The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 548/194)
  • Publication number: 20130123242
    Abstract: The present invention provides novel compounds represented by formula I: or pharmaceutically acceptable salts thereof useful for treating flaviviridae viral infection.
    Type: Application
    Filed: October 26, 2012
    Publication date: May 16, 2013
    Applicant: Vertex Pharmaceuticals (Canada) Incorporated
    Inventors: Laval Chan Chun Kong, Jean Bedard, Sanjoy Kumar Das, Nghe Nguyen-Ba, Oswy Z. Pereira, Thumkunta Jagadeeswar Reddy, Mohammad Arshad Siddiqui, Wuyi Wang, Constantin G. Yannopoulos
  • Publication number: 20130096056
    Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): where V, W, R1, R2, R3 and R4 are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.
    Type: Application
    Filed: September 14, 2012
    Publication date: April 18, 2013
    Applicant: XENON PHARMACEUTICALS INC.
    Inventors: Jianmin Fu, Duanjie Hou, Rajender Kamboj, Vishnumurthy Kodumuru, Natalia Pokrovskaia, Vandna Raina, Shaoyi Sun, Serguei Sviridov, Zaihui Zhang
  • Publication number: 20130072471
    Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-gated sodium channels. More particularly, the invention provides substituted aryl sulfonamides, compositions comprising these compounds, as well as methods of using these compounds or compositions in the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrence of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a voltage-gated sodium channel.
    Type: Application
    Filed: November 15, 2012
    Publication date: March 21, 2013
    Inventors: Brian Edward Marron, Paul Christopher Fritch, Christopher John Markworth, Andrew Thomas Maynard, Nigel Alan Swain
  • Patent number: 8399497
    Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
    Type: Grant
    Filed: November 23, 2010
    Date of Patent: March 19, 2013
    Assignee: Merck Serono SA
    Inventors: Anna Quattropani, David Covini, Vincent Pomel, Jerome Dorbais, Thomas Rueckle
  • Publication number: 20130066076
    Abstract: The present invention relates to processes for the preparation of biaryl oxazolidinones. These compounds are useful as anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents.
    Type: Application
    Filed: September 14, 2012
    Publication date: March 14, 2013
    Inventors: Yusheng Wu, Shili Chen, Yi Chen, Roger Hanselmann, Rongliang Lou, Jiacheng Zhou
  • Publication number: 20130065902
    Abstract: The present invention relates to 3-(heteroaryl-amino)-1,2,3,4-tetrahydro-9H-carbazole derivatives of the formula (I), wherein R1, R2 and R3 are as described in the description and their use as prostaglandin receptor modulators, most particularly as prostaglandin D2 receptor modulators, in the treatment of various prostaglandin-mediated diseases and disorders, to pharmaceutical compositions containing these compounds and to processes for their preparation.
    Type: Application
    Filed: March 21, 2011
    Publication date: March 14, 2013
    Applicant: Actelion Pharmaceuticals Ltd.
    Inventors: Hamed Aissaoui, Heinz Fretz, Julien Hazemann, Sylvia Richard-Bildstein, Romain Siegrist
  • Patent number: 8394798
    Abstract: The present invention provides compositions and methods for inducing neuronal cell differentiation.
    Type: Grant
    Filed: January 23, 2012
    Date of Patent: March 12, 2013
    Assignee: The Scripps Research Institute
    Inventors: Masaki Warashina, Kyung Hoon Min, Fred Gage, Peter Schultz, Sheng Ding, Tomoko Kuwabara
  • Patent number: 8383653
    Abstract: Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed.
    Type: Grant
    Filed: June 30, 2004
    Date of Patent: February 26, 2013
    Assignee: Albert Einstein College of Medicine of Yeshiva University
    Inventors: Vern L. Schramm, Anthony A. Sauve
  • Publication number: 20130018054
    Abstract: The present invention provides organic compounds of the following structure; A-L1-B—C-D-L2-E that are useful for treating or preventing conditions or disorders associated with DGAT1 activity in animals, particularly humans.
