1,2,3-thiadiazoles (including Hydrogenated) Patents (Class 548/127)
-
Publication number: 20120178623Abstract: Compounds of formula (I) are suitable for use as herbicides: wherein R is methyl, ethyl, vinyl, ethynyl or cyclopropyl, R1 is hydrogen, C1-C6alkyl, C1-C6haloalkyl, C3-C7cycloalkyl, C1-C6alkoxy, C1-C6haloalkoxy, vinyl, propenyl, ethynyl, propynyl, halogen, or optionally substituted phenyl, R2 is methyl, ethyl, vinyl, ethynyl or methoxy, R3 and R4 are hydrogen or together form a double bond, A is C3-C7cycloalkyl which is unsubstituted or substituted once or twice by C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy, C1-C6alkylcarbonyloxy, C2-C6alkenyl, ?O or ?N—R10, or A is cyclohexyl substituted once, at the 4-position, by one (C3-C6cycloalkyl)methoxy, C3-C6cycloalkyloxy, C2-C5alkenyl-CH2-oxy, or benzyloxy substituent, or A is decahydro-1-naphthyl or decahydro-2-naphthyl, or A is optionally substituted phenyl, and G is hydrogen or an agriculturally acceptable metal, sulfonium, ammonium or a latentiating group.Type: ApplicationFiled: July 15, 2010Publication date: July 12, 2012Applicant: SYNGENTA CROP PROTECTION LLCInventors: Daniel Jason Foley, Stephane André Marie Jeanmart, Adrian Longstaff, Robert William Parsons, Claire Janet Russell, John Benjamin Taylor, Jeffrey Steven Wailes
-
Publication number: 20120135975Abstract: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer's disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia.Type: ApplicationFiled: May 14, 2007Publication date: May 31, 2012Applicant: MERCK & CO., INC.Inventors: Vincent J. Colandrea, William K. Hagmann, Jeffrey J. Hale, Irene E. Whitney
-
Publication number: 20120122886Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted thiadiazolyl, and R2, R3, R4, R5, R6, R7 and R8 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.Type: ApplicationFiled: January 26, 2012Publication date: May 17, 2012Inventors: Li Chen, Lichun Feng, Minmin Yang, Michael Patrick Dillon, Yingjie Lai
-
Publication number: 20120122780Abstract: Described herein are compounds useful in the reduction of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.Type: ApplicationFiled: May 20, 2010Publication date: May 17, 2012Applicant: Ardea Biosciences Inc.Inventors: Martha De La Rosa, Jean-Luc Girardet
-
Publication number: 20120115915Abstract: Compositions and methods for inhibiting translation initiation are provided. Compositions, methods and kits for treating (1) cellular proliferative disorders, (2) non-proliferative, degenerative disorders, (3) viral infections, and/or (4) disorders associated with viral infections, using N,N?-diarylureas and/or N,N?-diarylthiourea compounds are described.Type: ApplicationFiled: May 28, 2010Publication date: May 10, 2012Applicant: President and Fellows of Harvard CollegeInventors: Bertal Huseyin Aktas, José A. Halperin, Michael Chorev
-
Publication number: 20120095040Abstract: The invention relates to compounds of the general formula (I) where: R2 is a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy, or NR8R9 group; m, n, o and p independently are a number from 0 to 3; A is a covalent bond, an oxygen atom, a C1-6-alkylene group or a —O—C1-6-alkylene group in which the end that is an oxygen atom is bonded to the R1 group while the end that is an alkylene group is bonded to the carbon of the bicyclic compound; R1 is an optionally substituted aryl or heteroaryl group; R3 is a hydrogen or fluorine atom or a C1-6-alkyl or trifluoromethyl group; R4 is an optionally substituted 5-membered heterocyclic compound; wherein the compounds can be in the state of a base or an acid addition salt. The invention can be used in therapeutics.Type: ApplicationFiled: May 11, 2010Publication date: April 19, 2012Applicant: SANOFIInventors: Ahmed Abouabdellah, Luc Even, Aude Fayol, Julien Vache, Philippe Yauche
-
Publication number: 20120088747Abstract: Compounds, compositions and methods for treating GHS-R mediated disorders are described herein.Type: ApplicationFiled: October 30, 2009Publication date: April 12, 2012Inventor: Jeffrey O. Saunders
-
Patent number: 8153682Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, G, Y, R1, R2, R3, and R4 are defined herein.Type: GrantFiled: July 18, 2008Date of Patent: April 10, 2012Assignee: Janssen Pharmaceutica, NVInventors: Shawn T. Branum, Raymond W. Colburn, Scott L. Dax, Christopher M. Flores, Michele C. Jetter, Yi Liu, Donald Ludovici, Mark J. Macielag, Jay M. Matthews, James J. McNally, Laura M. Reaney, Ronald K. Russell, Ning Qin, Christopher Teleha, Kenneth M. Wells, Scott C. Youells, Mark A. Youngman
