The Five-membered Nitrogen Hetero Ring Has Chalcogen As A Ring Member Patents (Class 514/253.1)
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Publication number: 20120283268Abstract: Thiazole and thiophene compounds are disclosed having utility in treating inflammatory conditions, immunoinflammatory conditions, autoimmune diseases, and cancers. Methods for the synthesis of these compounds are also disclosed.Type: ApplicationFiled: June 15, 2012Publication date: November 8, 2012Inventors: Anthony Giordano, Kamala K. Vasu, Hardik M. Thakar, Rajan S. Giri, Vasudevan Sudarsanam, Swapnil G. Yerande, Gajanan S. Inamdar
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Patent number: 8304412Abstract: The present application relates to novel 4-cycloalkyl- and 4-heterocycloalkyl-3,5-dicyano-2-thio-pyridine derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of hypertension and other cardiovascular disorders.Type: GrantFiled: November 17, 2007Date of Patent: November 6, 2012Assignee: Bayer Intellectual Property GmbHInventors: Peter Nell, Walter Hübsch, Barbara Albrecht-Küpper, Alexandros Vakalopoulos, Frank Süssmeier, Jörg Keldenich, Joachim Telser
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Publication number: 20120252815Abstract: The present invention relates to compounds of the formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, M1, M2, M3, Y1, Y2, V, W, n, m and o have the gleanings given herein, and physiologically acceptable salts, derivatives, prodrugs, solvates, tautomers and stereoisomers thereof, including mixtures thereof in all ratios, for use in the treatment of diseases which are influenced by inhibition of Sph kinase 1.Type: ApplicationFiled: November 18, 2010Publication date: October 4, 2012Applicant: Merck Patent Gesellschaft MIT Beschrankter HaftungInventors: Frank Stieber, Dirk Wienke
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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: 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: 20120252798Abstract: The present invention relates to new indole compounds, pharmaceutically acceptable salts or isomers thereof which are useful for the prevention or treatment of cellular necrosis and necrosis-associated diseases. The present invention also relates to a method and a composition for the prevention or treatment of cellular necrosis and necrosis-associated diseases, comprising said indole compounds as an active ingredient.Type: ApplicationFiled: June 11, 2012Publication date: October 4, 2012Inventors: Soon Ha KIM, Hyoung Jin Kim, Sun Young Koo, Sung Bae Lee, Heui Sul Park, Seung Hyun Yoon, Seung Yup Paek, Hyo Shin Kwak, Dong Ook Seo, Eok Park
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Publication number: 20120245176Abstract: A compound of Formula I is set forth, including pharmaceutically acceptable salts thereof: wherein Het is a 5 or 6-membered heterocycle with —N, —O, or —S adjacent to the —Ar substituent or adjacent to the point of attachment for the —Ar substituent; Ar is aryl or heteroaryl; R is —CH3, —CH2F, —CHF2 or —CH?CH2; V is —H, —CH3 or ?O; W is —NO2, —Cl, —Br, —CH2OH, or —CN; X is —Cl, —Br, —F, —CH3, —OCH3, or —CN; Y is —CH or —N; and Z is —CH or —N. This compound is useful in compositions for the prevention and treatment of influenza virus.Type: ApplicationFiled: September 23, 2011Publication date: September 27, 2012Inventors: Christopher W. Cianci, Samuel Gerritz, Sean Kim, David R. Langley, Guo Li, Bradley C. Pearce, Annapurna Pendri, Shuhao Shi, Weixu Zhai, Shirong Zhu
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Publication number: 20120245171Abstract: The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.Type: ApplicationFiled: December 3, 2010Publication date: September 27, 2012Applicant: GLAXO GROUP LIMITEDInventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Katherine Louise Jones, Paul Spencer Jones, Joelle Le, Christopher James Lunniss, Nigel James Parr, Timothy John Ritchie, John Edward Robinson, Juliet Kay Simpson, Christian Alan Paul Smethurst