    Type: Application
    Filed: September 13, 2012
    Publication date: January 17, 2013
    Applicant: NOVARTIS AG
    Inventors: Michael H. SERRANO-WU, Young-shin KWAK, Wenming Liu
  • Publication number: 20130012532
    Abstract: A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein R1 represents a C1 to C6 alkyl group which may be substituted by one to three groups selected from substituent group A, or the like (substituent group A: a hydroxy group, a halogeno group, a cyano group, a nitro group, an amino group, a carboxy group, a C1 to C3 alkyl group, etc.); R2, R3, and R8 each independently represent a hydrogen atom or a C1 to C3 alkyl group; R4, R5, R6, R7, R9, and R10 each independently represent a hydrogen atom or the like; and R11 represents a hydrogen atom or the like, has TAFIa enzyme inhibitory activity and is useful as a therapeutic drug for myocardial infarction, angina pectoris, acute coronary syndrome, cerebral infarction, deep vein thrombosis, pulmonary embolism, or the like.
    Type: Application
    Filed: March 14, 2011
    Publication date: January 10, 2013
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Tsutomu Nagata, Jun Kobayashi, Yoshiyuki Onishi, Masamichi Kishida, Kengo Noguchi
  • Publication number: 20130012708
    Abstract: A compound represented by the formula (1): wherein A is a nitrogen atom or CR4, B is an oxygen atom, a sulfur atom or NR9 (provided that when A is a nitrogen atom, B is not NH), R1 is a C2-14 aryl group, L1 is a bond, CR10R11, an oxygen atom, a sulfur atom or NR12, X is OR13, SR13 or NR14NR15, R2 is a hydrogen atom, a formyl group, a C1-10 alkyl group or the like, L2 is a bond or the like, L3 is a bond, CR17R18, an oxygen atom, a sulfur atom or NR19, L4 is a bond, CR20R21, an oxygen atom, a sulfur atom or NR22, Y is an oxygen atom, a sulfur atom or NR23, and R3 is a C2-14 aryl group, a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.
    Type: Application
    Filed: September 13, 2012
    Publication date: January 10, 2013
    Applicant: Nissan Chemical Industries Limited
    Inventors: Shingo Owada, Shunsuke Iwamoto, Kazufumi Yanagihara, Katsuaki Miyaji, Takanori Nakamura, Norihisa Ishiwata, Yutaka Hirokawa
  • Publication number: 20130005738
    Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.
    Type: Application
    Filed: September 12, 2012
    Publication date: January 3, 2013
    Applicant: ARIAD Pharmaceuticals, Inc.
    Inventors: William C. Shakespeare, Wei-Sheng Huang, David C. Dalgarno, Xiaotian Zhu, R. Mathew Thomas, Yihan Wang, Jiwei Qi, Rajeswari Sundaramoorthi, Dong Zou, Chester A. Metcalf, III, Tomi K. Sawyer, Jan Antoinette C. Romero
  • Publication number: 20130004457
    Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Application
    Filed: September 11, 2012
    Publication date: January 3, 2013
    Inventors: Carol Bachand, Makonen Bekema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Gan Wang, Lawrence G. Hamann
  • Publication number: 20120316208
    Abstract: Compounds which inhibit microbial growth or attenuate the virulence of pathogen microorganisms. Compounds of the invention inhibit UDP-galactopyranose mutase (UGM) and have activity as inhibitors of microbial growth of microorganisms which contain this enzyme and particularly those microorganisms in which this enzyme is responsible for the incorporation of galactofuranose residues, particularly for uridine 5?-diphosphate (UDP) galactopyranose mutase. Compounds of the invention inhibit UDP-galactopyranose mutase (UGM) and have activity to attenuate virulence of pathogenic microorganisms, including mycobacteria.
    Type: Application
    Filed: August 21, 2012
    Publication date: December 13, 2012
    Inventors: Laura Lee KIESSLING, Emily Carla DYKHUIZEN, John F. MAY
  • Publication number: 20120316148
    Abstract: The invention relates to compounds and methods for modulating one or more components of a kinase signaling cascade.
    Type: Application
    Filed: June 7, 2012
    Publication date: December 13, 2012
    Applicant: Dynamix Pharmaceuticals LTD.
    Inventors: Oren M. Becker, Itai Bloch, Efrat Ben-Zeev, Alina Shitrit, Avihai Yacovan, Sharon Gazal, Vered Behar, Alexander Konson, Nili Schutz, Sima Mirilashvili, Gali Golan
  • Publication number: 20120302569
    Abstract: This invention relates to phenyl thiazole I and its therapeutic and prophylactic uses, wherein the variables Rz, Q, J, R1, R3, R5, R6, and R7 are defined in the specification. Disorders treated and/or prevented include rheumatoid arthritis.
