The Additional Hetero Ring Contains Chalcogen As The Only Ring Hetero Atom Patents (Class 548/365.7)
-
Publication number: 20120202816Abstract: The present invention discloses a novel thyroid like compounds of formula (I), wherein R1 R2, R3, R4 and Z are as defined in the specification, method for its preparation, composition containing such compounds and use of such compounds and composition as medicament. Further, compounds of formula (I) has significantly low binding affinity to thyroid receptors and thus considerably devoid of thyrotoxic effects. The invention also relates to the use of the compound of formula (I) for the preparation of a medicament for treating various disease conditions such as obesity, dyslipidemia, metabolic syndrome and co-morbidities associated with metabolic syndrome.Type: ApplicationFiled: January 10, 2012Publication date: August 9, 2012Applicant: Torrent Pharmaceuticals, Ltd.Inventors: Laxmikant Chhipa, Shitalkumar Pukharaj Zambad, Ramesh Gupta, Davinder Tuli, Ashok Kasundra, Siralee Munshi, M. Amir Siddiqui, Subrat Kumar Bhattamisra, C. Dutt, Vijay Chauthaiwale
-
Patent number: 8236824Abstract: Novel heterocyclic compounds of the formula I in which R1, R2, R3, R4, R5, R6, R7, Alk and D have the meanings indicated in claim 1, are activators of glucokinase and can be used for the prevention and/or treatment of Diabetes Typ 1 and 2, obesity, neuropathy and/or nephropathy.Type: GrantFiled: September 9, 2008Date of Patent: August 7, 2012Assignee: Merck Patent Gesellschaft mit Beschränkter HaftungInventors: Lars Thore Burgdorf, Norbert Beier, Johannes Gleitz, Ulrich Emde, Christine Charon, Denis Carniato
-
Publication number: 20120196884Abstract: The present invention relates to sulphonamide derivatives, whith a urea moiety. The invention also relates to the use of the derivatives as inhibitors of collagen receptor integrins, especially ?2?1 integrin inhibitors e.g. in connection with diseases and medical conditions that involve the action of cells and platelets expressing collagen receptors, their use as a medicament, e.g. for the treatment of thrombosis, inflammation, cancer and vascular diseases, pharmaceutical compositions containing them and a process for preparing them. The sulphonamide derivatives have the general formula (I) or (I?).Type: ApplicationFiled: June 14, 2010Publication date: August 2, 2012Applicant: BIOTIE THERAPIES CORPORATIONInventors: Jarkko Tapani Koivunen, Jani Korhonen, Anne Marjamäki, Liisa Nissinen, Marjo Pihlavisto, Olli Taneli Pentikäinen
-
Patent number: 8232269Abstract: A compound of Formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein, R1 and R2 each independently represent H, halogen, CF3, C1-3 alkyl or C1-3 alkoxy; R3 represents C1-6 alkyl, C3-6 cycloalkyl, phenyl (optionally substituted by one or more substituents each independently selected from Ra) or Het (optionally substituted by one or more substituents each independently selected from OH, oxo, or C1-4 alkyl); R4 represents H or C1-3 alkyl; R5 represents C1-6 alkyl (optionally substituted by one or more substituents each independently selected from Rb), C3-6 cycloalkyl (optionally substituted by one or more substituents each independently selected from oxo or OH), or Het2 (optionally substituted by one or more substituents each independently selected from Rd); oxygen atom or 1 sulphur atom, or (c) 1 oxygen atom or 1 sulphur atom, (optionally substituted by one or more substituents each independently selected from OH, oxo or C1-4 alkyl); and R6 represents C1-3 alkyl (optionally substituType: GrantFiled: September 17, 2009Date of Patent: July 31, 2012Assignee: Pfizer Inc.Inventors: Karl Richard Gibson, Martin Peter Green, Toby James Underwood, Florian Wakenhut
-