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Publication number: 20120238539Abstract: A compound of Formula I is set forth, including pharmaceutically acceptable salts thereof: wherein Het is a 5 or 6-membered heterocycle with —N, —O, or —S adjacent to the —Ar substituent or adjacent to the point of attachment for the —Ar substituent; Ar is aryl or heteroaryl; R is —CH3, —CH2F, or —CH?CH2; W is —NO2, —Cl, —Br, —CHO, —CH?CH2, or —CN; X is —Cl, —CH3, or —CN; Y is —CH or —N; and Z is C1-C6 alkyl, C3-C6 cycloalkyl, substituted aryl, substituted heteroaryl, OR1, or NHR1, wherein R1 is selected from the group of H, aryl, heteroaryl, C1-C6 alkyl and C3-C6 cycloalkyl. This compound is useful in compositions for the prevention and treatment of influenza virus.Type: ApplicationFiled: September 6, 2011Publication date: September 20, 2012Inventors: Christopher W. Cianci, Samuel Gerritz, Guo Li, Bradley C. Pearce, Annapurna Pendri, Shuhao Shi, Weixu Zhai, Shirong Zhu
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Publication number: 20120238494Abstract: A method for recognizing and evaluating the presence and function of GnRH receptors on tumor cells including those originating in the brain and/or nervous system and/or the meninges and/or reactive neuroglia cells and/or primitive neuroectodermal tumor cells and/or on Kaposi sarcoma is provided. Furthermore, a method for reducing degenerate GnRH-positive tumor cells and/or for decreasing cellular replication of the above GnRH-positive tumor cells comprising administering to a cell or to a subject a replication decreasing amount of a GnRH agonist and/or GnRH antagonist and/or an erythropoietin agonist, and/or a thrombopoietin agonist, and/or a endothelin antagonist and/or a gonadotropin inhibiting hormone agonist is also provided. Furthermore, a diagnostic kit for detecting GnRH receptors on tumor cells according to the present methods is disclosed.Type: ApplicationFiled: March 27, 2012Publication date: September 20, 2012Inventor: JOHANNES C. VAN GROENINGHEN
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Publication number: 20120214790Abstract: The present invention provides compounds which show high effectiveness against positive symptoms, negative symptoms and cognitive dysfunction in schizophrenia and reduce conventional side-effect risks as well as have remarkable effects for central neurological diseases associated with cognitive dysfunction other than schizophrenia. N-Acyl cyclic amine derivatives of formula (1): wherein Ar1 and Ar2 are aryl or heteroaryl; V is nitrogen, or CR3; W1 is a single bond, —C(O)—, etc.; W2 is C1-alkylene; W3 is a single bond, methylene, —NH—, —CR4?CR5—, etc.; Ring Q is a group of formula (a) in which n is 0 or 1; m is 0 to 2; k is 1 to 3; Z is a single bond, methylene, oxygen, etc.; R1a, R1b and R1c are each, same or different, hydrogen, hydroxyl, halogen, cyano, C1-6 alkyl, etc.; or pharmaceutically acceptable salts thereof are provided.Type: ApplicationFiled: March 11, 2011Publication date: August 23, 2012Inventors: Megumi Maruyama, Naoya Kinomura, Satoshi Nojima, Masahiro Takamura, Keisuke Kakiguchi, Hiroto Tatamidani
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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: 20120202786Abstract: The invention provides a compound of formula I: wherein A1, A2, A3, R1, X, Y, and B have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of monoamine oxidase B (MAO-B) enzyme function and are useful for improving cognitive function and for treating psychiatric disorders in animals.Type: ApplicationFiled: April 16, 2012Publication date: August 9, 2012Applicant: Dart Neuroscience (Cayman) Ltd.Inventors: Alan P. Kaplan, Terence P. Keenan, Andrew J. McRiner
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Publication number: 20120202782Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or dysregulated B cell activities, particularly diseases or disorders that involve aberrant activation of inositol 1,4,5-trisphosphate 3-kinase B (ITPKb).Type: ApplicationFiled: April 12, 2012Publication date: August 9, 2012Applicant: IRM LLCInventors: Badry Bursulaya, Dai Cheng, Jiqing Jiang, Donald S. Karanewsky, Yi Liu, Shifeng Pan, Yongqin Wan, Xia Wang, Yun Feng Xie, Yang Yang