    Type: Application
    Filed: May 24, 2012
    Publication date: November 29, 2012
    Inventors: Paul Francis JACKSON, Kristi Anne Leonard, Joseph Kent Barbay, Aihua Wang, Brett Andrew Tounge, Yan Zhang, Umar S.M. Maharoof
  • Publication number: 20120295920
    Abstract: HIV inhibitors of formula wherein R1 is halo, C1-4alkoxy, trifluoromethoxy; n is 0 or 1; A is CH or N; R5 and R6 are hydrogen, C1-4alkyl, halo; R7 and R8 are C1-4alkyl or C1-4alkoxyC1-4alkyl; R9 is C1-4alkyl, cyclopropyl, trifluoromethyl, C1-4alkoxy, or dimethylamino; R10 is hydrogen, C1-4alkyl, cyclopropyl, trifluoromethyl, C1-4alkoxy, or dimethylamino; pharmaceutically acceptable addition salts and solvates thereof; pharmaceutical compositions containing these compounds as active ingredient and processes for preparing said compounds.
    Type: Application
    Filed: December 10, 2010
    Publication date: November 22, 2012
    Inventors: Genadiy Kalayanov, Bart Rudolf Romanie Kesteleyn, Kevin Parkes, Bengt Bertil Samuelsson, Wim Bert Griet Schepens, Johannes Wilhelmus J. Thuring, Hans Kristian Wallberg, Jörg Kurt Wegner
  • Publication number: 20120269864
    Abstract: The present invention is a compound of formula (I) or formula (II) which are suitable as NP-1 antagonists.
    Type: Application
    Filed: June 11, 2012
    Publication date: October 25, 2012
    Inventors: Haiyan Jia, Ian ZACHARY, Michelle TICKNER, Lili CHENG, Chris CHAPMAN, Katie ELLARD, Basil HARTZOULAKIS, Ashley JARVIS, Rosemary LYNCH, Jamie NALLY, David SELWOOD, Mark STEWART
  • Publication number: 20120258078
    Abstract: The present invention relates to novel Linked Tricyclic Aryl Compounds, compositions comprising at least one Linked Tricyclic Compound, and methods of using Linked Tricyclic Aryl Compounds for treating or preventing HCV infection in a patient.
    Type: Application
    Filed: May 28, 2010
    Publication date: October 11, 2012
    Applicant: Schering Corporation
    Inventors: Qingbei Zeng, Kevin X. Chen, Anilkumar Gopinadhan Nair, Stuart B. Rosenblum, Joseph A. Kozlowski, F. George Njoroge
  • Patent number: 8273778
    Abstract: Compounds which inhibit microbial growth or attenuate the virulence of pathogen microorganisms. Compounds of the invention inhibit UDP-galactopyranose mutase (UGM) and have activity as inhibitors of microbial growth of microorganisms which contain this enzyme and particularly those microorganisms in which this enzyme is responsible for the incorporation of galactofuranose residues, particularly for uridine 5?-diphosphate (UDP) galactopyranose mutase. Compounds of the invention inhibit UDP-galactopyranose mutase (UGM) and have activity to attenuate virulence of pathogenic microorganisms, including mycobacteria.
    Type: Grant
    Filed: April 27, 2009
    Date of Patent: September 25, 2012
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Laura Lee Kiessling, Emily Carla Dykhuizen, John F. May
  • Publication number: 20120238581
    Abstract: Compounds of formula (I), or a pharmaceutically acceptable salt, prodrug, salt of a prodrug, or a combination thereof. Pharmaceutical compositions of formula (I) and related methods for treating or preventing metabolic diseases or conditions.
    Type: Application
    Filed: May 31, 2012
    Publication date: September 20, 2012
    Inventors: Andrew J. Souers, Ju Gao, Todd M. Hasen, Rajesh R. Iyengar, Philip R. Kym, Bo Liu, Zhonghua Pei, Vince S. Yeh, Gang Zhao, Zhili Xin
  • Publication number: 20120238569
    Abstract: 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 inflammatory diseases and disorders such as, for example, asthma and COPD.