Patent number: 8227620Abstract: Pyrazole derivatives of the following formula (I), having affinity for the cannabinoidergic CB1 and/or CB2 receptors: wherein: R is a group selected from C1-C10 alkyl; aryl, arylalkyl or arylalkenyl, not substituted or having from one to four substituents, equal to or different from each other; A is a group selected from the following: an ether group of formula —(CH2)—O—(CH2)v—R? wherein v is equal to 1 or 2; R? is as defined in the present application; a ketone group of formula —C(O)—Z?, wherein Z? is as defined in the present application; a substituent having an hydroxyl function of formula —CH(OH)—Z?, being as defined in the present application; an amide substituent of formula —C(O)—NH-T?, T? being as defined in the present application; B is a group as defined in the present application; D is an heteroaryl optionally substituted.Type: GrantFiled: December 22, 2009Date of Patent: July 24, 2012Assignee: Neuroscienze Pharmaness S.C. A.R.L.Inventors: Paolo Lazzari, Stefania Ruiu, Gerard Aime Pinna, Gabriele Murineddu
-
Publication number: 20120178780Abstract: Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.Type: ApplicationFiled: March 19, 2012Publication date: July 12, 2012Inventors: Jill E. WOOD, Hanno Wild, Daniel H. Rogers, John Lyons, Michael Katz, Yolanda Caringal, Robert Dally, Wendy Lee, Roger A. Smith, Cheri Blum
-
Publication number: 20120164102Abstract: The pharmaceutically acceptable salts of bicycle-substituted pyrazolon azo derivatives represented by the general formula (I), their preparation methods, pharmaceutical compositions containing the same and their use as a therapeutic agent, especially as thrombopoietin (TPO) mimetics and their use as agonists of thrombopoietin receptor. The definitions of substituents in the general formula (I) are the same as the description.Type: ApplicationFiled: May 28, 2010Publication date: June 28, 2012Inventors: Peng Cho Tang, Hejun Lü, Hongbo Fei, Yiqian Chen
-
Patent number: 8202894Abstract: Compounds of the formula (I) in which the substituents are as defined in claim 1 are suitable for use as microbiocides.Type: GrantFiled: June 30, 2008Date of Patent: June 19, 2012Assignee: Syngenta Crop Protection LLCInventors: Harald Walter, Daniel Stierli, Hans Tobler
-
Publication number: 20120130085Abstract: The invention provides a process for the preparation of a compound of formula (I) in particular, wherein a compound of formula (II) is reacted with a dialkylsulphate. R1 is C1-C4haloalkyl; R2 is optionally substituted alkyl, optionally substituted aryl or optionally substituted heteroaryl; and R3 is methyl or ethyl.Type: ApplicationFiled: July 27, 2010Publication date: May 24, 2012Applicant: SYNGENTA CROP PROTECTION, LLCInventors: Linhua Wang, Jefferson Thomas Ebert
-
Publication number: 20120115893Abstract: Substituted bicyclic carboxamide and urea compounds corresponding to formula (I) processes for the preparation thereof, pharmaceutical compositions containing these compounds, and a method of using these compounds for the treatment and/or inhibition of pain and other conditions mediated at least in part via the vanilloid receptor 1.Type: ApplicationFiled: November 9, 2011Publication date: May 10, 2012Applicant: Gruenenthal GmbHInventors: Robert FRANK, Thomas CHRISTOPH, Sven FRORMANN
-
Publication number: 20120114535Abstract: Provided are an RNase activity inhibitory compound to effectively control the activity of the RNase promoting degradation of extracted RNAs and, in addition, a sample storage container including the same. The RNase activity inhibitory compound and the sample storage container according to the present invention may be effectively used to store RNAs during RNA extraction or the extracted RNAs.Type: ApplicationFiled: June 12, 2009Publication date: May 10, 2012Applicant: BIONEER CORPORATIONInventors: Jong Hoon Kim, Hwangseo Park, Han Oh Park