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Publication number: 20120196871Abstract: The present invention relates to an industrial process of preparing pharmaceutical compounds having the formula I: which are useful as certain tyrosine kinase inhibitors and more particularly as c-kit and bcr-abl inhibitors. The groups R1 and R2, identical or different, represent each a hydrogen, halogen atom, an alkyl, an alkoxy, a trifluoromethyl, an amino, an alkylamino, a dialkylamino, a solubilising group; m is 0-5 and n is 0-4; the group R3 represents an aryl or an heteroaryl group as described in claims herein.Type: ApplicationFiled: March 8, 2012Publication date: August 2, 2012Applicant: AB SCIENCEInventors: Alain MOUSSY, Philippe REGINAULT, François BELLAMY, Anne LERMET
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Publication number: 20120190681Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1, R2, R3, A, B, Z, n, and m are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as ALK and methods of treating diseases such as cancer.Type: ApplicationFiled: January 20, 2012Publication date: July 26, 2012Applicant: ABBOTT LABORATORIESInventors: Anil Vasudevan, Thomas D. Penning, Marina Pliuschev
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Patent number: 8227470Abstract: The present invention relates to a method for treating solid cancers including non-small 5 cell lung cancer, pancreatic, bladder, breast and ovarian cancer as well as advanced biliary tract cancers comprising administering at least one antineoplasticagent such as a nucleotide analog, for example gemcitabine, or an antimitotic such as docetaxel, in combination with a tyrosine kinase inhibitor selected from 2-aminoarylthiazoles and 2-aminoaryloxazoles.Type: GrantFiled: January 11, 2008Date of Patent: July 24, 2012Assignee: AB ScienceInventors: Alain Moussy, Jean-Pierre Kinet
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Publication number: 20120129843Abstract: This invention relates to thiazole I and its therapeutic and prophylactic uses, wherein the variables Rz, Q, J, R1, R3, R5, and R6 are defined in the specification. Disorders treated and/or prevented include rheumatoid arthritis.Type: ApplicationFiled: November 16, 2011Publication date: May 24, 2012Inventors: Yan ZHANG, Brett Andrew Tounge, Aihua Wang, Michael Hawkins, Kristi Anne Leonard, Joseph Kent Barbay, Umar S.M. Maharoof
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Publication number: 20120129870Abstract: The present invention is directed to piperidinyl and piperazinyl derivatives of formula (II) useful as inhibitors of the NPY Y2 receptor, pharmaceutical compositions comprising said compounds, processes for the preparation of said compounds and the use of said compounds for the treatment and/or prevention of disorders, diseases and conditions mediated by the NPY Y2 receptor.Type: ApplicationFiled: December 17, 2008Publication date: May 24, 2012Inventors: Wenying Chai, Jill A. Jablonowski, Dale A. Rudolph, Chandravadan R. Shah, Devin M. Swanson, Victoria D. Wong
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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: 20120114600Abstract: The invention provides compounds of formula (I): wherein the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are inhibitors of replication of the hepatitis C virus. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat hepatitis C viral infections, and processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: November 3, 2011Publication date: May 10, 2012Applicant: THERAVANCE, INC.Inventors: Robert Murray McKINNELL, Daniel D. LONG, Lori Jean VAN ORDEN, Lan JIANG, Mandy LOO, Daisuke Roland SAITO, Shella ZIPFEL, Eric L. Stangeland, Kassandra Lepack, Gavin Ogawa
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Patent number: 8173645Abstract: Compounds are provided for use with glucokinase that comprise the formula: 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: GrantFiled: March 20, 2008Date of Patent: May 8, 2012Assignee: Takeda San Diego, Inc.Inventors: Zacharia Cheruvallath, Jun Feng, Prasuna Guntupalli, Stephen L. Gwaltney, Joanne Miura, Mark Sabat, Mingnam Tang