    Type: Application
    Filed: February 17, 2012
    Publication date: September 20, 2012
    Inventors: Paul Gillespie, Christophe Michoud, Kenneth Carey Rupert, Kshitij Chhabilbhai Thakkar
  • Patent number: 8257931
    Abstract: A composition and method for inhibiting proliferation of a tumor cell compared to a non-tumor cell. Also described are methods of screening for a composition that inhibits cap-dependent translation compared to cap-independent translation of proteins.
    Type: Grant
    Filed: January 20, 2006
    Date of Patent: September 4, 2012
    Assignee: President and Fellows of Harvard College
    Inventors: Gerhard Wagner, Michael Chorev, Nathan John Moerke, Bertal Huseyin Aktas, José Halperin
  • Publication number: 20120202687
    Abstract: This document discloses molecules having the following formulas (“Formula One” & “Formula Two” and “Formula Three”) The Ar1, Het, Ar2, R1, R2, R3, R4, and R5 are further described herein.
    Type: Application
    Filed: February 6, 2012
    Publication date: August 9, 2012
    Inventors: Gary D. Crouse, Thomas C. Sparks, William H. Dent, III, CaSandra L. McLeod, Lawrence C. Creemer, David A. Demeter, Amanda E. Fritz, Lindsey G. Fischer, Erich W. Baum
  • Patent number: 8236835
    Abstract: The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.
    Type: Grant
    Filed: September 19, 2007
    Date of Patent: August 7, 2012
    Assignees: Novartis AG, Xenon Pharmaceuticals Inc.
    Inventors: Natalie Dales, Zaihui Zhang, Rajender Kamboj, Jianmin Fu, Shaoyi Sun, Natalia Pokrovskaia, Serguei Sviridov
  • Publication number: 20120196861
    Abstract: The present invention relates to compounds of the general formula (I), and the pharmaceutically acceptable salt or solvate thereof, as anti-inflammatory and immunomodulatory agents.
    Type: Application
    Filed: January 27, 2012
    Publication date: August 2, 2012
    Applicant: 4SC Discovery GmbH
    Inventors: Johann LEBAN, Stefan TASLER, Roland BAUMGARTNER, Wael SAEB, Carine CHEVRIER
  • Publication number: 20120196866
    Abstract: The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
    Type: Application
    Filed: April 6, 2012
    Publication date: August 2, 2012
    Applicant: UCB PHARMA, S.A.
    Inventors: Benoît Kenda, Yannick Quesnel, Ali Ates, Philippe Michel, Laurent Turet, Joël Mercier
  • Publication number: 20120178713
    Abstract: The present invention relates to phenyl sulfonamides useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including for example the treatment of pain.
    Type: Application
    Filed: March 14, 2012
    Publication date: July 12, 2012
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Esther Martinborough, Lev T.D. Fanning, Urvi Sheth, Dean Wilson, Andreas P. Termin, Timothy D. Neubert, Nicole Hilgraf, Tara Leanne Hampton, Tara Whitney, Aarti Sameer Kawatkar, Danielle Lehsten, Dean Stamos, Jinglan Zhou, Vijayalaksmi Arumugam, Corey Anderson
  • Patent number: 8211924
    Abstract: The present invention relates to 1-(azolin-2-yl)amino-1,2-diphenylethane compounds of the formula I and to their salts which are useful for combating animal pests. The invention also relates to a method for controlling animal pests by using these compounds, to seed and to an agricultural and veterinary composition comprising said compounds. wherein A is a radical of formulae A.1 or A.
    Type: Grant
    Filed: July 2, 2008
    Date of Patent: July 3, 2012
    Assignee: BASF SE
    Inventors: Markus Kordes, Christopher Koradin, Ronan Le Vezouet, Ernst Baumann, Deborah L. Culbertson, Douglas D. Anspaugh, Hassan Oloumi-Sadeghi, Cecille Ebuenga
  • Publication number: 20120157414
    Abstract: The present invention provides novel pyrazolines that are useful as cannabinoid receptor blockers and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, inflammatory disorders, cardiometabolic disorders, hepatic disorders, and/or cancers.