-
Publication number: 20120108505Abstract: The present invention relates to compounds of the general formula (I): wherein R1, R2, R3, R5, s, and Z are selected independently of each other and are as defined herein, to compositions comprising the compounds, and methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.Type: ApplicationFiled: June 10, 2010Publication date: May 3, 2012Inventors: Eric J. Gilbert, Michael W. Miller, Andrew W. Stamford, William J. Greenlee
-
Patent number: 8143288Abstract: Compounds having the structure of formula I are described. The compounds can inhibit hepatitis C virus (HCV) replication, and in particular can inhibit the function of the HCV NS5A protein.Type: GrantFiled: June 5, 2006Date of Patent: March 27, 2012Assignee: Bristol-Myers Squibb CompanyInventors: Michael Serrano-Wu, Makonen Belema, Lawrence B. Snyder, Nicholas A. Meanwell, Denis R. St. Laurent, Ramesh Kakarla, Van N. Nguyen, Yuping Qiu, Xuejie Yang, John E. Leet, Min Gao, Donald R. O'Boyle, II, Julie A. Lemm, Fukang Yang
-
Publication number: 20120071516Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: September 22, 2011Publication date: March 22, 2012Applicant: CalciMedica, Inc.Inventors: Jianguo Cao, Jeffrey P. Whitten, Yazhong Pei, Zhijun Wang, Evan Rogers, Jonathan Grey
-
Publication number: 20120065407Abstract: The present invention relates to improvements in processes towards the production 3-difluoromethyl-1-methyl-1H-pyrazole-4-carboxylic acid, which is a useful intermediate in fungicide production. In particular, the invention relates to a process for treating a compound of formula III, wherein R1 is C1-C6 alkyl and R2 is CF3, CF2H or CFH2, comprising the steps of a) contacting a compound of formula III with base, and b) separating the compound of formula III and the base.Type: ApplicationFiled: April 20, 2010Publication date: March 15, 2012Applicant: SYNGENTA CROP PROTECTION, LLCInventors: Graham McDougald, James Peter Muxworthy, Beverley Ann Wilde
-
Publication number: 20120053200Abstract: The present invention relates to N-1-Benzyl-2-hydroxy-3-(hetero)arylamino-propyl)-isophthalamides of formula I having BACE2 inhibitory activity and their use as therapeutically active substances, their manufacture and pharmaceutical compositions. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. type 2 diabetes.Type: ApplicationFiled: August 23, 2011Publication date: March 1, 2012Inventors: Harald Mauser, Matthias Nettekoven, Sébastien Schmitt
-
Publication number: 20120046280Abstract: Disclosed are biologically active hetero pyrrole analogs such as imidazoles, thiazoles, oxazoles and pyrazoles capable of interacting with the CB1 and/or CB2 cannabinoid receptors. Aspects disclose hetero pyrrole analogs acting as CB1 and/or CB 1 receptor antagonists, having selectivity for the CB 1 or CB2 receptor, acting as neutral antagonists, acting preferentially on CB 1 receptors located in the peripheral nervous system, and/or acting as nitric oxide donors. Pharmaceutical preparations employing the disclosed analogs and methods of administering therapeutically effective amounts of the disclosed analogs to provide a physiological effect are also disclosed.Type: ApplicationFiled: February 19, 2009Publication date: February 23, 2012Inventors: Alexandros Makriyannis, Venkata K. Vemuri, Teresa Olszewska
-
