The -c(=x)- Group Is Bonded Directly To The Nitrogen Patents (Class 548/195)
-
Publication number: 20130059896Abstract: Inhibitors of LIM kinase 2 are disclosed, along with pharmaceutical compositions comprising them and methods of their use.Type: ApplicationFiled: January 21, 2011Publication date: March 7, 2013Inventors: Nicole Cathleen Goodwin, David Brent Rawlins
-
Patent number: 8383657Abstract: The invention relates to novel thiazolylidine urea and amide derivatives that are PAMs of neuronal nicotinic receptors, compositions comprising the same, processes for preparing such compounds, and methods for using such compounds and compositions.Type: GrantFiled: December 18, 2008Date of Patent: February 26, 2013Assignee: Abbott LaboratoriesInventors: Ramin Faghih, Gregory A. Gfesser, Kathleen H. Mortell, Murali Gopalakrishnan
-
Publication number: 20130045982Abstract: Disclosed are benzamide derivatives useful in slowing the expansion of cancer cells including the killing of cancer cells and in the treatment of cancer.Type: ApplicationFiled: December 17, 2010Publication date: February 21, 2013Applicant: THE TRANSLATIONAL GENOMICS RESEARCH INSTITUTEInventors: Tong Wang, Stephen Gately
-
Publication number: 20130039870Abstract: Cosmetic or dermatological preparations having an effective content of one or more thiazoles of the general formulaType: ApplicationFiled: February 21, 2011Publication date: February 14, 2013Applicant: Beiersdorf AGInventors: Ludger Kolbe, Cathrin Scherner
-
Patent number: 8372983Abstract: Provided herein are novel compounds that inhibit ribonucleotide reductase (RR) by binding to RRM2 and interfering with the activity of the RRM1/RRM2 holoenzyme, as well as methods of synthesizing these novel compounds. The compounds may be used to inhibit RR activity and to treat various conditions associated with RRM2 expression, such as for example certain cancer types, mitochondrial diseases, or degenerative diseases.Type: GrantFiled: February 1, 2012Date of Patent: February 12, 2013Assignee: City Of HopeInventors: David Horne, Christopher Lincoln
-
Patent number: 8362267Abstract: Disclosed are a novel thiazole-containing benzophenone derivative represented by formula 1, and an isomer thereof, a pharmaceutically acceptable salt thereof, a hydrate thereof and a solvate thereof, a pharmaceutical composition comprising the derivative, a use of the derivative as therapeutic agent and a method for preparing the derivative. The benzophenone thiazole derivatives inhibit formation of microtubules and eliminate actively proliferating cells of malignant tumors to control general cell proliferation. In formula 1, R, R1 and R2 are defined as above.Type: GrantFiled: March 5, 2009Date of Patent: January 29, 2013Assignee: Chong Kun Dang Pharmaceutical Corp.Inventors: Nam-Song Choi, Young-Hoon Kim, Jae-Kwang Lee, Hee-Ryong Kang, Ho-Jin Choi, Seung-Kee Moon, Soo-Jin Kim, Gyu-Tae Park, Byeong-Hoon Han, Dal-Hyun Kim, Jae-Hoon Choi, Sung-Sook Lee, Soon-Kil Ahn, Kyung-Joo Lee, Su-Yeal Bae
-
Publication number: 20130023463Abstract: A compound of the formula is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.Type: ApplicationFiled: April 19, 2012Publication date: January 24, 2013Applicant: ABBOTT LABORATORIESInventors: Charles A. Flentge, Hui-Ju Chen, David A. DeGoey, William J. Flosi, David J. Grampovnik, Peggy P. Huang, Dale J. Kempf, Larry L. Klein, Allan C. Krueger, Darold L. Madigan, John T. Randolph, Minghua Sun, Ming C. Yeung, Chen Zhao
-
