacture of olmesartan and pharmaceutically acceptable salts and esters thereof as an active ingredient of a medicament for the treatment of hypertension and related diseases and conditions.Type: GrantFiled: July 27, 2006Date of Patent: May 17, 2011Assignee: KRKAInventors: Silvo Zupancic, Anica Pecavar, Miha Vrbinc, Renata Osolnik
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Publication number: 20110111467Abstract: Disclosed is a method for the preparation of carbamic acid (R)-1-aryl-2-tetrazolyl-ethyl esters, comprising the enantioselective enzyme reduction of a 1-aryl-2-tetrazolyl-ethyl ketone to form a (R)-1-aryl-2-tetrazolyl-ethyl alcohol and the carbamation of said alcohol.Type: ApplicationFiled: October 14, 2010Publication date: May 12, 2011Inventors: Sang Chul Lim, Moo Yong Uhm, Dae Won Lee, Hui Ho Kim, Dong Ho Lee, Hyun Seok Lee
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Publication number: 20110112051Abstract: The present invention relates generally to pyrrolidine and thiazolidine DPP-IV inhibitor compounds. The present invention also provides synthetic methods for preparation of such compounds, methods of inhibiting DPP-IV using such compounds and pharmaceutical formulations containing them for treatment of DPP-IV mediated diseases, in particular, Type-2 diabetes.Type: ApplicationFiled: January 13, 2011Publication date: May 12, 2011Applicant: Alantos Pharmaceuticals Holding, Inc.Inventors: Heiko KROTH, Tim Feuerstein, Frank Richter, Jürgen Boer, Michael Essers, Bert Nolte, Matthias Schneider, Matthias Hochguertel, Fritz-Frieder Frickel, Arthur Taveras, Christoph Steeneck
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Publication number: 20110104043Abstract: The subject of the invention is the (50) continuous flow system for the synthesis of nanoparticles which consist of the (1a) feeding unit connected to the flow path, at least one (2) first reactor unit possessing the (13) heatable reactor-zone, the (3) second reactor unit which follows (2) in the same cascade; the (5) mixing unit and the (1b) second feeding unit between (2) and (3) reactor units, the (9) and (10) feeding pumps connected to the raw material source and/or (22) control unit which is capable of controlling at least one (18) pressure controller and/or controlling the temperature of at least one (13) heatable reactor-zone; each (13) heatable reactor-zone is followed by (14) cooling unit in the cascade. In addition, the subject of this invention is a process for the synthesis of nanoparticles, preferably metal-containing nanoparticles, and nanoparticles of biologically active organic molecules wherein the process is accomplished in the device according to FIG. 1.Type: ApplicationFiled: April 28, 2009Publication date: May 5, 2011Applicant: Nangenex Nanotechnology IncorporatedInventors: Krisztián Niesz, Attila Wootsch, Maxime Groualle, Zsolt Ötvös, Ferenc Darvas
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Publication number: 20110105763Abstract: An N-[(2?-(1-triphenyl methyl tetrazole-5-yl)biphenyl]-4-yl]methyl]-L-valine benzyl ester organic salt of formula (IVA) wherein A represents an organic carboxylic acid, a process for its preparation and its use in the synthesis of valsartan or salts thereof.Type: ApplicationFiled: May 7, 2008Publication date: May 5, 2011Applicant: CIPLA LIMITEDInventors: Rajendra Narayanrao Kankan, Dharmaraj Ramachandra Rao, Srinivas Laxminarayan Pathi, Ravikumar Puppala
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Publication number: 20110105539Abstract: A process for obtaining 2?-halo-4-methylbiphenyls is described, which comprises reacting 4 halotoluene with a 1,2-dihalobenzene in the presence of elemental metal such as magnesium, lithium or zinc, wherein 0 to 0.9 molar, particularly 0 to 0.2 molar excess of 4-halotoluene in regard to 1,2-dihalobenzene is used, and arised organometal intermediates are quenched by elemental mental halogen. In addition, the coupling of arised 2?-halo-4-methylbiphenyls with 2-(1-propyl)-4-methyl-6-(1?-methylbenzimidazole-2-il)benzimidazole to afford 3?-(2?-halo-biphenyl-4-ylmethyl)-1,7?-dimethyl-2?-propyl-1H,3?H-[2,5?]bibenzoimidazolyl, which can be further converted to organometallic compound and said organometallic compound is further reacted with formic acid derivative, such as N,N-dimethylformamide, alkylformiate or carbon dioxide to obtain telmisartan, is also described.Type: ApplicationFiled: March 19, 2009Publication date: May 5, 2011Applicant: LEK Pharmaceuticals D.D.Inventors: Anton Copar, Zdenko Casar, Andrej Premrl