Patent number: 8119624Abstract: The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein: Ring A is (4-12)-membered heterocyclyl; Ring B is a fused benzene ring selected from the group consisting of: Ring A, ring B, ring C, R1, R1a, R2, R3, R4, L2, n, t, w, and z are as defined in the specification. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a condition that is mediated by the modulation of glucokinase, the method comprising administering to a mammal an effective amount of a compound of formula (I).Type: GrantFiled: October 27, 2010Date of Patent: February 21, 2012Assignee: Pfizer Inc.Inventors: Hao Bai, Simon Bailey, Dilip Ramakant Bhumralkar, Feng C. Bi, Fengli Guo, Mingying He, Paul Stuart Humphries, Anthony Lai Ling, Jihong Lou, Seiji Nukui, Ru Zhou
-
Publication number: 20120021903Abstract: A description is given of 4-(4-haloalkyl-3-thiobenzoyl)pyrazoles of the formula (I) and of their use as herbicides. In this formula (I), X, Y, R1, R2, R3, and R4 are radicals such as hydrogen and organic radicals such as alkyl.Type: ApplicationFiled: July 20, 2011Publication date: January 26, 2012Applicant: BAYER CROPSCIENCE AGInventors: HARTMUT AHRENS, ELMAR GATZWEILER, ISOLDE HÄEUSER-HAHN, CHRISTOPHER HUGH ROSINGER
-
Patent number: 8097732Abstract: Disclosed are compounds of formula (I) or pesticidally acceptable salts thereof, wherein, for example, W is ?N—, ?CH—, ?CR7— or ?C(NR8R9)—, R7 is halogen, R8 and R9 are independently of one another hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocyclyl, aralkyl or heterocyclylalkyl, R1 is cyano, halogen, haloalkyl or CS NH2, R2 is alkyl or cycloalkyl, R3 is hydrogen, alkyl or cycloalkyl, R4 is hydrogen, alkyl or cycloalkyl, R5 is haloalkyl, haloalkoxy, halogen or —SF5, R6 is hydrogen, halogen, haloalkyl, nitro or NR16R17, R16 and R17 are independently of one another hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocyclyl, aralkyl or heterocyclylalkyl, X is —S—, —SO—, or —SO2—, Y is —O—, —S—, —SO—, or SO2—, Z is hydrogen, halogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocyclyl, aralkyl, heterocyclylalkyl or NR18R19, and R18 and R19 are hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocyclyl, aralkyl, heterocyclylalkyl.Type: GrantFiled: June 18, 2007Date of Patent: January 17, 2012Assignee: Merial LimitedInventors: David T. Chou, Michael Maier, Friederike Petry, Werner Knauf
-
Publication number: 20120010249Abstract: The present invention relates to novel anthranilic diamide derivatives of the general formula (I) in which R1, R2, R3, R4, R5, R6, A, Q and n have the meanings given in the description, to their use as insecticides and acaricides for controlling animal pests, also in combination with other agents for activity boosting, and a plurality of processes for their preparation.Type: ApplicationFiled: June 14, 2011Publication date: January 12, 2012Applicant: BAYER CROPSCIENCE AGInventors: Rüdiger FISCHER, Christoph GRONDAL, Markus HEIL, Heinz-Juergen WROBLOWSKY, Ernst Rudolf GESING, Arnd VOERSTE, Ulrich GÖRGENS
-
Patent number: 8093282Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof, are disclosed, wherein J1, U1, U2, B, Y, and A are as described. Methods, compositions, and medicaments related thereto are also disclosed.Type: GrantFiled: May 1, 2009Date of Patent: January 10, 2012Assignee: Allergan, Inc.Inventors: David W. Old, Danny T. Dinh
-
Publication number: 20110319438Abstract: The invention is concerned with novel sulfonamide derivatives of formula (I) wherein R2, R3, R4, A, X, Y1, Y2, Y3, Y4 and Z1 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.Type: ApplicationFiled: September 7, 2011Publication date: December 29, 2011Inventors: Konrad Bleicher, Simona Maria Ceccarelli, Odile Chomienne, Patrizio Mattei, Tanja Schulz-Gasch, Christoph Martin Stahl
-
