Polycyclo Ring System Having The 1,3-thiazole Ring As One Of The Cyclos Patents (Class 546/270.1)
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Publication number: 20130116430Abstract: An object of the present invention is to provide to a compound and a pharmaceutical composition, which have excellent Syk-inhibitory activity. The present invention provides a nicotinamide derivative represented by the following formula (I) (wherein R1 represents a halogen atom; R2 represents a C1-12 alkyl group, a C2-12 alkenyl group, a C2-12 alkynyl group, a C3-8 cycloalkyl group, an aryl group, an ar-C1-6 alkyl group or a heterocyclic group, each optionally having at least one substituent; R3 represents an aryl group or a heterocyclic group each optionally having at least one substituent; and R4 and R5 each independently represent a hydrogen atom; and R2 and R4 may form a cyclic amino group optionally having at least one substituent together with the nitrogen atom to which they bind) or a salt thereof, and a pharmaceutical composition for use in the treatment of a Syk-related disease which comprises the nicotinamide derivative or a salt thereof.Type: ApplicationFiled: December 28, 2012Publication date: May 9, 2013Applicant: FUJIFILM CORPORATIONInventors: Hideyasu FUJIWARA, Kimihiko SATO, Shinsuke MIZUMOTO, Yuichiro SATO, Hideki KURIHARA, Yohei KUBO, Hiyoku NAKATA, Yasutaka BABA, Takashi TAMURA, Hidenobu KUNIYOSHI, Shinji HAGIWARA, Mari YAMAMOTO
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Publication number: 20130079325Abstract: Pyridine and pyrimidine compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.Type: ApplicationFiled: November 14, 2012Publication date: March 28, 2013Inventors: Jennifer R. Allen, Biswas Kaustav, Frank Chavez, Ning Chen, Frenel Fils De Morin, James R. Falsey, Michael J. Frohn, Paul E. Harrington, Daniel B. Horne, Essa Hu Harrington, Matthew R. Kaller, Roxanne Kunz, Holger Monenschein, Thomas T. Nguyen, Alexander J. Pickrell, Andreas Reichelt, Shannon Rumfelt, Robert M. Rzasa, Kelvin Sham, Guomin Yao
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Patent number: 8399465Abstract: Compounds with two fused bicyclic heteroaryl moieties and their pharmaceutical compositions, and methods of using them as leukotriene A4 hydrolase (LTA4H) modulators and for the treatment of diseases, disorders and conditions mediated by LTA4H.Type: GrantFiled: May 12, 2010Date of Patent: March 19, 2013Assignee: Janssen Pharmaceutica NVInventors: Genesis Bacani, Christa C. Chrovian, Wendy Eccles, Anne M. Fourie, Laurent Gomez, Cheryl A. Grice, Aaron M. Kearney, Adrienne M. Landry-Bayle, Alice Lee-Dutra, Alejandro Santillán, Jr., Virginia M. Tanis, John J. M. Wiener
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Publication number: 20130060025Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, X, Z1, Z2, Z3, Z4 and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: September 12, 2012Publication date: March 7, 2013Inventors: Luke W. Ashcraft, Gustave Bergnes, Chihyuan Chuang, Scott Collibee, Pu-Ping Lu, Bradley Morgan, Alex Muci, Xiangping Qian, Jeffrey Warrington, Zhe Yang
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Publication number: 20130053403Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and methods of using the same in the treatment or prevention of diseases mediated by the activation of b3-adrenoceptor.Type: ApplicationFiled: April 25, 2011Publication date: February 28, 2013Inventors: Richard Berger, Scott D. Edmondson, Bart H. Harper
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Publication number: 20130053345Abstract: Novel compounds of structure Formula I: or an enantiomer, diastereomer, tautomer, prodrug or salt thereof, wherein A, D, Di, E, J, L, n, Q, R2 and R4 are defined herein, are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the GPR119 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.Type: ApplicationFiled: May 4, 2011Publication date: February 28, 2013Inventors: Xiang-Yang Ye, Dean A. Wacker, Jeffrey A. Robl, Ying Wang
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Patent number: 8383932Abstract: A compound for an organic photoelectric device, represented by the following Chemical Formula 1:Type: GrantFiled: April 19, 2010Date of Patent: February 26, 2013Assignee: Cheil Industries, Inc.Inventors: Ho-Kuk Jung, Myeong-Soon Kang, Jin-Seong Park, Nam-Soo Kim, Kyu-Yeol In, Eiu-Su Kang, Mi-Young Chae