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Publication number: 20110104162Abstract: The present invention relates to a compound of general formula (I): and also to the pharmaceutically acceptable salts thereof, to the isomers or isomer mixtures thereof in all proportions, in particular to an enantiomer mixture, and especially to a racemic mixture. The present invention also relates to the use of these compounds as a medicament, and in particular for the treatment of cancer, and also to the compositions containing them.Type: ApplicationFiled: June 15, 2009Publication date: May 5, 2011Applicant: Cytomics SystemsInventors: Denis Carniato, Karine Jaillardon, Olivier Busnel, Mathieu Gutmann, Jean-Francois Briand, Benoit Deprez, Dominique Thomas, Cécile Bougeret
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Publication number: 20110092551Abstract: The invention is directed to compounds having the formula: wherein: Ar, r, R2-3, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: December 21, 2010Publication date: April 21, 2011Applicant: THERAVANCE, INC.Inventors: Paul ALLEGRETTI, Seok-Ki CHOI, Roland GENDRON, Paul R. FATHEREE, Keith JENDZA, Robert Murray McKINNELL, Darren McMURTRIE, Brooke OLSON
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Publication number: 20110093959Abstract: The present invention provides for anrelate to an animal model for characterizing emesis, and for screening and characterizing emetic and antiemetic agents. In several embodiments, the Least Shrew, Cryptotis parva, provides a specific and rapid behavioral animal model to screen concomitantly both the CNS penetration and the antiemetic potential of antiemetic agents to relieve, for example, chemotherapy-induced emesis.Type: ApplicationFiled: January 30, 2009Publication date: April 21, 2011Applicant: WESTERN UNIVERSITY OF HEALTH SCIENCESInventor: Nissar A. Darmani
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Publication number: 20110092713Abstract: The present invention provides a method for producing a 1-biphenylmethylimidazole compound having superior angiotensin II receptor antagonistic activity, or an intermediate thereof. The present invention provides a method for producing a compound having the formula (5) (R1, Ra: H, an alkyl group) by oxidizing a compound having the formula (1) (Ra: H, an alkyl group) using an oxidizing agent in the presence of a radical initiation reagent, and then reacting with an ammonia-generating reagent and a compound having the formula R1CHO(R1: H, an alkyl group) or a compound having the formula R1C(ORb)3 (R1: H, an alkyl group; Rb: an alkyl group).Type: ApplicationFiled: June 8, 2009Publication date: April 21, 2011Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Koji Sato, Tsutomu Yagi, Kenji Sakuratani, Yuichiro Tani
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Publication number: 20110091541Abstract: Preparation of AT1 receptors antagonists formulations using the cyclodextrins, their derivatives and/or biodegradable polymers for the treatment of arterial hypertension, other cardiovascular disease and their complications. Until now, no applications using the AT11 receptor antagonists and cyclodextrins or derivatives and/or biodegradable polymers for the treatment of arterial hypertension, other cardiovascular diseases and their complications, was found in the technical state of art. The present invention is characterized by the combination of two different technologies: one is the molecular encapsulation of AT11 receptor antagonists in cyclodextrins and the other is the microencapsulation in biodegradable polymers. It also comprises the increase of the effectiveness of the AT11 receptor antagonists as well as an increase in their bio-availability.Type: ApplicationFiled: December 23, 2010Publication date: April 21, 2011Applicant: Universidade Federal de Minas GeraisInventors: Rubén Dario Sinisterra Millán, Robson Augusto Souza Dos Santos, Fréderic Jean Georges Frezard, Washington Xavier De Paula
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Publication number: 20110086854Abstract: There are provided compounds of the formula wherein X, Y, R1, R2, R3, R3, R4, and R5 are as described herein and enantiomers and pharmaceutically acceptable salts and esters thereof which are useful as anticancer agents.Type: ApplicationFiled: October 6, 2010Publication date: April 14, 2011Inventors: David Joseph Bartkovitz, Xin-Jie Chu, Jin-Jun Liu, Tina Morgan Ross, Zhuming Zhang
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Publication number: 20110086889Abstract: The invention relates to tetrazole compounds of formula (I) wherein X, Y, Z, R1, R2 and R3 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: June 10, 2009Publication date: April 14, 2011Inventors: Hamed Aissaoui, Christoph Boss, Christine Brotschi, John Gatfield, Ralf Koberstein, Romain Siegrist, Thierry Sifferlen, Jodi Williams