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Publication number: 20120108576Abstract: The present invention provides compounds, salts and hydrates of Formula I, wherein the variables Ar1, R2, R3, R4, r, q, and t are defined herein. Certain compounds of Formula I described herein possess potent antiviral activity. The invention also provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. Certain compounds described herein inhibit assembly of the HCV replication complex. The invention also provides pharmaceutical compositions containing one or more compounds of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease. These infectious diseases include viral infections, particularly HCV infections.Type: ApplicationFiled: November 30, 2011Publication date: May 3, 2012Applicant: ACHILLION PHARMACEUTICALS, INC.Inventors: Suoming Zhang, Avinash Phadke, Cuixian Liu, Xiangzhu Wang, Jesse Quinn, Dawei Chen, Venkat Gadhachanda, Shouming Li, Milind Deshpande
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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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Patent number: 8163746Abstract: Provided is an agent for treating or preventing urinary frequency, urinary urgency and urinary, incontinence which are associated with overactive bladder, a lower urinary tract disease such as interstitial cystitis and chronic prostatitis accompanied by lower urinary tract pain, and various diseases accompanied by pain. A novel azolecarboxamide derivative in which an azole ring such as thioazole or oxazole is bonded to a benzene ring, pyridine ring or pyrimidine ring through carboxamide was confirmed to have a potent trkA receptor-inhibitory activity and found to be an agent for treating or preventing lower urinary tract disease and various diseases accompanied by pain, which is excellent in efficacy and safety, and thus the present invention was accomplished.Type: GrantFiled: April 19, 2007Date of Patent: April 24, 2012Assignee: Astellas Pharma Inc.Inventors: Keizo Sugasawa, Kenichi Kawaguchi, Takaho Matsuzawa, Ryushi Seo, Hironori Harada, Akira Suga, Tomoaki Abe, Hidenori Azami, Shunichiro Matsumoto, Takashi Shin, Masayuki Tanahashi, Toru Watanabe
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Publication number: 20120094996Abstract: There is provided compounds of formula (I): wherein R1, R2 and R3 have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. PI3-K, particularly class I PI3K) is desired and/or required, and particularly in the treatment of cancer.Type: ApplicationFiled: April 1, 2010Publication date: April 19, 2012Applicant: Centro Nacional de Investigaciones Oncologicas (CNIO)Inventors: Joaquin Pastor Fernández, Guido Kurz, Sonia Martinez Gonzalez
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Publication number: 20120082702Abstract: Disclosed are nicotinamide compounds of Formula (I): or stereoisomers or pharmaceutically acceptable salts thereof. Also disclosed are methods of using such compounds in the treatment of at least one Btk associated condition, such as, for example, inflammatory disease, and pharmaceutical compositions comprising such compounds.Type: ApplicationFiled: June 10, 2010Publication date: April 5, 2012Inventors: George V. DeLucca, Qing Shi, Chunjian Liu, Jingwu Duan, Andrew J. Tebben
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Publication number: 20120071467Abstract: Compounds or pharmacologically acceptable salts thereof are provided. In various embodiments the compounds have an antagonistic effect on a neurokinin NK1 receptor, a neurokinin NK2 receptor, and a muscarine M3 receptor. The compounds are useful as therapeutic agents for bronchial asthma, chronic obstructive pulmonary disease, or the like.Type: ApplicationFiled: September 16, 2011Publication date: March 22, 2012Applicant: Daiichi Sankyo Company, LimitedInventors: Takuya Ikeda, Takanori Yamazaki, Hiroshi Tsuchida
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Publication number: 20120071489Abstract: The present invention relates to a compound represented by the formula wherein each symbol is as defined in the present specification, which has a superior RBP4-lowering action and is useful as a pharmaceutical composition for the prophylaxis or treatment of a disease or condition mediated by an increase in RBP4.Type: ApplicationFiled: April 16, 2010Publication date: March 22, 2012Inventors: Shizuo Kasai, Kevin Francis McGee, JR.