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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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Publication number: 20130040943Abstract: This disclosure relates to compounds of formula I: wherein R1, R2, R3, R4, X and Y have the meanings denoted in the disclosure. The compounds of formula I have antithrombotic activity and in particular inhibit the protease-activated receptor 1 (PAR1). The disclosure further relates to a method for producing the compound of formula I and to the use thereof as a pharmaceutical product.Type: ApplicationFiled: October 16, 2012Publication date: February 14, 2013Applicant: SANOFIInventor: SANOFI
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Publication number: 20130035332Abstract: The present invention is directed to benzothiazol-one and thiazolo pyridine-one derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. 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 metabotropic glutamate receptors are involved.Type: ApplicationFiled: April 25, 2011Publication date: February 7, 2013Inventors: Mark E. Layton, Michael J. Kelly
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Publication number: 20130018052Abstract: The present invention provides a novel 2-pyridyl substituted imidazole derivative, or a pharmaceutically acceptable salt or solvate thereof, which selectively inhibits the transforming growth factor-? (TGF-?) type I receptor (ALK5) and/or the activin type I receptor (ALK4); a pharmaceutical composition comprising same as an active ingredient; and a use of the 2-pyridyl substituted imidazole derivative for the manufacture of a medicament for preventing or treating a disease mediated by ALK5 and/or ALK4 receptors in a mammal.Type: ApplicationFiled: July 13, 2012Publication date: January 17, 2013Applicant: SK CHEMICALS CO., LTD.Inventors: Ju Young LEE, Keun-Ho RYU, Jae-Sun KIM, Yong-Hyuk KIM, Dong Chul SHIN, Bong-yong LEE, Sang-hwan KANG, Hyun-Jung LEE, Hoechul JUNG, Young Ah SHIN, Euisun PARK, Jaeseung AHN
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Patent number: 8350048Abstract: The present invention relates to compounds that have CYP450 inhibiting properties and are therefore useful as boosters of certain drugs, i.e. they are able to increase at least one of the pharmacokinetic variables of certain drugs when co-administered. The invention further provides the use of said compounds as improvers of the bioavailability of certain drugs. Methods for the preparation of the compounds of the invention and pharmaceutical compositions are also provided.Type: GrantFiled: December 5, 2008Date of Patent: January 8, 2013Assignee: Janssen R&D IrelandInventors: Tim Hugo Maria Jonckers, Wim Bert Griet Schepens, Geerwin Yvonne Paul Haché, Beate Sabine Hallenberger, Jennifer Chiyomi Sasaki, Judith Eva Baumeister, Gerben Albert Van 'T Klooster
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Publication number: 20130005752Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.Type: ApplicationFiled: June 19, 2012Publication date: January 3, 2013Applicant: Viamet Pharmaceuticals, Inc.Inventors: William J. Hoekstra, Christopher M. Yates, Robert J. Schotzinger, Michael R. Loso, Zachary A. Buchan, Michael T. Sullenberger
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Publication number: 20120329788Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.Type: ApplicationFiled: June 19, 2012Publication date: December 27, 2012Applicant: Viamet Pharmaceuticals, Inc.Inventors: William J. Hoekstra, Christopher M. Yates, Robert J. Schotzinger, Michael R. Loso, Zachary A. Buchan, Michael T. Sullenberger, Gary D. Gustafson
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Publication number: 20120321563Abstract: The invention provides agents that target carbonic anhydrase, which can be used as imaging agents or therapeutic agents. The agents can be used to image tumor hypoxia as well as other physiological processes in a subject.Type: ApplicationFiled: May 9, 2012Publication date: December 20, 2012Inventors: Kevin Groves, Bagna Bao