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Patent number: 7923567Abstract: The invention relates to novel compound of formula (IV), which is an organic acid salt of N-[(2?-cyanobiphenyl-4-yl)methyl]-(L)-valine ester. This compound is an useful intermediate for process of preparation of Valsartan of formula (I), chemically known as (S)-N-(1-Carboxy-2-methylprop-1-yl)-N-pentanoyl-N-[2?-(1H-terazol-5-yl)biphenyl-4-ylmethyl]amine. This invention also relates to a process for preparing Valsartan using novel intermediate of formula (IV).Type: GrantFiled: June 15, 2010Date of Patent: April 12, 2011Assignee: Alembic LimitedInventors: Rohit Ravikant Soni, Sanjay Lakhabhai Vasoya, Ravindra Charudatta Ghotikar, Anand Kumar Pandey, Hetal Remeshchandra Shah
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Publication number: 20110082295Abstract: To develop a highly safe measure to treat Alzheimer's disease using a secretase-inhibiting substance, there is provided a compound represented by the following general formula (I) or a salt thereof: wherein A represents a phenyl group or the like, R1 represents a chlorine atom, a bromine atom, or a nitro group or the like, R2, R3, R4, and R5 each represent a hydrogen atom or the like, and L represents CH2—CH2 or CH?CH.Type: ApplicationFiled: May 27, 2009Publication date: April 7, 2011Applicants: Tokyo Institute of Technology, Kyoto UniversityInventors: Hachiro Sugimoto, Takashi Takahashi, Ichiro Hijikuro, Michiaki Okuda
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Publication number: 20110071197Abstract: There is provided compounds of formula I, wherein ring A, D1, D2a, D2b, D3, L1, Y1, L3 and Y3 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of leukotriene C4 synthase is desired and/or required, and particularly in the treatment of a respiratory disorder and/or inflammation.Type: ApplicationFiled: April 16, 2009Publication date: March 24, 2011Inventors: Peter Nilsson, Martins Katkevics, Benjamin Pelcman
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Publication number: 20110064695Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with said compounds.Type: ApplicationFiled: September 10, 2010Publication date: March 17, 2011Inventors: Yao-Ling Qiu, Ce Wang, Lu Ying, Xiaowen Peng, Yat Sun Or
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Publication number: 20110065765Abstract: A compound having the structure R—Y wherein R is, for example, Y is selected from the group consisting of 1) R5, 2) —C(R1R2)(C(R3R4))0-1Y1R5, and 3) —C(R1R2)—O—Y1R5; R1, R2, R3 and R4 are independently selected from the group consisting of hydrogen and C1-4 alkyl; R5 is Y1 is selected from the group consisting of —C(O)—O— and —P(O)(OR6)—O—; and R6 is hydrogen or CH3, or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.Type: ApplicationFiled: May 6, 2009Publication date: March 17, 2011Inventors: Amjad Ali, Michael Man-chu Lo, Iyassu K. Sebhat, Chris Franklin, Nicoletta Almirante, Silvia Stefanini, Stefano Biondi, Ennio Ongini
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Publication number: 20110052674Abstract: New angiotensin II receptor blocker nitroderivatives of general formula (I) and pharmaceutically acceptable salts or stereoisomers thereof: and their use for treating cardiovascular, renal and chronic liver diseases, inflammatory processes and metabolic syndromes.Type: ApplicationFiled: February 19, 2009Publication date: March 3, 2011Applicants: MERCK SHARP & DOHME CORP., NICOX S.A.Inventors: Nicoletta Almirante, Alessia Nicotra, Valentino Mandelli, Stefano Biondi, Silvia Stefanini, Iyassu K. Sebhat, Michael Man-Chu Lo
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Publication number: 20110046599Abstract: Compositions and methods for modifying biologically active substances to achieve multi-day delivery of such substances, particularly through oral or parenteral administration, are disclosed. The compositions include the biologically active substance conjugated to a carrier having a suitably long half life, typically more than one day, wherein the conjugate optionally contains a spacer linking the carrier to the biologically active substance. Pharmaceutical formulations of the conjugates are also disclosed, as are methods of extending delivery of a single dose of a biologically active substance for more than one day.Type: ApplicationFiled: June 26, 2008Publication date: February 24, 2011Inventor: Agis Kydonieus
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Publication number: 20110046105Abstract: The invention relates to compounds of formula (I) wherein the groups R and R?, A, D, E, G, L, p and R1 to R10 have the stated meanings and to their physiologically compatible salts. Said compounds are suitable, for example, as anti-obesity drugs.Type: ApplicationFiled: August 6, 2010Publication date: February 24, 2011Applicant: SANOFI-AVENTISInventors: Gerhard Jaehne, Siegfried Stengelin, Matthias Gossel, Thomas Klabunde, Irvin Winkler