Publication number: 20130012546Abstract: The present invention relates to hydroximoyl-tetrazole derivatives of formula (I), their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions. wherein A represents a tetrazoyl group, Het represents a pyridyl group or a thiazolyl group and X represents various substituents.Type: ApplicationFiled: December 28, 2010Publication date: January 10, 2013Inventors: Christian Beier, Jurgen Benting, David Bernier, Pierre-Yves Coqueron, Philippe Desbordes, Christophe Dubost, Stephanie Gary, Pierre Genix, Daniela Portz, Ulrike Wachendorff-Neumann
-
Patent number: 8349871Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: GrantFiled: September 21, 2011Date of Patent: January 8, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Alessandra Bartolozzi, Angela Berry, Eugene Richard Hickey, Doris Riether, Achim Sauer, David Smith Thomson, Lifen Wu, Renee M. Zindell, Patricia Amouzegh, Nigel James Blumire, Stephen Peter East, Monika Ermann, Someina Khor, Innocent Mushi
-
Patent number: 8344153Abstract: The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3K?. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: GrantFiled: June 9, 2010Date of Patent: January 1, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Kevin Michael Cottrell, Alex Aronov, Robert J. Davies, Jon H. Come, David Messersmith, Jinwang Xu, Upul Keerthi Bandarage, Jingrong Cao
-
Patent number: 8338467Abstract: Disclosed herein are compounds of formula (I) wherein R1, R2, R3, R25a, R26a, X, and n are as defined in the specification. Pharmaceutical compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and pharmaceutical compositions are also described.Type: GrantFiled: September 26, 2011Date of Patent: December 25, 2012Assignee: AbbVie Inc.Inventors: Teodozyj Kolasa, Jennifer M. Frost, Meena V. Patel, Steven P. Latshaw, Arturo Perez-Medrano, Xueqing Wang, Karin Rose Marie Tietje, Sridhar Peddi, William A. Carroll
-
Publication number: 20120316124Abstract: The present invention relates to compounds formula (I), wherein P is P1, P2, heterocyclyl or heterocyclyl substituted by one to five Z; and wherein A1, A2, A3, A4, G1, R1, R2, R3, R4, R5, R6, R17, R18, R19 and R20 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.Type: ApplicationFiled: February 17, 2011Publication date: December 13, 2012Applicant: SYNGENTA CROP PROTECTION LLCInventors: Thomas Pitterna, Myriem El Qacemi, Jerome Yves Cassayre, Peter Renold, Vladimir Bobosik
-
Publication number: 20120309972Abstract: There are provided a tetrazolyloxime derivative, a salt thereof, and a fungicide, that have excellent control effects against plant diseases. The fungicide contains, as an active ingredient, at least one selected from the group consisting of tetrazolyloxime derivatives represented by formula (6) and salts thereof. In formula (6), X represents a halogen atom, A represents a tetrazolyl group, R represents a halogen atom or the like, D represents a single bond or an oxygen atom, E represents a single bond or an alkylene chain, R2a and R2b each independently represents an alkoxy group or the like, and R3 represents a hydrogen atom or an alkyl group.Type: ApplicationFiled: February 14, 2011Publication date: December 6, 2012Applicant: NIPPON SODA CO., LTD.Inventors: Syuichi Ito, Ichirou Urihara, Hazumi Nomura, Yukuo Mukohara
-
Publication number: 20120309794Abstract: The present invention concerns compounds, some of which are novel, and their pharmaceutical applications. The compounds of the invention inhibit the enzyme lactate dehydrogenase (LDH) involved both in the metabolic process of hypoxic tumour cells, and in the process used by parasitic protozoa that cause malaria to obtain most of the energy they need.Type: ApplicationFiled: November 5, 2010Publication date: December 6, 2012Applicant: UNIVERSITÀ DI PISAInventors: Filippo Minutolo, Marco Macchia, Carlotta Granchi, Sarabindu Roy, Gino Giannaccini, Antonio Lucacchini
-