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Publication number: 20120321562Abstract: This invention relates to new fluorescent chemical entities, including fluorescent molecules that comprise a carboxyl or carbonyl functionalized pyridine moiety. This invention also relates to the corresponding reactive versions of such molecules. This invention also relates to the corresponding conjugates with moieties such as peptides, proteins, various biomolecules, carbocyclic and heterocyclic compounds, sugars, and their uses thereof.Type: ApplicationFiled: April 18, 2012Publication date: December 20, 2012Inventors: Milind Rajopadhye, Narasimhachari Narayanan, Jeffrey D. Peterson
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Publication number: 20120289698Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, X, Z1, Z2, Z3, Z4 and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: April 13, 2012Publication date: November 15, 2012Inventors: Luke W. Ashcraft, Gustave Bergnes, Chihyuan Chuang, Scott Collibee, Pu-Ping Lu, Bradley Morgan, Alex Muci, Xiangping Qian, Jeffrey Warrington, Zhe Yang
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Publication number: 20120288501Abstract: New substituted benz-azole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.Type: ApplicationFiled: July 24, 2012Publication date: November 15, 2012Applicant: Novartis Vaccines and Diagnostics, Inc. formerly known as Chiron CorporationInventors: Payman Amiri, Wendy Fantl, Barry Haskell Levine, Daniel J. Poon, Savithri Ramurthy, Paul A. Renhowe, Sharadha Subramanian, Leonard Sung
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Publication number: 20120288855Abstract: Chemical compounds having a high selectivity for double stranded DNA over RNA and single stranded DNA are disclosed. The chemical compounds are stains that become fluorescent upon illumination and interaction with double stranded DNA, but exhibit reduced or no fluorescence in the absence of double stranded DNA. The compounds can be used in a variety of biological applications to qualitatively or quantitatively assay DNA, even in the presence of RNA.Type: ApplicationFiled: July 26, 2012Publication date: November 15, 2012Applicant: LIFE TECHNOLOGIES CORPORATIONInventors: Jolene A. Bradford, Ching-Ying Cheung, Shih-Jung Huang, Patrick R. Pinson, Stephen T. Yue
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Patent number: 8304556Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.Type: GrantFiled: January 11, 2012Date of Patent: November 6, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Darryl McConnell, Maria Impagnatiello, Dirk Kessler, Oliver Kraemer, Siegfried Schneider, Lars Van Der Veen, Ulrike Weyer-Czernilofsky, Tobias Wunberg
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Patent number: 8299065Abstract: Compound of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; AIk is an optionally substituted, divalent C1-C6 alkylene, alkenylene or alkynylene radical which may contain an ether (—O—), thioether (—S—) or amino (—NR)— link, wherein R is hydrogen, —CN or C1-C3 alkyl; X is —C(?O)NR6—, or —C(?O)O— wherein R6 is hydrogen, optionally substituted C1-C6 alkyl, C2-C6 alkenyl or C2-C6 alkynyl; Z1 is —N? or —CH?Z2 is —N? or —C(R1)?; R1 is hydrogen, methyl, ethyl, ethenyl, ethynyl, methoxy, mercapto, mercaptomethyl, halo, fully or partially fluorinated (C1-C2)alkyl, (C1-C2JaIkoxy or (C1-C2)alkylthio, nitro, or nitrile (—CN); R2 is a group Q1-[Alk1]q-Q2-, wherein q is 0 or 1; AIk1 is an optionally substituted, divalent, straight chain or branched C1-C6 alkylene, or C2-C6 alkenylene or C2-C6 alkynylene radical which may contain or terminate in an ether (—O—), thioether (—S—) or amino (—NR)— link; Q2 is an optionally substituted divalent monocyclic carbocyclic or heterocyclic raType: GrantFiled: December 12, 2008Date of Patent: October 30, 2012Assignee: Biota Europe Ltd.Inventors: David John Haydon, Lloyd George Czaplewski
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Publication number: 20120271054Abstract: The present invention provides a compounds 7a-f to 18a-f and 19a-f to 30a-f of general formula A, useful as potential anticancer agents against human cancer cell lines. The present invention further provides a process for the preparation of imidazothiazole-chalcone hybrids 7a-f to 18a-f and 19a-f to 30a-f of general formula A.Type: ApplicationFiled: October 7, 2010Publication date: October 25, 2012Applicant: COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCHInventors: Ahmed Kamal, Dastagiri Dudekula, Surendranadha Reddy Jonnala, Vijaya Bharathi Earla