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Publication number: 20110039851Abstract: The invention relates to a compound of formula (I): or a tautomer thereof or a pharmaceutically acceptable salt thereof, wherein R1 to R11, W, X, Y, Z, and n are as defined herein. The invention also relates to methods of using the compounds of formula (I) and compositions thereof to treat various diseases and disorders in a patient. The invention also relates to processes for preparing the compounds of formula (I) and intermediates useful in these processes.Type: ApplicationFiled: October 14, 2008Publication date: February 17, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Kaka Dey, Donghong Amy Gao, Daniel R. Goldberg, Alexander Heim-Riether, John Edward Mangette, Ingo Andreas Mugge, Roger John Snow, Alan David Swinamer, Jiang-Ping Wu, Zhaoming Xiong, Yu Yang
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Publication number: 20110034701Abstract: Present invention is to provide one pot synthesis of candesartan without isolating the ester intermediate.Type: ApplicationFiled: October 9, 2007Publication date: February 10, 2011Inventors: Dutt Tyagi Om, Nageswara Rao Karusala, Uma Sankara Sastry Tummalapalli, Mohan Bandari, Seeta Ramanjaneyulu Gorantla
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Patent number: 7884211Abstract: Caspase activity and apoptosis are promoted using active, dimeric Smac peptide mimetics of the general formula M1-L-M2, wherein moieties M1 and M2 are monomeric Smac mimetics and L is a covalent linker. Target cancerous or inflammatory cells are contacted with an effective amount of an active, dimeric Smac mimetic, and a resultant increase in apoptosis of the target cells is detected. The contacting step may be effected by administering to a pharmaceutical composition comprising a therapeutically effective amount of The compoundic mimetic, wherein the individual may be subject to concurrent or antecedent radiation or chemotherapy for treatment of a neoproliferative pathology.Type: GrantFiled: July 24, 2009Date of Patent: February 8, 2011Assignee: Board of Regents, The University of Texas SystemInventors: Patrick G. Harran, Xiaodong Wang, Jef K. De Brabander, Lin Li, Ranny Mathew Thomas, Hidetaka Suzuki
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Publication number: 20110028447Abstract: This invention relates to compounds, pharmaceutical compositions and methods for the treatment of a condition mediated by CB1 receptor activity in a mammalian subject including a human, which comprises administering to a mammal in need of such treatment a therapeutically effective amount of the compound of formula (I) wherein R1, R2 and R3 are as defined in this specification.Type: ApplicationFiled: February 26, 2009Publication date: February 3, 2011Inventors: Ingrid Price Buchler, Michael Joseph Hayes, Shridhar Gajanan Hegde, Susan Landis Hockerman, Darin Eugene Jones, Steven Wade Kortum, Joseph Gerace Rico, Ruth Elizabeth TenBrink, Kun Ken Wu
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Publication number: 20110028446Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L1, M and R11 are as defined herein. The compounds of Formula (I) are selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.Type: ApplicationFiled: October 8, 2010Publication date: February 3, 2011Inventors: Donald J.P. Pinto, Joanne M. Smallheer, James R. Corte, Zilun Hu, Cullen L. Cavallaro, Paul J. Gilligan, Mimi L. Quan, Leon M. Smith, II
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Patent number: 7879893Abstract: The present invention relates to novel ligands for the HisB10 Zn2+ sites of the R-state insulin hexamer having the formula A-B-C-D-X (III), wherein: A is a chemical group which reversibly binds to a HisB10 Zn2+ sites of an insulin hexamer; B is a linker; C is a fragment consisting of 0 to 5 neutral amino acids; D is a fragment comprising 1 to 20 positively charged groups independently selected from amino or guanidino groups; and X is —OH, —NH2 or a diamino group. The present invention also relates to R-state insulin hexamers comprising such ligands, and aqueous insulin preparations comprising such R-state insulin hexamers.Type: GrantFiled: September 13, 2002Date of Patent: February 1, 2011Assignee: Novo Nordisk A/SInventors: Helle Birk Olsen, Niels C. Kaarsholm, Peter Madsen, Soren Ostergaard, Svend Ludvigsen, Palle Jakobsen, Anders Klarskov Petersen, Dorte Bjerre Steensgaard