    Type: Application
    Filed: November 18, 2011
    Publication date: June 21, 2012
    Applicant: JENRIN DISCOVERY
    Inventors: John F. McElroy, Robert J. Chorvat
  • Publication number: 20120157457
    Abstract: The present invention provides compositions and methods for inducing neuronal cell differentiation.
    Type: Application
    Filed: January 23, 2012
    Publication date: June 21, 2012
    Applicants: The Salk Institute for Biological Studies, The Scripps Research Institute
    Inventors: Masaki Warashina, Kyung Hoon Min, Fred Gage, Peter G. Schultz, Sheng Ding, Tomoko Kuwabara
  • Publication number: 20120129872
    Abstract: This invention relates to thiazole I and its therapeutic and prophylactic uses, wherein the variables A, Q, J, R1, R3, and R5 are defined in the specification. Disorders treated and/or prevented include rheumatoid arthritis.
    Type: Application
    Filed: November 16, 2011
    Publication date: May 24, 2012
    Inventors: Kristi Anne Leonard, Yan Zhang, Brett Andrew Tounge, Aihua Wang, Michael Hawkins, Paul Francis Jackson, Joseph Kent Barbay, Umar S.M. Maharoof
  • Publication number: 20120129842
    Abstract: This invention relates to bisthiazole I and its therapeutic and prophylactic uses, wherein the variables A, R5, R6, and R7 are defined in the specification. Disorders treated and/or prevented include rheumatoid arthritis.
    Type: Application
    Filed: November 16, 2011
    Publication date: May 24, 2012
    Inventors: Paul Francis JACKSON, Brett Andrew Tounge, Kristi Anne Leonard, Yan Zhang, Aihua Wang, Michael Hawkins, Umar S.M. Maharoof, Joseph Kent Barbay
  • Publication number: 20120129897
    Abstract: This invention relates to thiazole I and its therapeutic and prophylactic uses, wherein the variables A, Q, J, R1, R3, and R5 are defined in the specification. Disorders treated and/or prevented include rheumatoid arthritis.
    Type: Application
    Filed: November 16, 2011
    Publication date: May 24, 2012
    Inventors: Joseph Kent Barbay, Kristi Anne Leonard, Yan Zhang, Brett Andrew Tounge, Aihua Wang, Michael Hawkins, Paul Francis Jackson, Umar S.M. Maharoof
  • Publication number: 20120122862
    Abstract: The present invention is a compound of formula (I) or formula (II) which are suitable as NP-1 antagonists.
    Type: Application
    Filed: January 30, 2012
    Publication date: May 17, 2012
    Inventors: Haiyan Jia, Ian Zachary, Michelle Tickner, Lili Cheng, Chris Chapman, Katie Ellard, Basil Hartzoulakis, Ashley Jarvis, Rosemary Lynch, Jamie Nally, David Selwood, Mark Stewart
  • Publication number: 20120108576
    Abstract: 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: Application
    Filed: November 30, 2011
    Publication date: May 3, 2012
    Applicant: ACHILLION PHARMACEUTICALS, INC.
    Inventors: Suoming Zhang, Avinash Phadke, Cuixian Liu, Xiangzhu Wang, Jesse Quinn, Dawei Chen, Venkat Gadhachanda, Shouming Li, Milind Deshpande
  • Publication number: 20120071524
    Abstract: The present invention relates to novel compounds having anti-cancer activity, methods of making these compounds, and their use for treating cancer and drug-resistant tumors, e.g. melanoma, metastatic melanoma, drug resistant melanoma, prostate cancer and drug resistant prostate cancer.
    Type: Application
    Filed: August 24, 2011
    Publication date: March 22, 2012
    Inventors: Yan Lu, Chien-Ming Li, Zhao Wang, Jianjun Chen, Wei Li, James T. DALTON, Duane D. Miller, Charles Duke, Sunjoo Ahn
  • Patent number: 8138182
    Abstract: The present invention relates to a diketohydrazine derivative of formula (I) and a pharmaceutically acceptable salt thereof (the symbols in the formula have the same meaning as described in the specification). The compound of formula (I) has an inhibitory activity against cysteine protease, and it is useful for the treatment of inflammatory diseases, immune diseases, ischemic diseases, respiratory diseases, circulatory diseases, blood diseases, neuronal diseases, hepatic or biliary diseases, osseous or articular diseases, metabolic diseases, etc. And the compound has inhibitory activity against elastase and it is also useful for the treatment of COPD (chronic obstacle pulmonary diseases).