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Patent number: 8138191Abstract: A synergistically effective combination of an anti-cancer agent and a therapeutic compound, such as an mTOR-Rictor complex inhibitor, a Serine 473 phosphorylation inhibitor, an AKT2 inhibitor, or a combination thereof, for use in the treatment of cancer, and methods and uses thereof. Also included are methods and uses of a thiosemicarbazone for treating a cancer in a mammal in need thereof characterized by over-expression of RAS, by an EGFR mutation, and/or by over-expression of AKT2.Type: GrantFiled: July 17, 2009Date of Patent: March 20, 2012Assignee: Critical Outcome Technologies Inc.Inventor: Wayne R. Danter
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Publication number: 20120065213Abstract: Described herein are compounds that are useful as ROCK inhibitors. These compounds, and pharmaceutically acceptable compositions thereof, are useful for treating or lessening the severity of a variety of disorders, including cardiovascular, inflammatory, neurological, or proliferative diseases or disorders.Type: ApplicationFiled: October 5, 2011Publication date: March 15, 2012Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Jeremy Green, Jingrong Cao, Upul Bandarage, Jon Come, Craig Marhefka
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Publication number: 20120059016Abstract: The present invention relates to piperidine and pyrazine derivatives according to formulae (Ia), (Ib) and (II) as autotaxin inhibitors and the use of such compounds for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by increased lysophosphatic acid levels and/or the activation of autotaxin, in particular of different cancers.Type: ApplicationFiled: March 3, 2010Publication date: March 8, 2012Inventors: Kai Schiemann, Melanie Schultz, Wolfgang Staehle
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Publication number: 20120052055Abstract: Invented is a method of treating thrombocytopenia in a human, in need thereof which comprises the in vivo administration of a therapeutically effective amount of a peptide or a non-peptide TPO receptor agonist and an anti-clotting agent or agents, and optional further active ingredients, to such human.Type: ApplicationFiled: May 6, 2010Publication date: March 1, 2012Applicant: Glaxosmithkline LLCInventors: Connie L. Erickson-Miller, Michael Arning
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Publication number: 20120046286Abstract: The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): And salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular PI3-kinase activity.Type: ApplicationFiled: April 28, 2010Publication date: February 23, 2012Inventors: Julie Nicole Hamblin, Paul Spencer Jones, Suzanne Elaine Keeling, Joelle Le, Charlotte Jane Mitchell, Nigel James Parr
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Publication number: 20120045412Abstract: The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.Type: ApplicationFiled: October 28, 2011Publication date: February 23, 2012Applicant: Gilead Sciences, Inc.Inventors: Lawrence S. Melvin, JR., Michael Graupe, Chandrasekar Venkataramani, Juan A. Guerrero
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Publication number: 20120028981Abstract: Provided herein are electrophilically enhanced kinase inhibitors. Also provided herein are methods of making and utilizing the same.Type: ApplicationFiled: November 5, 2009Publication date: February 2, 2012Applicant: PRINCIPIA BIOPHARMA INC.Inventor: Richard Miller
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Publication number: 20120028979Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.Type: ApplicationFiled: October 6, 2011Publication date: February 2, 2012Inventors: Gregory BASARAB, Pamela HILL, Brian SHERER, Fei ZHOU