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Patent number: 8293769Abstract: Benzoxazole and benzothiazole compounds and their oxides, esters, prodrugs, solvates, and pharmaceutically acceptable salts thereof are disclosed. Compositions of the compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier, and uses of the compounds, either alone or in combination with at least one additional therapeutic agent are also disclosed. The embodiments are useful for inhibiting cellular proliferation, inhibiting the growth and/or metathesis of tumors, treating or preventing cancer, treating or preventing degenerating bone diseases such as rheumatoid arthritis, and/or inhibiting molecules such as CSF 1R.Type: GrantFiled: May 20, 2008Date of Patent: October 23, 2012Assignee: Novartis AGInventors: Simon C. Ng, Keith B. Pfister, Martin Sendzik, James Sutton, Allan S. Wagman, Marion Wiesmann
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Publication number: 20120264704Abstract: The present application relates to novel substituted dihydropyrazolone derivatives, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and hematological diseases and kidney diseases, and for promoting wound healing.Type: ApplicationFiled: October 26, 2007Publication date: October 18, 2012Inventors: Kai Thede, Ingo Flamme, Felix Oehme, Jens-Kerim Ergüden, Friederike Stoll, Joachim Schuhmacher, Hanno Wild, Peter Kolkhof, Hartmut Beck, Metin Akbaba, Mario Jeske
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Publication number: 20120263646Abstract: Disclosed are new imaging agents and their use for the in vivo diagnostic of neurodegenerative diseases, notably Alzheimer's disease and related diseases.Type: ApplicationFiled: October 15, 2010Publication date: October 18, 2012Applicant: GUERBETInventors: Sarah Catoen, Thierry Gautheret
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Publication number: 20120252814Abstract: Compounds of the following formula are provided for use with glucokinase: wherein the variables are as 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 said compounds.Type: ApplicationFiled: March 21, 2012Publication date: October 4, 2012Applicant: TAKEDA CALIFORNIA, INC.Inventors: Zacharia Cheruvallath, Jun Feng, Prasuna Guntupalli, Stephen L. Gwaltney, Joanne Miura, Mark Sabat, Mingnam Tang, Haxia Wang
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Publication number: 20120252759Abstract: Compounds of the formula Ia and Ib, in which R1, R1?, R2, R3, R5, R6 and R7 have the meanings indicated in claim 1, are kinase inhibitors and can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: November 9, 2010Publication date: October 4, 2012Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKER HAFTINGInventors: Timo Heinrich, Hannes Koolman
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Publication number: 20120252800Abstract: The present invention relates to novel bicyclic thiazoles which are positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (“mGluR5”) and which are useful for the treatment or prevention of disorders associated with glutamate dysfunction and diseases in which the mGluR5 subtype of receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which mGluR5 is involved.Type: ApplicationFiled: December 16, 2010Publication date: October 4, 2012Applicant: Janssen Pharmaceutica N.V.Inventors: Gregor James MacDonald, Gary John Tresadern, Andrés Avelino Trabanco-Suárez, Joaquin Pastor-Fernández
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Publication number: 20120232118Abstract: Potent and selective ligands for the dopamine 3 (D3) receptor are disclosed. The D3 receptor ligands have a structural formula: wherein R1 is C1-6 alkyl or C3-6cycloalkyl; or wherein R2 is substituted with one or two halogen(s) or OC1-3alkyl.Type: ApplicationFiled: February 28, 2012Publication date: September 13, 2012Applicants: UNIVERSITY OF KANSAS, THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Shaomeng Wang, Jianyong Chen, Gregory Collins, Beth Levant, James H. Woods