    Type: Grant
    Filed: September 24, 2009
    Date of Patent: March 20, 2012
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Akira Hatayama, Hiroshi Tsuruta, Yasuo Ochi, Haruo Imawaka, Kazuyuki Ohmoto
  • Publication number: 20120053181
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.
    Type: Application
    Filed: April 28, 2010
    Publication date: March 1, 2012
    Applicant: Merck Sharp & Dohme, Corp.
    Inventors: Peter Lin, Lehua Chang, Scott D. Edmondson
  • Patent number: 8119626
    Abstract: The problem of the present invention is to provide a useful compound as a glucokinase activating agent, which is the oxime derivative of the formula [I]: wherein Ring A is aryl or heteroaryl; Q is cycloalkyl, heterocycle, alkyl or alkenyl; Ring T is heteroaryl or heterocycle; R1 and R2 are independently hydrogen atom, halogen atom, cycloalkylsulfonyl or the like; R3 and R4 are independently hydrogen atom, hydroxy, oxo, halogen atom or the like; R5 is hydrogen atom, halogen atom, cyano, nitro, tetrazolyl or the like; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: November 20, 2008
    Date of Patent: February 21, 2012
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Kazutoshi Sugawara, Tetsuji Matsudaira, Hiroshi Sugama, Masao Nawano, Rikiya Ohashi
  • Publication number: 20120029029
    Abstract: The present invention is directed to substituted thiazol-2-ylamine derivatives and pharmaceutically acceptable salts thereof that inhibit 11?HSD1 and that may be useful in the treatment of diseases in which modulation or inhibition of 11?HSD1 is beneficial or where a reduction in intracellular glucorticoid levels is desirable. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases, disorders, or conditions in which modulation or inhibition of 11?HSD1 is beneficial or where a reduction in intracellular glucorticoid levels is desirable.
    Type: Application
    Filed: July 25, 2011
    Publication date: February 2, 2012
    Applicant: HIGH POINT PHARMACEUTICALS, LLC
    Inventors: Dharma Rao Polisetti, Suparna Gupta
  • Publication number: 20120028981
    Abstract: Provided herein are electrophilically enhanced kinase inhibitors. Also provided herein are methods of making and utilizing the same.
    Type: Application
    Filed: November 5, 2009
    Publication date: February 2, 2012
    Applicant: PRINCIPIA BIOPHARMA INC.
    Inventor: Richard Miller
  • Publication number: 20120015926
    Abstract: This invention relates to compounds of the Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) or a pharmaceutically acceptable salt thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.
    Type: Application
    Filed: November 9, 2009
    Publication date: January 19, 2012
    Inventors: Ling Tong, Brian J. Lavey, Bandarpalle B. Shankar, Seong Heon Kim, Wensheng Yu, Joseph A. Kozlowski, Michael K.C. Wong, Lei Chen, Guowei Zhou, Razia K. Rizvi, Robert Feltz, Aneta Maria Kosinski, De-Yi Yang, Chaoyang Dai, Luke Fire, Vinay Girijavallabhan, Dansu Li, Janeta Popovici-Muller, Judson E. Richard, Kristen E. Rosner, M. Arshad Siddiqui, Liping Yang
  • Patent number: 8080668
    Abstract: The present application provides novel thiazole derivatives that are useful as activators of Adenosine 5?-Monophosphate-Activated Protein Kinase and pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: June 30, 2006
    Date of Patent: December 20, 2011
    Assignees: Dr. Reddy's Laboratories Limited, Dr. Reddy's Laboratories, Inc.
    Inventors: Vijay Kumar Potluri, Saibal Kumar Das, Pradip Kumar Sasmal, Javed Iqbal, Parimal Misra, Ranjan Chakrabarti, Rashmi Talwar
  • Publication number: 20110301143
    Abstract: Heterocyclic compounds of structural formula (I), or a pharmaceutically acceptable salt thereof, wherein W is a R1— substituted heteroaryl, R1 is an heteroaryl ring substituted with an ester or carboxylic acid containing radical, X-T is N—CR5R6, C?CR5 or CR13—CR5R6, Y is a bond or —C(O)—, a and b represent an integer selected from 1 to 4, and Ar is an optionally substituted phenyl or naphtyl, are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD) The heterocyclic compounds are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, atherosclerosis, obesity, diabetes, neurological disease, Metabolic Syndrome, insulin resistance, cancer, liver steatosis, and non-alcoholic steatohepatitis.