Patent number: 8318774Abstract: 3-((Thiazol-2-yl)amino)propylproiolamide compounds of the formula I: wherein the variables are as defined herein, are useful to prevent or treat a disease or disorder involving mGluR5 receptor regulation. Also disclosed are pharmaceutical compositions containing the compounds and methods of making the compounds.Type: GrantFiled: June 26, 2008Date of Patent: November 27, 2012Assignee: Gruenenthal GmbHInventors: Michael Haurand, Klaus Schiene, Sven Kühnert, Melanie Reich
-
Publication number: 20120295938Abstract: The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.Type: ApplicationFiled: March 9, 2012Publication date: November 22, 2012Inventors: BRADLEY TEEGARDEN, DENNIS CHAPMAN, MARC DECAIRE, PETER I. DOSA, KONRAD FEICHTINGER, HONNAPPA JAYAKUMAR, THUY-ANH TRAN, SONJA STRAH-PLEYNET, JAY XU
-
Patent number: 8314247Abstract: A hydrazone derivative of formula [I]: wherein Ring A is aryl or heteroaryl, Ring T is heteroaryl or heterocycle, R1 and R2 are independently hydrogen atom, halogen atom, cycloalkylsulfonyl, etc., R3 and R4 combine each other together with the adjacent nitrogen atom to form substituted or unsubstituted heterocycle, R5 is hydrogen atom, halogen atom, cyano, nitro, tetrazolyl, etc., and R6 is hydrogen atom, etc.; or a pharmaceutically acceptable salt thereof is useful as a glucokinase activation agent.Type: GrantFiled: January 9, 2008Date of Patent: November 20, 2012Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Iwao Takamuro, Kazutoshi Sugawara, Hiroshi Sugama
-
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
-
Publication number: 20120263659Abstract: The invention relates to a TRPM8 modulator for achieving a cooling effect on the skin or a mucous membrane.Type: ApplicationFiled: November 22, 2010Publication date: October 18, 2012Applicants: BASF SE, SYMRISE AGInventors: Thomas Subkowski, Michael Backes, Heiko Oertling, Arnold Machinek, Hubert Loges, Ulrike Simchen, Horst Surburg, Claus Bollschweiler, Jens Wittenberg, Wolfgang Siegel
-
Publication number: 20120258963Abstract: 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: ApplicationFiled: June 20, 2012Publication date: October 11, 2012Inventors: Richard Berger, Lehua Chang, Scott D. Edmondson, Stephen D. Goble, Sookhee Nicole Ha, Nam Fung Kar, Ihor E. Kopka, Bing Li, Gregori J. Morriello, Chris R. Moyes, Dong-Ming Shen, Liping Wang, Cheng Zhu
-
Publication number: 20120253048Abstract: Provided herein are novel compounds that inhibit ribonucleotide reductase (RR) by binding to RRM2 and interfering with the activity of the RRM1/RRM2 holoenzyme, as well as methods of synthesizing these novel compounds. The compounds may be used to inhibit RR activity and to treat various conditions associated with RRM2 expression, such as for example certain cancer types, mitochondrial diseases, or degenerative diseases.Type: ApplicationFiled: February 1, 2012Publication date: October 4, 2012Inventors: Yun Yen, David Horne, Christopher Lincoln
-
Publication number: 20120238569Abstract: 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: ApplicationFiled: February 17, 2012Publication date: September 20, 2012Inventors: Paul Gillespie, Christophe Michoud, Kenneth Carey Rupert, Kshitij Chhabilbhai Thakkar
-
Patent number: 8268818Abstract: The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3K?. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: GrantFiled: September 4, 2007Date of Patent: September 18, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Tiansheng Wang, Jeremy Green, Brian Ledford, François Maltais, Andreas P. Termin, Mark Cornebise, Jonathan Parsons, Adam Tanner, James Westcott
-