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Publication number: 20120214994Abstract: The present invention relates to (3-fluoro-2-hydroxy)propyl-functionalized aryl derivatives or to the pharmaceutically acceptable salt thereof, to a method for preparing same, and to a pharmaceutical composition containing same as active ingredients for the diagnosis or treatment of neurodegenerative brain diseases. The aryl derivatives of the present invention are (3-fluoro-2-hydroxy)propyl-functionalized to increase the polarity thereof, and therefore the drugs containing the aryl derivatives can easily permeate into the cerebrovascular membrane, thus increasing the effectiveness of the drugs. As the aryl derivatives of the present invention strongly bind to ?-amyloid, the aryl derivatives, when labeled with radioisotope, can be used as a diagnostic agent for non-invasively diagnosing early Alzheimer's disease.Type: ApplicationFiled: September 14, 2010Publication date: August 23, 2012Inventors: Dae-Yoon Chi, Byoung-Se Lee, Sirion Uthaiwan, So-Young Chu, Yu-Jin Bae, Chansoo Park, Dae-Hyuk Moon, Jin-Sook Ryu, Jae-Seung Kim, Seung-Jun Oh
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Patent number: 8247565Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benfit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: GrantFiled: September 27, 2010Date of Patent: August 21, 2012Assignee: Sirtris Pharmaceuticals, Inc.Inventors: Jean Bemis, Jeremy S. Disch, Michael Jirousek, Walter Joseph Lunsmann, Pui Yee Ng, Chi B. Vu
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Publication number: 20120207679Abstract: The present invention relates to novel heteroaryl substituted benzothiazole derivatives, precursors thereof, and therapeutic uses for such compounds, having the structural formula (I) below: and to their pharmaceutically acceptable salt, compositions and methods of use. Furthermore, the invention relates to novel heteroaryl substituted benzothiazole derivatives that are suitable for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. More specifically, the present invention relates to a method of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease as well as measuring clinical efficacy of Alzheimer's disease therapeutic agents.Type: ApplicationFiled: April 23, 2012Publication date: August 16, 2012Applicant: ASTRAZENECA ABInventors: Ylva Gravenfors, Catrin Jonasson, Jonas Malmström, Gunnar Nordvall, David Pyring, Can Slivo, Daniel Sohn, Peter Ström, David Wensbo
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Publication number: 20120207729Abstract: The invention relates to substituted benzothiazoles, benzoxazoles—and their counterparts having pyridine and pyrimidine rings replacing the benzene ring—that are PDE4 inhibitors useful for treating stroke, myocardial infarct, and cardiovascular inflammatory conditions, to pharmaceutical compositions comprising these compounds, and to methods for the treatment of stroke, myocardial infarct, and cardiovascular inflammatory conditions in a mammal. The compounds have general formula I: in which A and B are carbocycles or heterocycles.Type: ApplicationFiled: April 24, 2012Publication date: August 16, 2012Applicant: DECODE GENETICS EHFInventors: Jasbir SINGH, Mark E. GURNEY, Alex BURGIN, Alexander KISELYOV, Munagala RAO
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Publication number: 20120196891Abstract: A heterocyclic compound represented by formula (1): wherein A1, A2, R1, R2, R3, R4, n and so on are defined in tha description, has an excellent control effect on arthropod pests and is useful for control of arthropod pests.Type: ApplicationFiled: September 30, 2010Publication date: August 2, 2012Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventor: Mitsuhiko Iwakoshi
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Publication number: 20120165322Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: June 29, 2011Publication date: June 28, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Brian Nicholas Cook, Jennifer A. Kowalski, Xiang Li, Daniel Richard Marshall, Sabine Schlyer, Robert Sibley, Lana Louise Smith-Keenan, Fariba Soleymanzadeh, Ronald John Sorcek, Erick Richard Roush Young, Yunlong Zhang