    Type: Application
    Filed: February 18, 2010
    Publication date: December 8, 2011
    Inventors: Elise Isabel, Nicolas Lachance, Jean-Philippe Leclerc, Serge Leger, Renata M. Oballa, David Powell, Yeeman K. Ramtohul, Patrick Roy, Geoffrey K. Tranmer, Renee Aspiotis, Lianhai Li, Evelyn Martins
  • Publication number: 20110269748
    Abstract: This invention concerns the use of a compound of formula (I) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein Z is hydrogen, halo, C1-6alkyl, Het1, HO—C1-6alkyl-, cyano-C1-6alkyl-, amino-C(?O)—C1-6alkyl-, formylamino-C1-6alkyl-, C1-6alkyl-C(?O)—NH—C1-6alkyl-, mono- or di(C1-6alkyl)amino-C(?O)—C1-6alkyl-, phenyl-C1-6alkyl-, or Het4-C1-6alkyl-; Q is phenyl, pyridyl, benzofuranyl, 2,3-dihydro-benzofuranyl, pyrazolyl, isoxazolyl or indazolyl wherein each of said ring systems is optionally being substituted with up to three substituents each independently selected from halo, cyano, C1-6alkyl, C1-6alkyl-O—, C1-6alkylthio, Ar or polyhaloC1-6alkyl; L is phenyl, pyridyl, pyrimidazolyl, 8-Azapyrimidazolyl, pyridazinyl, imidazothiazolyl or furanyl wherein each of said ring systems may optionally be substituted with one or two or more substituents, each substituent independently being selected from halo, hydroxy, amino, cyano, C1-6alkyl
    Type: Application
    Filed: February 13, 2008
    Publication date: November 3, 2011
    Inventors: Johannes Wilhelmus John F. Thuring, Gregor James MacDonald, Christopher James Grantham, Theodorus Dinklo, Anne Simone Josephine Lesage
  • Publication number: 20110263556
    Abstract: This invention relates to compounds of formula I, their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions such as inflammatory/nociceptive pain. A, M, R1, R2, R7, Ra, Rb, Q3, Q4, Q6, Z2, Z4, Z5, Z6 and W have meanings given in the description.
    Type: Application
    Filed: October 20, 2010
    Publication date: October 27, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Henning PRIEPKE, Henri DOODS, Raimund KUELZER, Roland PFAU, Dirk STENKAMP, Robert ROENN, Benjamin PELCMAN
  • Publication number: 20110245501
    Abstract: The present invention relates to substituted tetracycline compounds and related methods for increasing the antifungal activity of an antifungal agent. The methods include administering to a subject an effective amount of a substituted tetracycline compound in combination with an antifungal agent such that the subject is treated for the fungal associated disorder.
    Type: Application
    Filed: June 14, 2011
    Publication date: October 6, 2011
    Applicant: Paratek Pharmaceuticals, Inc.
    Inventors: Michael Draper, Mark L. Nelson
  • Patent number: 8026364
    Abstract: A compound having the general structure shown in Formula I: or pharmaceutically acceptable salt and/or solvates thereof are useful in treating diseases or conditions mediated by NK1 receptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.
    Type: Grant
    Filed: March 30, 2010
    Date of Patent: September 27, 2011
    Assignee: OPKO Health, Inc.
    Inventors: Sapna S. Shah, Anandan Palani, Xianhai Huang, Dong Xiao, Sunil Paliwal, Hon-Chung Tsui, Michelle Laci Wrobleski, Ashwin U. Rao, Cheng Wang, Neng-Yang Shih
  • Publication number: 20110224269
    Abstract: The invention relates to compounds, compositions, and methods for diminishing pain in a subject in need thereof comprising administering the compounds and compositions herein described.
    Type: Application
    Filed: March 8, 2011
    Publication date: September 15, 2011
    Inventors: James C. Mannion, Scott L. Dax