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Publication number: 20110015234Abstract: The invention is concerned with novel indazole derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used in the prevention or treatment of diseases which are modulated by L-CPT1 inhibitors.Type: ApplicationFiled: September 8, 2010Publication date: January 20, 2011Inventors: Jean Ackermann, Konrad Bleicher, Simona M. Ceccarelli, Odile Chomienne, Patrizio Mattei
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Publication number: 20110009409Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: July 2, 2010Publication date: January 13, 2011Inventors: Brooke Blair, Paul R. Fatheree, Melissa Fleury, Roland Gendron, Ryan Hudson, Robert Murray McKinnell, Michael Wilson
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Publication number: 20110009370Abstract: The present invention provides for compositions and methods for modulating tissue growth using tissue growth modulators, which are agents that either enhance or inhibit tissue growth as desired by a particular indication by modulating the PG or Wnt signaling pathways, or employing modulators of both PG and Wnt signaling pathways for a synergistic effect or highly selective effect.Type: ApplicationFiled: October 22, 2007Publication date: January 13, 2011Applicant: CHILDREN'S MEDICAL CENTER CORPORATIONInventors: Leonard I. Zon, Trista E. North, Wolfram Goessling
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Publication number: 20110009385Abstract: A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein: R3 is selected from cyclopentyl and cyclohexyl; R9 is a substituted 5 or 6-membered aryl or heteroaryl group or a 6,5- or 6,6-fused biaryl or heterobiaryl group. Compounds of formula (I) exhibit surprisingly high dual efficacies for human cathepsin S and K and are useful for the treatment of rheumatoid arthritis, osteoarthritis, chronic obstructive pulmonary disease (COPD), atherosclerosis, cardiovascular diseases which exhibit significant damage and remodeling of extracellular matrix (ECM) and chronic pain.Type: ApplicationFiled: August 9, 2010Publication date: January 13, 2011Applicant: Amura Therapeutics LimitedInventors: MARTIN QUIBELL, John P. Watts, Nicholas S. Flinn
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Publication number: 20110009386Abstract: A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein: one of R3 and R4 is H, and the other is selected from C1-6-alkyl, C1-6-haloalkyl, C1-6-alkoxy, and C6-12-aralkyl; or R3 and R4 are each independently selected from C1-6-alkyl and halo; R9 is a substituted 5 or 6-membered aryl or heteroaryl group or a 6,5- or 6,6-fused biaryl or heterobiaryl group. Compounds of formula (I) exhibit surprisingly high efficacies for human cathepsin S, excellent selectivity verses other mammalian cathepsins and are useful for treatment of diseases such as rheumatoid arthritis, multiple sclerosis, myasthenia gravis, transplant rejection, diabetes, Sjogrens syndrome, Grave's disease, systemic lupus erythematosis, osteoarthritis, psoriasis, idiopathic thrombocytopenic purpura, allergic rhinitis, asthma, atherosclerosis, obesity, chronic obstructive pulmonary disease and chronic pain.Type: ApplicationFiled: August 9, 2010Publication date: January 13, 2011Applicant: Amura Therapeutics LimitedInventors: Martin Quibell, John P. Watts, Nicholas S. Flinn
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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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Patent number: 7858651Abstract: The invention discloses imidazole-5-carboxylic acid derivatives, and their preparation methods. The derivatives of the invention are Angiotensin II receptor antagonists with angiotensin II antagonistic activity and antihypertensive activity, and thereby can be used as a therapeutical agent to treat hypertension.Type: GrantFiled: July 31, 2006Date of Patent: December 28, 2010Assignee: Shanghai Allist Pharmaceutical, Inc.Inventors: Jianhui Guo, Dong An
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Patent number: 7858645Abstract: The invention is concerned with novel indazole derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used in the prevention or treatment of diseases which are modulated by L-CPT1 inhibitors.Type: GrantFiled: October 19, 2007Date of Patent: December 28, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Jean Ackermann, Konrad Bleicher, Simona M. Ceccarelli, Odile Chomienne, Patrizio Mattei
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Publication number: 20100323410Abstract: Disclosed is a method for the preparation of carbamic acid (R)-1-aryl-2-tetrazolyl-ethyl ester, comprising the asymmetric reduction of arylketone and the carbamation of alcohol.Type: ApplicationFiled: October 14, 2009Publication date: December 23, 2010Inventors: Sang Chul Lim, Moo Yong Uhm, Nahm Ryune Cho, Dae Won Lee, Ju Young Lee, Hui Ho Kim, Dong Ho Lee