Patent number: 8084451Abstract: Disclosed are biologically active hetero pyrrole analogs such as imidazoles, thiazoles, oxazoles and pyrazoles capable of interacting with the CB1 and/or the CB2 cannabinoid receptors. One aspect discloses hetero pyrrole analogs acting as antagonists for the CB1 and/or the CB2 receptors. Another aspect discloses hetero pyrrole analogs having selectivity for the CB1 or CB2 cannabinoid receptor. Also disclosed are pharmaceutical preparations employing the disclosed analogs and methods of administering therapeutically effective amounts of the disclosed analogs to provide a physiological effect.Type: GrantFiled: January 10, 2006Date of Patent: December 27, 2011Assignee: University of ConnecticutInventors: Alexandros Makriyannis, Venkata Kiran Rao Vemuri, Teresa Olszewska
-
Publication number: 20110312964Abstract: Compounds of the formula I wherein R1a is H; and R1b is C1-C6 alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and R2b are H, halo, C1-C4alkyl, C1-C4haloalkyl, C1-C4alkoxy; or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a branched C5-C10alkyl chain, C2-C4haloalkyl or C3-C7cycloalkylmethyl, R4 is Het, Carbocyclyl, optionally substituted as defined in the specification and pharmaceutically acceptable salts, hydrates and N-oxides thereof; are inhibitors of cathepsin S and have utility in the treatment of psoriasis, autoimmune disorders and other disorders such as asthma, arteriosclerosis, COPD and chronic painType: ApplicationFiled: December 18, 2009Publication date: December 22, 2011Applicant: Medivir UK LTDInventors: Susana Ayesa, Anna Karin Belfrage, Björn Classon, Urszula Grabowska, Ellen Hewitt, Vladimir Ivanov, Daniel Jönsson, Pia Kahnberg, Peter Lind, Magnus Nilsson, Lourdes Odén, Mikael Pelcman, Horst Wähling
-
Patent number: 8071782Abstract: This invention concerns the synthesis of highly substituted pyrazoles, which are structural components of pharmacological compounds, through reaction of hydrazones with nitroolefins.Type: GrantFiled: October 2, 2008Date of Patent: December 6, 2011Assignee: Janssen Pharmaceutica NVInventors: Xiaohu Deng, Neelakandha S. Mani
-
Publication number: 20110288142Abstract: An improved AKT inhibiting compound, crystalline N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide hydrochloride.Type: ApplicationFiled: January 28, 2010Publication date: November 24, 2011Inventors: Pingyun Y. Chen, Jeffrey Gaulding
-
Publication number: 20110282070Abstract: A benzoylpyrazole compound represented by the formula (I) or its salt: wherein R1 is alkyl or cycloalkyl, R2 is a hydrogen atom or alkyl, R3 is alkyl; cycloalkyl; haloalkyl; alkoxyalkyl; alkoxycarbonylalkyl; alkenyl; or arylalkyl which may be substituted by R8, R4 is alkyl; haloalkyl; alkoxy; halogen; nitro; cyano; alkylthio; alkylsulfinyl; or alkylsulfonyl, R5 is a hydrogen atom; alkyl; alkenyl; alkynyl; halogen; cyano; cyanoalkyl; cyanoalkeny; haloalkyl; alkoxyalkyl; haloalkoxyalkyl; amino(thiocarbonyl)alkyl which may be substituted by at least one substituent selected from alkyl, cyano, is cyanoalkyl, (alkylthio)carbonylalkyl, alkyl(thiocarbonyl)alkyl, —C(O)OR7 and —C(O)SR7; thiocyanatoalkyl; alkoxy; alkenyloxy; alkynyloxy; haloalkoxy; alkoxyalkoxy; haloalkoxyalkoxy; alkoxyhaloalkoxy; haloalkoxyhaloalkoxy; alkoxyalkoxyalkyl; alkylthio; alkoxyalkylthio; haloalkoxyalkylthio; alkoxyhaloalkylthio; haloalkoxyhaloalkylthio; alkylthioalkylthio; haloalkylthioalkylthio; alkylthiohaloalkylthio; haloalkylthiohaloType: ApplicationFiled: July 21, 2011Publication date: November 17, 2011Applicant: ISHIHARA SANGYO KAISHA, LTD.Inventors: Hiroshi SHIMOHARADA, Masamitsu Tsukamoto, Masahiko Ikeguchi, Hiroshi Kikugawa, Makiko Sano, Yoshinori Kitahara, Hidemasa Kominami, Tatsuya Okita
-
Publication number: 20110281924Abstract: Compounds of formula (I), in which the substituents are as defined in claim 1, are suitable for use as microbiocides.Type: ApplicationFiled: January 14, 2010Publication date: November 17, 2011Applicant: SYNGENTA CROP PROTECTION LLCInventors: Harald Walter, Daniel Stierli
-