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Publication number: 20120157403Abstract: Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein represents an optional double bond, the dotted line is optionally a bond or no bond, resulting in a double bond or a single bond, as permitted by the valency requirement and wherein E, A, G M, Het, B, X, R3, R10, R11, R32 and R33 are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.Type: ApplicationFiled: February 24, 2012Publication date: June 21, 2012Inventors: Samuel Chackalamannil, Mariappan V. Chelliah, Yuguang Wang, Yan Xia
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Patent number: 8203001Abstract: The present invention encompasses compounds of general formula (1) wherein R1, M1, L1 and Q are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or anomalous cell proliferation, and the use thereof for preparing a pharmaceutical composition with the above-mentioned properties.Type: GrantFiled: June 13, 2007Date of Patent: June 19, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Ulrich Reiser, Peter Ettmayer, Oliver Kraemer, Peter Sennhenn, Walter Spevak
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Publication number: 20120129811Abstract: This invention relates to tricycle I and its therapeutic and prophylactic uses, wherein the variables C1, C2, Z1, Z2, Q, J, R1, and R3 are defined in the specification. Disorders treated and/or prevented include rheumatoid arthritis.Type: ApplicationFiled: November 16, 2011Publication date: May 24, 2012Inventors: Aihua WANG, Yan Zhang, Kristi Anne Leonard, Michael Hawkins, Brett Andrew Tounge, Umar S.M. Maharoof, Joseph Kent Barbay
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Patent number: 8178560Abstract: A compound of formula: where Ar1, Ar2, X, R3, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a “Cycloheteroalkenyl Compound”); compositions comprising an effective amount of a Cycloheteroalkenyl Compound; and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Cycloheteroalkenyl Compound are disclosed herein.Type: GrantFiled: June 17, 2010Date of Patent: May 15, 2012Assignee: Purdue Pharma L.P.Inventors: Qun Sun, Xin Wen
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Publication number: 20120115845Abstract: A compound of formula I or a pharmaceutically acceptable salt thereof in which R1, R2, R3, R4 and m are as described in the specification for use in the treatment of obesity and/or diabetes.Type: ApplicationFiled: November 7, 2011Publication date: May 10, 2012Inventors: Jack McQueen ALLEN, Roger John Butlin, Clive Green, William McCoull, Graeme Richard Robb, James Matthew Wood
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Publication number: 20120108585Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: August 11, 2009Publication date: May 3, 2012Applicant: Sirtris Pharmaceuticals, Inc.Inventor: Chi B. Vu
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Publication number: 20120108618Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R3 and X are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.Type: ApplicationFiled: April 22, 2010Publication date: May 3, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Lars Van Der Veen, Darryl Mcconnell, Siegfried Schneider, Matthias Grauert, Andreas Schoop, Tobias Wunberg
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Publication number: 20120108567Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.Type: ApplicationFiled: January 11, 2012Publication date: May 3, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Darryl McCONNELL, Maria IMPAGNATIELLO, Dirk KESSLER, Oliver KRAEMER, Siegfried SCHNEIDER, Lars VAN DER VEEN, Ulrike WEYER-CZERNILOFSKY, Tobias WUNBERG
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Publication number: 20120108637Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands and methods for using such compounds and compositions.Type: ApplicationFiled: December 22, 2011Publication date: May 3, 2012Applicant: Abbott LaboratoriesInventors: Marlon D. COWART, Yi-Yin Ku, Sou-Jen Chang, Dilinie P. Fernando, Timothy A. Grieme, Robert J. Altenbach