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Publication number: 20100316607Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: June 15, 2010Publication date: December 16, 2010Inventors: Yat Sun Or, Xiaowen Peng, Lu Ying, Ce Wang, Yao-Ling Qiu
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Publication number: 20100316601Abstract: The bicyclo-substituted pyrazolon-azo derivatives of formula (I) or pharmaceutical acceptable salts, hydrates or solvates thereof, methods for their preparation, pharmaceutical compositions containing the same and their use as a therapeutic agent, especially as thrombopoietin (TPO) mimetics and their use as agonists of thrombopoietin receptor are disclosed. The definition of substituents in formula (I) are the same as defined in the description.Type: ApplicationFiled: January 4, 2009Publication date: December 16, 2010Inventors: Peng Cho Tang, Hejun Lü, Hao Zheng, Yiqian Chen, Hongbo Fel, Shenglan Wang, Li Wang
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Publication number: 20100311800Abstract: The present invention relates to nitrooxyderivatives of angiotensin II receptor antagonists.Type: ApplicationFiled: February 19, 2009Publication date: December 9, 2010Inventors: Nicoletta Almirante, Alessia Nicotra, Silvia Stefanini, Stefano Biondi, Ennio Ongini, Amjad Ali, Michael Man-chu Lo
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Publication number: 20100305324Abstract: A phamaceutical composition comprising a phenyltetrazole derivative of formula (I) or a pharmaceutical acceptable salt thereof is effective in preventing or treating osteoporosis, obesity, diabetes, or hyperlipidemia, by regulating protein TAZ. wherein, A is ethyl or n-butyl; R1 is methyl, —CH2OH, —CO2CH3, —CH2F, —CH(OCH3)2, —CH2OC(?O)CH3, styryl or —CH2OCH2SCH3; R2 is H, Br, —CO2CH3, phenyl, pyridin-2-yl, pyridin-3-yl, ?or styryl; R3 is H or methyl; X is CH or N; and P is H or —CH(CH3)OCH2CH3.Type: ApplicationFiled: April 22, 2010Publication date: December 2, 2010Applicant: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGYInventors: Nak Jeong KIM, Myung-Ae Bae, Sung-Eun Yoo, Namsook Kang, Jung Nyoung Heo, Kyu Yang Yi, Jee Hee Suh, Sung Youn Chang, Eun Sook Hwang, Jeong-Ho Hong
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Publication number: 20100305131Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, B1, X and n are defined herein. The invention also relates a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: May 27, 2010Publication date: December 2, 2010Inventors: Gary Mark Coppola, Yuki Iwaki, Rajeshri Ganesh Karki, Toshio Kawanami, Gary Michael Ksander, Muneto Mogi, Robert Sun
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Publication number: 20100292283Abstract: This invention relates to novel phenyl-acetamide and phenyl-propionamide derivatives that are found to be potent modulators of potassium channels and, as such, are valuable candidates for the treatment of diseases or disorders as diverse as those which are responsive to the modulation of potassium channels.Type: ApplicationFiled: November 26, 2008Publication date: November 18, 2010Inventors: Antonio Nardi, Jeppe Kejser Christensen
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Publication number: 20100292190Abstract: The present invention relates to compounds of general formula (I) as tublin polymerisation inhibitors and methods for preparing such compounds.Type: ApplicationFiled: February 14, 2006Publication date: November 18, 2010Applicant: Bionomics LimitedInventors: Jason Hugh Chaplin, Gurmit Singh Gill, Damian Wojciech Grobelny, Bernard Luke Flynn
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Publication number: 20100286149Abstract: This invention relates to novel benzamide derivatives that are found to be potent modulators of potassium channels and, as such, are valuable candidates for the treatment of diseases or disorders as diverse as those which are responsive to the modulation of potassium channels.Type: ApplicationFiled: November 25, 2008Publication date: November 11, 2010Inventors: Antonio Nardi, Jeppe Kejser Christensen
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Patent number: 7825152Abstract: The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.Type: GrantFiled: April 9, 2007Date of Patent: November 2, 2010Assignee: Novartis AGInventors: Trixi Brandl, Jiping Fu, Francois Lenoir, David Thomas Parker, Michael Patane, Branko Radetich, Prakash Raman, Pascal Rigollier, Mohindra Seepersaud, Oliver Simic, Aregahegn Yifru, Rui Zheng