Publication number: 20120225887Abstract: 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: ApplicationFiled: April 10, 2012Publication date: September 6, 2012Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Zacharia Cheruvallath, Stephen L. Gwaltney, Andrew John Jennings, Mark Sabat, Jeffrey A. Stafford, Mingnam Tang, Haxia Wang
-
Publication number: 20120214735Abstract: Acetamide derivatives, their stereoisomers, tautomers, prodrugs, pharmaceutically acceptable salts, polymorphs, solvates and formulations thereof for the prophylaxis, management, treatment, control of progression, or adjunct treatment of diseases and/or medical conditions where the activation of glucokinase would be beneficial, are disclosed. The disclosure also provides process of preparation of these acetamide derivatives.Type: ApplicationFiled: February 17, 2012Publication date: August 23, 2012Applicant: Advinus Therapeutics LimitedInventors: Debnath Bhuniya, Anil Deshpande, Sachin Kandalkar, Balasaheb Kobal, Santosh Kurhade, Vinod Vyavahare, Rahul Kaduskar
-
Publication number: 20120214815Abstract: The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: April 6, 2012Publication date: August 23, 2012Applicant: UCB Pharma, S.A.Inventors: Benoît KENDA, Yannick QUESNEL, Ali ATES, Philippe MICHEL, Laurent TURET, Joël MERCIER
-
Patent number: 8236835Abstract: 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: GrantFiled: September 19, 2007Date of Patent: August 7, 2012Assignees: Novartis AG, Xenon Pharmaceuticals Inc.Inventors: Natalie Dales, Zaihui Zhang, Rajender Kamboj, Jianmin Fu, Shaoyi Sun, Natalia Pokrovskaia, Serguei Sviridov
-
Publication number: 20120178765Abstract: The present invention provides an amide derivative having a stilbene or 1,2-diphenylethane moiety within the molecule thereof, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The amide derivative of the present invention activates glucokinase remarkably, and therefore they can be usefully applied for treating glucokinase-mediated diseases, such as hyperglycemia and diabetes.Type: ApplicationFiled: September 17, 2010Publication date: July 12, 2012Applicant: YUHAN CORPORATIONInventors: Won-Hui Yi, Tae-Dong Han, Koo-Yeon Lee, Young-Hwan Kim, Eun-Hye Jung, Dong-Hoon Lee, Yoo-Hoi Park, Kyung-Nan Min, Jae-Gyu Kim, Byung-Kyu Lee
-
Publication number: 20120172374Abstract: Compounds represented by the formula (I) or pharmaceutically acceptable salts thereof: R2—Y—Z-Q-A-R1??Formula (I) wherein R1, R2, Y, Z, Q, and A are as defined. These compounds are inhibitors of tubulin polymerization by binding at colchicines binding site and are useful in the treatment of tumors or mitotic diseases such as cancers, gout, and other conditions associated with abnormal cell proliferation.Type: ApplicationFiled: December 29, 2011Publication date: July 5, 2012Applicant: DEVELOPMENT CENTER FOR BIOTECHNOLOGYInventors: Meng-Hsin Chen, Shih-Hsien Chuang, Yi-Jen Chen, Lien-Hsiang Chang, Tsung-Hui Li, Ching-Hui Chen, Win-Yin Wei
-
Patent number: 8211925Abstract: The present invention relates to N-heteroaryl-benzamides, pharmaceutical compositions comprising the same, and methods of using the same. The N-heteroaryl-benzamides are useful in diseases or medical conditions mediated by glucokinase.Type: GrantFiled: April 27, 2007Date of Patent: July 3, 2012Assignee: TransTech Pharma, Inc.Inventors: Anthony Murray, Jesper Lau, Lone Jeppsen, Per Vedsø, Dharma Rao Polisetti, Bapu Reddy Gaddam, Daniel P. Christen, Kalpathy Chidambareswaran Santhosh, Jeremy T. Cooper, Robert Carl Andrews
-