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Patent number: 8163928Abstract: The present invention relates to novel heteroaryl substituted benzothiazole derivatives, precursors thereof, and therapeutic uses for such compounds, having the structural formula (I) below: [Chemical formula should be inserted here. Please see paper copy] and to their pharmaceutically acceptable salt, compositions and methods of use. Furthermore, the invention relates to novel heteroaryl substituted benzothiazole derivatives that are suitable for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. More specifically, the present invention relates to a method of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease as well as measuring clinical efficacy of Alzheimer's disease therapeutic agents.Type: GrantFiled: January 25, 2007Date of Patent: April 24, 2012Assignee: AstraZeneca ABInventors: Ylva Gravenfors, Catrin Jonasson, Jonas Malmstrom, Gunnar Nordvall, David Pyring, Can Slivo, Daniel Sohn, Peter Strom, David Wensbo
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Publication number: 20120095021Abstract: The present disclosure provides a compound of general formula A useful as potential anti-tubercular agents.Type: ApplicationFiled: September 14, 2011Publication date: April 19, 2012Inventors: Ahmed Kamal, Rajesh VCRNC Shetti, P. Swapna, Shaik Azeeza, A. Malla Reddy, Inshad Ali Khan, Sheikh Tasduq Abdullah, Sandeep Sharma, Nitin Pal Kalia
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Patent number: 8143258Abstract: Provided is a fused heterocycle derivative showing a strong Raf inhibitory activity. A compound represented by the formula wherein each symbol is as defined in the present specification, or a salt thereof.Type: GrantFiled: December 1, 2009Date of Patent: March 27, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Masanori Okaniwa, Terufumi Takagi, Masaaki Hirose
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Publication number: 20120071475Abstract: Provided is a compound or a pharmaceutically acceptable salt thereof which inhibits the activity of PI3K to regulate many biological processes including the growth, differentiation, survival, proliferation, migration, metabolism, and the like of cells and is therefore useful for the prophylaxis/therapy of diseases including inflammatory diseases, arteriosclerosis, vascular/circulatory diseases, cancer/tumors, immune system diseases, cell proliferative diseases, infectious diseases, and the like. The above problem was solved by providing a urea derivative shown in the present specification, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: April 26, 2010Publication date: March 22, 2012Applicant: SHIONOGI & CO., LTD.Inventors: Daisuke Taniyama, Yasunori Mitsuoka, Kayoko Hata
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Publication number: 20120071512Abstract: The present invention provides a compound of formula I; 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 12, 2010Publication date: March 22, 2012Applicant: NOVARTIS AGInventors: Qi-Ying Hu, Sylvie Chamoin, Christopher M. Adams, Chun Zhang
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Patent number: 8133901Abstract: The invention relates to piperidine compounds of formula (I): wherein X—R1 represents —N(H)-pyrimidinyl, wherein said pyrimidinyl is unsubstituted or mono-substituted wherein the substituent is selected from (C1-4)alkyl or halogen, or X—R1 represents —NH—C(O)-heterocyclyl, wherein the heterocyclyl is selected from benzofuranyl and imidazo[2,1-b]-thiazolyl, wherein said heterocyclyl is unsubstituted or independently mono-, di- or tri-substituted wherein the substituents are independently selected from (C1-4)alkyl; A represents a phenyl- or thiazolyl-group, wherein the phenyl or thiazolyl is unsubstituted or mono-substituted with (C1-4)alkyl; B represents a phenyl-group, wherein the phenyl is unsubstituted or mono-, or di- substituted, wherein the substituents are independently selected from the group consisting of (C1-4)alkyl, (C1-4)alkoxy, trifluoromethyl, cyano and halogen; to pharmaceutically acceptable salts thereof, and to the use of such compounds use as medicaments, especially as orexin receptor antType: GrantFiled: November 29, 2007Date of Patent: March 13, 2012Assignee: Actelion Pharmaceuticals Ltd.Inventors: Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, Thierry Sifferlen