Publication number: 20110257014Abstract: The invention provides compounds of the formula (I) and salts thereof which are described herein. The compounds (I) or salts thereof are suitable for use as herbicides and plant growth regulators, in particular as herbicides for the selective control of harmful plants in crops of useful plants, and can be prepared by the described processes.Type: ApplicationFiled: December 14, 2010Publication date: October 20, 2011Applicant: BAYER CROPSCIENCE AGInventors: Harald Jakobi, Arianna Martelletti, Jan Dittgen, Dieter Feucht, Isolde H?user-Hahn, Christopher Hugh Rosinger
-
Publication number: 20110257379Abstract: A system for screening a small molecule library with 250,000 molecules to find out a compound of an anti-hypertensive drug aiming at human Angiotensin II type IA receptor is provided. The system includes a first database having a three-dimensional structure datum of a human Angiotensin II type IA receptor, a second database having molecular data of a plurality of small molecules, and a computer acquiring the three-dimensional structure datum and the molecular data from the first database and the second database respectively, wherein the computer has a molecular docking software for calculating a free energy of the human Angiotensin II type IA receptor bound to each of the plurality of small molecules, ranks the plurality of small molecules according to the respective free energy so as to select a top small molecule in the ranking as the compound of the drug.Type: ApplicationFiled: June 27, 2011Publication date: October 20, 2011Inventor: Hsin-Hsien Wu
-
Patent number: 8022093Abstract: New polymorphs of Eltrombopag and Eltrombopag ethanolamine salt have been obtained and characterized. These polymorphs and pharmaceutical compositions comprising them are useful, for example, in treating conditions leading to thrombocytopenia.Type: GrantFiled: April 19, 2011Date of Patent: September 20, 2011Assignee: Pliva Hrvatska D.O.O.Inventors: Edislav Leksic, Helena Ceric, Tina Mundorfer, Irena Zrinski Antonac, Zrinka Mastelic Samardzic
-
Publication number: 20110224262Abstract: Pyrazole derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.Type: ApplicationFiled: November 24, 2009Publication date: September 15, 2011Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Thuy-Anh Tran, Jason B. Ibarra, Young-Jun Shin, Brett Ullman, Ning Zou, Xi Zeng
-
Publication number: 20110224202Abstract: Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.Type: ApplicationFiled: March 10, 2011Publication date: September 15, 2011Applicant: Omeros CorporationInventors: Neil S. Cutshall, Jennifer Lynn Gage, Thomas Neil Wheeler, Thomas L. Little
-
Publication number: 20110212860Abstract: The present invention provides compounds and methods for modulation of the quorum sensing of bacteria. In an embodiment, the compounds of the present invention are able to act as replacements for naturally occurring bacterial quorum sensing ligands in a ligand-protein binding system; that is, they imitate the effect of natural ligands and produce an agonistic effect. In another embodiment, the compounds of the present invention are able to act in a manner which disturbs or inhibits the naturally occurring ligand-protein binding system in quorum sensing bacteria; that is, they produce an antagonistic effect. The compounds of the present invention comprise N-acylated-homoserine lactones (AHLs) comprised of a wide range of acyl groups.Type: ApplicationFiled: February 22, 2011Publication date: September 1, 2011Inventors: Helen E. Blackwell, Grant D. Geske, Jennifer C. Campbell
-
Publication number: 20110196009Abstract: Invented are novel heterocyclic carboxamide compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.Type: ApplicationFiled: October 14, 2009Publication date: August 11, 2011Inventors: Meagan Rouse, Mark Andrew Seefeld