Publication number: 20120165339Abstract: A cyclopropane derivative represented by the following formula (I) or a pharmaceutically acceptable salt thereof has orexin receptor inhibitory action, and thus, is extremely useful as an agent for preventing or treating sleep disorder or dyssomnia caused by orexin, including insomnia as a typical example: wherein A1, A2 and A3 each independently represent an aryl group, a heterocyclyl group or the like, R1, R2 and R3 each independently represent a hydrogen atom, a C1-6 alkyl group or the like, X represents an oxygen atom or the like, and L represents a bond or the like.Type: ApplicationFiled: December 20, 2011Publication date: June 28, 2012Applicant: EISAI R&D MANAGEMENT CO., LTD.Inventors: Taro Terauchi, Ayumi Takemura, Yuji Kazuta, Fumihiro Ozaki, Takashi Doko, Yu Yoshida, Toshiaki Tanaka, Keiichi Sorimachi, Yoshimitsu Naoe, Carsten Beuckmann
-
Publication number: 20120142666Abstract: Compounds of the formula (I), (II) and (III) 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: June 8, 2010Publication date: June 7, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Eugene Richard Hickey, Doris Riether, David Smith Thomson, Lifen Wu, Renee M. Zindell
-
Publication number: 20120142668Abstract: Disclosed are 4-amino-2-butenamides of Formula (I) having pharmacological activity, pharmaceutical compositions containing them, and methods for the treatment of diseases mediated by the cathepsin C enzyme such as chronic obstructive pulmonary disease.Type: ApplicationFiled: August 11, 2010Publication date: June 7, 2012Inventors: Niall Anderson, Ann M. Bullion, Neysa Nevins, Michael R. Palovich, Steven L. Sollis, Michael D. Wall, Jakob Busch-Petersen, Brian Evans, Huijie Li
-
Publication number: 20120142700Abstract: The present invention relates to heterocyclic compounds of formula (I) which have microbiocidal activity, in particular fungicidal activity, as well as methods of using the compounds of formula (I) to control microbes.Type: ApplicationFiled: August 5, 2010Publication date: June 7, 2012Applicant: SYNGENTA CROP PROTECTION, LLCInventors: Sarah Sulzer-Mosse, Clemens Lamberth, Mathias Stephan Respondex, Laura Quaranta
-
Publication number: 20120142677Abstract: 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: December 15, 2009Publication date: June 7, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Angela Berry, Rajashekhar Betageri, Eugene Richard Hickey, Someina Khok, Doris Riether, Lifen Wu, Renee M. Zindell
-
Publication number: 20120129842Abstract: 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: ApplicationFiled: November 16, 2011Publication date: May 24, 2012Inventors: Paul Francis JACKSON, Brett Andrew Tounge, Kristi Anne Leonard, Yan Zhang, Aihua Wang, Michael Hawkins, Umar S.M. Maharoof, Joseph Kent Barbay
-
Publication number: 20120121727Abstract: 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: January 23, 2012Publication date: May 17, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Kai THEDE, Ingo FLAMME, Felix OEHME, Jens-Kerim ERGÜDEN, Friederike STOLL, Joachim SCHUHMACHER, Hanno WILD, Peter KOLKHOF, Hartmut BECK, Jörg KELDENICH, Metin AKBABA, Mario JESKE
-
Publication number: 20120122939Abstract: A new class of alkylsulfonyl-substituted thiazolide compounds is described. These compounds show strong activity against hepatitis virus.Type: ApplicationFiled: January 19, 2012Publication date: May 17, 2012Inventors: Jean-Francois Rossignol, J. Edward Semple
-
Patent number: 8178689Abstract: The present invention provides novel compounds of formula I, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.Type: GrantFiled: June 9, 2011Date of Patent: May 15, 2012Assignee: Hoffman-La Roche Inc.Inventor: Ramakanth Sarabu
-