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Patent number: 8106048Abstract: The present invention relates to compounds of the general formula (I) and salts and physiologically functional derivatives thereof, (I) wherein R1 is independently hydrogen, alkyl, cycloalkyl, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, arylalkyl or substituted arylalkyl; R2 is independently —NR3R4, (II) or (III) R3 is independently alkyl, cycloalkyl, alkoxy, alkylamine, —OH, —SH, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl, R4 is independently alkyl, cycloalkyl, alkoxy, alkylamine, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl; R5 is independently H, COR6, CO2R6, SOR6, SO2R6, SO3R6, alkyl, cycloalkyl, alkoxy, —NH2, alkylamine, —NR7COR6, halogen, —OH, —SH, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl; R6 is independently H, alkyl, cycloalkyl, —NH2, alkylamine, aryl or heteroaryl; R7 is independently H, alkyl, cycloalkyl, alkoxy, —OH, —SH, alkylthio, hydroxyalkyl, aryl, or heteroaryl;Type: GrantFiled: July 29, 2005Date of Patent: January 31, 2012Assignee: 4SC AGInventors: Johann Leban, Harald Schmitt, Kristina Wolf, Stefano Pegoraro, Andreas Wuzík
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Publication number: 20120022075Abstract: The present invention relates to a compound or a pharmacologically acceptable salt thereof having superior glucokinase activating activity, and is a compound represented by general formula (I), or pharmacologically acceptable salt thereof: [wherein, A represents, for example, an oxygen atom or sulfur atom, R1 represents, for example, a C1-C6 alkyl group, a C1-C6 alkoxy group or a C1-C6 halogenated alkyl group, A and R1 together with the carbon atom bonded thereto form a heterocyclic group that may be substituted with 1 to 3 group(s) independently selected from Substituent Group ?, R2 represents a phenyl group that may be substituted with 1 to 5 group(s) independently selected from Substituent Group ? or a heterocyclic group that may be substituted with 1 to 3 group(s) independently selected from Substituent Group ?, R3 represents a hydroxy group or a C1-C6 alkoxy group, and Substituent Group ? consists of, for example, a halogen atom, a C1-C6 alkyl group, a C1-C6 alkyl group substituted with 1 or 2 hydType: ApplicationFiled: August 5, 2011Publication date: January 26, 2012Inventors: Akihiro FURUKAWA, Takehiro FUKUZAKI, Yukari ONISHI, Hideki KOBAYASHI, Takeshi HONDA, Yumi MATSUI, Masahiro KONISHI, Kenjiro UEDA, Tetsuyoshi MATSUFUJI
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Patent number: 8101618Abstract: A compound represented by the formula (I): or a pharmaceutically acceptable salt thereof, wherein: R1 represents a branched lower alkyl group having from 3 to 9 carbon atoms or the like; R2 represents a 6-membered heteroaryl group having 1 or 2 nitrogen atoms or the like; R3 represents a hydrogen atom, an alkanoylamino group or the like; R4 represents a hydrogen atom, a lower alkyl group or the like; X1 represents an oxygen atom or a sulfur atom; X2 represents an oxygen atom or a single bond; and m indicates an integer of from 0 to 4. This compound has a metabotropic glutamate receptor 1 inhibitory effect, and therefore is useful for the treatment of a brain disorder such as convulsion, acute pain, inflammatory pain, chronic pain, cerebral infraction or transient cerebral ischemic attack, a mental dysfunction such as schizophrenia, and a disease such as anxiety and drug addition.Type: GrantFiled: April 5, 2006Date of Patent: January 24, 2012Assignee: MSD K.K.Inventors: Hiroshi Kawamoto, Toshifumi Kimura, Hisashi Ohta, Akio Sato, Atsushi Satoh, Gentaroh Suzuki
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Publication number: 20120015954Abstract: A compound of formula: wherein Ar1, A, R3, x, and m are as disclosed herein and Ar2 is a benzothiazolyl, benzooxazolyl, or benzoimidazolyl group or a pharmaceutically acceptable salt thereof (a “Benzoazolylpiperazine Compound”), compositions comprising a Benzoazolylpiperazine 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 Benzoazolylpiperazine Compound are disclosed.Type: ApplicationFiled: August 18, 2011Publication date: January 19, 2012Applicant: Purdue Pharma L.P.Inventors: Qun Sun, Laykea Tafesse, Sam Victory
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Publication number: 20120015957Abstract: The present invention is directed to piperidinyl and piperazinyl derivatives of formula (I) useful as inhibitors of the NPY Y2 receptor, pharmaceutical compositions comprising said compounds, processes for the preparation of said compounds and the use of said compounds for the treatment and/or prevention of disorders, diseases and conditions mediated by the NPY Y2 receptor.Type: ApplicationFiled: December 17, 2008Publication date: January 19, 2012Inventors: Wenying Chai, Curt A. Dvorak, Jill A. Jablonowski, Dale A. Rudolph, Chandravadan R. Shah, Victoria D. Wong