-
Publication number: 20110166159Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: March 17, 2011Publication date: July 7, 2011Applicant: CalciMedica, Inc.Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
-
Publication number: 20110160459Abstract: The invention is directed to 5-(hetero)aryl-4,5-dihydro-(1H)-pyrazole (pyrazoline) derivatives as cannabinoid CB1 receptor agonists, to pharmaceutical compositions comprising these compounds, to methods for their syntheses, methods for preparing novel intermediates useful for their syntheses, and methods for preparing compositions. The invention also relates to the uses of such compounds and compositions, administered to patients to achieve a therapeutic effect in disorders in which CB1 receptors are involved, or that can be treated via manipulation of those receptors. Compounds of the present invention include compounds of formula (I): wherein the substituents have the definitions given in the specification.Type: ApplicationFiled: March 8, 2011Publication date: June 30, 2011Inventors: Josephus H.M. LANGE, Hicham ZILAOUT, Bernard J. VAN VLIET
-
Patent number: 7968542Abstract: A compound represented by the formula (I) (wherein R1, R2, R3 and R4 are as defined in the description), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.Type: GrantFiled: July 13, 2006Date of Patent: June 28, 2011Assignee: Nissan Chemical Industries, Ltd.Inventors: Katsuaki Miyaji, Kazufumi Yanagihara, Yukihiro Shigeta, Shunsuke Iwamoto, Masato Horikawa, Yutaka Hirokawa, Shingo Owada, Satoshi Nakano, Hirofumi Ota, Norihisa Ishiwata
-
Publication number: 20110144345Abstract: The benzoyl derivative of the present invention is represented by formula (I) (in the formula, E represents an alkoxy group, an alkoxycarbonyl group or the like, R1 represents a halogen atom, an organic group or the like, p represents an integer of 0 to 3, R2 and R3 each independently represents an alkyl group or the like, Q represents a group selected from the groups represented by the following formulas Q1 to Q8: (in the formula, * represents binding site, G represents oxygen atom or the like), R4 to R5, R8 to R13 represents hydrogen atom, an alkyl group or the like), R6 represents cyano group or the like, X represents —C(R12)(R13)— or —N(R12)—, Y represents oxo group, an alkyl group or the like, m represents an integer of 0 to 4)) or salt thereof.Type: ApplicationFiled: August 3, 2009Publication date: June 16, 2011Applicant: NIPPON SODA CO., LTD.Inventors: Tetsuo Tamai, Kazuaki Tsukuda, Shigeo Yamada, Yasuhiro Miyashita, Shingo Hirai
-
Patent number: 7960425Abstract: A compound represented by the formula (I) (wherein R1, R2, R3 and R4 are as defined in the description), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.Type: GrantFiled: July 19, 2006Date of Patent: June 14, 2011Assignee: Nissan Chemical Industries, Ltd.Inventors: Katsuaki Miyaji, Yutaka Hirokawa, Masato Horikawa, Norihisa Ishiwata
-
Publication number: 20110130381Abstract: Inhibitors of dihydroorotate dehydrogenase (DHODH) for the Plasmodium enzyme have been identified and characterized. The inhibitors have high specificity, submicromolar efficacy against cultured parasite strains, exhibit drug-like properties, and are not overtly cytotoxic.Type: ApplicationFiled: May 7, 2009Publication date: June 2, 2011Inventors: Cecilia Bastos, Michael L. Booker, Cassandra A. Celatka, Jon C. Clardy, Joseph Cortese, Vishal P. Patel, Renato Skerlj, Roger C. Wiegand, Dyann F. Wirth
-
Publication number: 20110130431Abstract: 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: ApplicationFiled: February 8, 2011Publication date: June 2, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Angela BERRY, Pier Francesco CIRILLO, Eugene Richard HICKEY, Doris RIETHER, David THOMSON, Renee M. ZINDELL, Nigel BLUMIRE, Chandana CHOWDHURY, Monika ERMANN, James Edward JENKINS, Innocent MUSHI, Christopher Francis PALMER, Malcolm TAYLOR