Patent number: 8173649Abstract: A compound represented by the following formula (1): (wherein the carbon atom denoted by * is in the R-configuration; R1 and R2 are each independently a hydrogen atom, a halogen atom, an amino group, a hydroxyl group, a hydroxyamino group, a nitro group, a cyano group, a sulfamoyl group, a C1-C6 alkyl group, a C1-C6 alkoxy group, a C1-C6 alkylsulfanyl group, a C1-C6 alkylsulfinyl group or a C1-C6 alkylsulfonyl group; and A is a substituted or unsubstituted heteroaryl group), or a pharmaceutically acceptable salt thereof.Type: GrantFiled: December 21, 2007Date of Patent: May 8, 2012Assignees: Kyorin Pharmaceutical Co., Ltd., Teijin Pharma LimitedInventors: Yasumichi Fukuda, Yoshikazu Asahina, Ayako Nakamura, Kenji Fujita, Tomohiro Ide, Fumiyoshi Kobayashi, Shinji Kobayashi, Kanji Komatsu, Masanori Yamamoto
-
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
-
Publication number: 20120101101Abstract: Provided are an agent for the treatment and/or prophylaxis of a movement disorder, the agent for the treatment and/or prophylaxis wherein the movement disorder is extrapyramidal syndrome, the agent for the treatment and/or prophylaxis wherein the movement disorder is bradykinesia, gait disturbance, dystonia, dyskinesia or tardive dyskinesia, the agent for the treatment and/or prophylaxis wherein the movement disorder is a side effect of L-DOPA and/or dopamine agonist therapy, and the like, each containing a thiazole derivative represented by the formula (I) wherein R1 represents aryl and the like, and R2 represents pyridyl or the like, or a pharmaceutically acceptable salt thereof as an active ingredient.Type: ApplicationFiled: April 28, 2010Publication date: April 26, 2012Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Noriaki Uesaka, Takashi Sawada, Tomoyuki Kanda
-
Publication number: 20120101137Abstract: The object of the present invention is to provide a compound having a glucokinase-activating effect. A pharmaceutical composition comprising a compound represented by the general formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient: wherein X means a nitrogen atom or CR6, wherein R6 means a hydrogen atom or a halogen atom; R1 means a hydrogen atom, a C1-C6 alkyl group, a C1-C6 alkoxy group or a C1-C6 alkylthio group; R2 means a hydrogen atom or a fluorine atom; R3 means a hydrogen atom or a C1-C6 alkyl group; and one of R4 and R5 means a hydrogen atom or a C1-C6 alkyl group, and the other means a C1-C6 alkylenecarboxylic acid, a C1-C6 alkylsulfonyl group, a C1-C6 alkylcarbonyl group, or CONH2.Type: ApplicationFiled: June 26, 2010Publication date: April 26, 2012Applicant: SANWA KAGAKU KENKYUSHO CO., LTD.Inventors: Tokuyuki Yamashita, Kaori Chikamatsu, Naoki Takahashi, Hisakazu Iwai, Masakazu Kogami, Masao Sakairi, Nobuhide Watanabe, Hiroki Fujieda, Daisuke Kataoka, Mitsuhiro Makino, Noriyasu Kato, Toshiyuki Miyazawa, Kazushige Nagai, Nobuyoshi Kasugai, Hiroyo Kataoka, Naoki Hiramatsu, Nobuaki Tsuruta, Yurie Yamada, Mika Miyoshi, Sei Murakami, Izumi Goto, Tohru Izuchi, Kimie Suzuki, Satoko Harada, Martin Lang, Markus Hans-Juergen Seifert, Kristina Kaarina Wolf
-
Publication number: 20120095220Abstract: The invention relates to a continuous method for producing amides of aliphatic carboxylic acids by reacting at least one carbonic acid ester of formula (I) R3—COOR4 (I), wherein R3 represents hydrogen or an optionally substituted aliphatic hydrocarbon group with 1 to 100 carbon atoms and R4 represents a hydrocarbon group with 1 to 30 carbon atoms, or wherein R3 and R4 form an optionally substituted ring with 5, 6 or 7 ring members, with at least one amine of formula (II) HNR1R2 (II), wherein R1 and R2 independently represent hydrogen or a hydrocarbon group with 1 to 100 C atoms, in a reaction tube the longitudinal axis of which extends in the direction of propagation of the microwaves of a monomode microwave applicator, under microwave irradiation to form carboxamide.Type: ApplicationFiled: June 9, 2010Publication date: April 19, 2012Applicant: CLARIANT FINANCE (BVI) LIMITEDInventors: Matthias Krull, Roman Morschhaeuser