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Publication number: 20120010182Abstract: The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to new sulfonamide Nav1.7 inhibitors of formula (I): or pharmaceutically acceptable salts thereof, wherein Z1, Ra, Rb, R1, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.Type: ApplicationFiled: July 8, 2011Publication date: January 12, 2012Applicants: ICAGEN INC., PFIZER LIMITEDInventors: Alan Daniel Brown, Marcel John De Groot, Brian Edward Marron, David James Rawson, Thomas Ryckmans, Robert Ian Storer, Paul Anthony Stupple, Nigel Alan Swain, Christopher William West
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Publication number: 20120004217Abstract: A compound of formula: wherein Ar1, A, R3, x, and m are as disclosed herein and Ar2 is a benzothiazolyl, benzooxazolyl, or benzoimidazolyl group or a pharmaceutically acceptable salt thereof (a “Benzoazolylpiperazine Compound”), compositions comprising a Benzoazolylpiperazine 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 Benzoazolylpiperazine Compound are disclosed.Type: ApplicationFiled: August 8, 2011Publication date: January 5, 2012Applicant: Purdue Pharma L.P.Inventors: Qun SUN, Laykea TAFESSE, Sam VICTORY
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Patent number: 8088771Abstract: The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.Type: GrantFiled: July 28, 2009Date of Patent: January 3, 2012Assignee: Gilead Sciences, Inc.Inventors: Lawrence S. Melvin, Jr., Michael Graupe, Chandrasekar Venkataramani, Juan A. Guerrero
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Publication number: 20110312930Abstract: The present application relates to novel aryl compounds with aminoalkyl substituents, to processes for their preparation, to their use for treatment and/or prevention of diseases and to their use for the preparation of medicaments for treatment and/or prevention of diseases, in particular for treatment and/or prevention of hyperproliferative and angiogenic diseases and those diseases which arise from metabolic adaptation to hypoxic states. Such treatments can be carried out as monotherapy or also in combination with other medicaments or further therapeutic measures.Type: ApplicationFiled: October 31, 2009Publication date: December 22, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Michael Härter, Hartmut Beck, Peter Ellinghaus, Kerstin Berhörster, Susanne Greschat, Karl-Heinz Thierauch
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Publication number: 20110312939Abstract: The present invention relates to new compounds of general formula (I), wherein the groups R1 to R3, X1, X2, X3 and L1 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 in such a treatment.Type: ApplicationFiled: September 28, 2009Publication date: December 22, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Steffen Steurer, Peter Ettmayer, Andreas Mantoulidis
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Publication number: 20110312944Abstract: Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: ApplicationFiled: February 16, 2010Publication date: December 22, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Alessandra Bartolozzi, Angela Berry, Pier Francesco Cirillo, Eugene Richard Hickey, Doris Riether, Lifen Wu, Renee M. Zindell
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Publication number: 20110306619Abstract: Provided are heterocyclic compounds, their synthesis and pharmaceutical compositions including them for the treatment of disorders, in particular, cancer.Type: ApplicationFiled: February 25, 2010Publication date: December 15, 2011Applicant: URIFER LTD.Inventors: Uri Nir, Sally Shpungin, Etai Yaffe, Moshe Cohen
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Publication number: 20110301155Abstract: The present invention aims to provide a glucokinase activator useful as a pharmaceutical agent such as an agent for the prophylaxis or treatment of diabetes, obesity and the like, and the like.Type: ApplicationFiled: June 18, 2008Publication date: December 8, 2011Inventors: Tsuneo Yasuma, Shigekazu Sasaki, Osamu Ujikawa, Yasufumi Miyamoto, Stephen L. Gwaltney, Sheldon Cao, Andy Jennings