-
Publication number: 20110112073Abstract: The present invention relates to HSF activating compounds, methods for their discovery, and their research and therapeutic uses, as well as pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, mixtures (including both R and S enantiomeric forms and racemic mixtures thereof), and pharmaceutical Formulations thereof. In particular, the present invention provides compounds capable of facilitating HSF1 homotrimerization, and methods of using such compounds as therapeutic agents to treat a number of conditions associated with irregular HSF1 activity.Type: ApplicationFiled: November 12, 2010Publication date: May 12, 2011Applicant: DUKE UNIVERSITYInventors: Dennis J. Thiele, Daniel W. Neef, Jose S. Mendoza
-
Publication number: 20110104162Abstract: The present invention relates to a compound of general formula (I): and also to the pharmaceutically acceptable salts thereof, to the isomers or isomer mixtures thereof in all proportions, in particular to an enantiomer mixture, and especially to a racemic mixture. The present invention also relates to the use of these compounds as a medicament, and in particular for the treatment of cancer, and also to the compositions containing them.Type: ApplicationFiled: June 15, 2009Publication date: May 5, 2011Applicant: Cytomics SystemsInventors: Denis Carniato, Karine Jaillardon, Olivier Busnel, Mathieu Gutmann, Jean-Francois Briand, Benoit Deprez, Dominique Thomas, Cécile Bougeret
-
Patent number: 7932283Abstract: The present invention relates to N-cyclopropyl-sulfonylamide derivatives of formula (I) wherein the substituents are cyclic groups, 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:Type: GrantFiled: April 5, 2007Date of Patent: April 26, 2011Assignee: Bayer Cropscience AGInventors: Hans-Georg Schwarz, Sandra Gassmann, Karl-Heinz Kuck, Peter Dahmen, Ulrike Wachendorff-Neumann, Stéphane Carbonne, Stéphanie Gary, Christopher Steele, Alain Villier, Jean-Pierre Vors
-
Publication number: 20110092496Abstract: A compound represented by the formula (I) (wherein R1, R2, R3 and R4 are as defined in the description), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.Type: ApplicationFiled: November 29, 2010Publication date: April 21, 2011Applicant: Nissan Chemical Industries, Ltd.Inventors: Katsuaki MIYAJI, Kazufumi Yanagihara, Yukihiro Shigeta, Shunsuke Iwamoto, Masato Horikawa, Yutaka Hirokawa, Shingo Owada, Satoshi Nakano, Hirofumi Ota, Norihisa Ishiwata
-
Publication number: 20110092539Abstract: The present invention relates to a heterocyclic derivative according to formula (I); wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of psychiatric diseases where an enhancement of synaptic responses mediated by AMPA receptors is required, including schizophrenia, depression and Alzheimer's disease.Type: ApplicationFiled: June 3, 2009Publication date: April 21, 2011Inventors: Jonathan Gillespie, Craig Jamieson, Zoran Rankovic
-
Publication number: 20110077409Abstract: Cyano-substituted sulfilimines are produced efficiently and in high yield from the corresponding sulfides by reaction with cyanamide and hypochlorite.Type: ApplicationFiled: November 18, 2010Publication date: March 31, 2011Inventors: David E. Podhorez, Ronald Ross, JR., James R. McConnell
-
Publication number: 20110071182Abstract: Invented are novel heterocyclic carboxamide compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.Type: ApplicationFiled: December 23, 2008Publication date: March 24, 2011Inventors: Mark A. Seefeld, Meagan B. Rouse, Dirk A. Heerding