-
Patent number: 8158663Abstract: The present invention relates to thiazolidinylidene containing compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, and X are as defined in the specification, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.Type: GrantFiled: December 12, 2007Date of Patent: April 17, 2012Assignee: Abbott LaboratoriesInventors: William A. Carroll, Michael J. Dart, Tongmei Li, Arturo Perez-Medrano, Sridhar Peddi
-
Patent number: 8158825Abstract: The present invention relates to a novel class of modified malonate derivatives. The modified malonate compounds can be used to treat cancer. The modified malonate compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: GrantFiled: June 21, 2006Date of Patent: April 17, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Jonathan Grimm, Paul Harrington, Richard Heidebrecht, Jr., Thomas Miller, Karin Otte, Phieng Siliphaivanh, David Sloman, Matthew Stanton, Kevin Wilson, David Witter, Solomon Kattar, Paul Tempest
-
Patent number: 8148412Abstract: The present invention describes 2,3-di-substituted N-heteroaromatic propionamides, of Formula (I) wherein the substitution at the 3-position is an optionally substituted phenyl ring and the substitution at the 2-position is an alkyl or cycloalkyl group; pharmaceutical compositions comprising the same; and, methods of using the same. The propionamides are glucokinase activators for the treatment of type II diabetes.Type: GrantFiled: December 5, 2005Date of Patent: April 3, 2012Assignee: Novo Nordisk A/SInventors: Lone Jeppesen, Marit Kristiansen
-
Publication number: 20120071513Abstract: The present invention provides novel compounds and pharmaceutical compositions thereof, as well as methods for using the compounds and pharmaceutical compositions for treating tumors. Examples of specific tumor types that the compounds may be used to treat include, but are not limited to sarcomas, melanomas, neuroblastomas, carcinomas (including but not limited to lung, renal cell, ovarian, liver, bladder, and pancreatic carcinomas), and mesotheliomas.Type: ApplicationFiled: November 28, 2011Publication date: March 22, 2012Applicant: COMPASS PHARMACEUTICALS LLCInventors: David Kanne, John Ward, Gary Look, X. Michael Wang, Diva Chan, Tina Lee, Donald R. James, Richard Gless, John Schullek, Charles Vacin
-
Publication number: 20120065247Abstract: Provided herein are compounds and methods for use in preventing or treating a viral infection mediated by a virus comprising an IRES-containing RNA molecule or cancer related to an increase or decrease in IRES-mediated translation of an RNA molecule. Also provided are methods of inhibiting or promoting IRES-mediated translation. Also provided are methods of screening for an agent that inhibits IRES-mediated translation.Type: ApplicationFiled: March 26, 2010Publication date: March 15, 2012Applicants: DiscoveryBiomed, Inc., The UAB Research FoundationInventors: Sunnie R. Thompson, Erik Mills Schwiebert, John H. Streiff
-
Publication number: 20120058893Abstract: Ketosultams and diketopyridines of the formula (I) and use thereof as herbicides are described. In this formula (I), G, X, Y and Z are each radicals such as hydrogen and organic radicals such as alkyl. W represents organic radicals such as alkyl. A represents a heterocycle.Type: ApplicationFiled: August 31, 2011Publication date: March 8, 2012Applicant: BAYER CROPSCIENCE AGInventors: Stefan LEHR, Christian WALDRAFF, Elmar GATZWEILER, Isolde HÄUSER-HAHN, Ines HEINEMANN, Christopher Hugh ROSINGER