-
Publication number: 20120077806Abstract: Disclosed herein are methods of inhibiting a deubiquitinase (DUB), methods of treating pathogenic infections (e.g., viral, bacterial, and/or parasitic), methods of inhibiting cell proliferation, methods of treating a neurodegenerative disease, methods of treating one or more symptoms of a neurodegenerative disease or a genetic disorder, and compounds.Type: ApplicationFiled: September 23, 2011Publication date: March 29, 2012Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Nicholas J. Donato, Christiane Wobus, Hollis D. Showalter, Moshe Talpaz, Jeffrey W. Perry, Roderick J. Sorenson, Mary X. O'Riordan, Yafei Jin
-
Patent number: 8119643Abstract: Biologically active chemical compounds, namely benzoimidazolyl-pyrazine derivatives and structurally related compounds, are disclosed herein. Such compounds include those represented by structural formula (II): and as described in further detail within. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: GrantFiled: March 20, 2007Date of Patent: February 21, 2012Assignee: Synta Pharmaceuticals Corp.Inventors: Shoujun Chen, Jun Jiang, Junyi Zhang, Yu Xie
-
Patent number: 8119644Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted thiadiazolyl, and R2, R3, R4, R5, R6, R7 and R8 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.Type: GrantFiled: December 12, 2009Date of Patent: February 21, 2012Assignee: Roche Palo Alto LLPInventors: Li Chen, Lichun Feng, Minmin Yang, Michael Patrick Dillon, Yingjie Lai
-
Publication number: 20120040999Abstract: Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: Formula (I); are inhibitors of p38 and are useful in the treatment of inflammation such as in the treatment of asthma, COPD, ARDS, rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis, gouty arthritis and other arthritic conditions; inflamed joints, eczema, psoriasis or other inflammatory skin conditions such as sunburn; inflammatory eye conditions including conjunctivitis; pyresis, pain and other conditions associated with inflammation.Type: ApplicationFiled: April 26, 2010Publication date: February 16, 2012Inventors: Hiroo Koyama, Soumya P. Sahoo, Ginger Xu-Qiang Yang, Daniel J. Miller
-
Publication number: 20120022027Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel semicarbazides, sulfonyl carbazides, ureas and related compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to Arenaviridae (Junin, Machupo, Guanavito, Sabia and Lassa), Filoviridae (ebola and Marburg viruses), Flaviviridae (yellow fever, omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).Type: ApplicationFiled: October 28, 2010Publication date: January 26, 2012Applicant: Siga Technologies Inc.Inventors: Dongcheng Dai, Tove Bolken, Sean M. Amberg, Dennis E. Hruby, Thomas R. Bailey, Jack H. Nunberg, Celestine Johnson Thomas
-
Publication number: 20120015941Abstract: The present invention provides novel amide and sulfonamide substituted heterocyclic urea compounds having useful antibacterial activity. Use of these compounds as pharmaceutical compositions and method of their production are also provided.Type: ApplicationFiled: July 23, 2008Publication date: January 19, 2012Applicant: CRESTONE, INC.Inventors: Joseph Guiles, Thale Jarvis, Sarah Strong, Xicheng Sun, Jian Qiu, John C. Rohloff
-
Publication number: 20120004243Abstract: The invention concerns a compound of the Formula (I), wherein Qa is heteroaryl and is substituted with halogeno; R1 and R2 are hydrogen; and Qb is phenyl or heteroaryl, and Qb may optionally bear 1 or 2 substituents selected from hydroxy, halogeno and (1-6C)alkyl, or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.Type: ApplicationFiled: April 5, 2011Publication date: January 5, 2012Applicant: AstraZeneca ABInventors: Dearg Sutherland Brown, John Graham Cumming, Ian Alun Nash
-
Patent number: 8088927Abstract: The present invention relates to N-cycloalkyl-benzyl-amide derivatives of formula (I) wherein the substituents are as in the description, 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: November 15, 2006Date of Patent: January 3, 2012Assignee: Bayer Cropscience AGInventors: Darren Mansfield, Pierre-Yves Coqueron, Philippe Desbordes, Alain Villier, Marie-Claire Grosjean-Cournoyer, Stéphanie Gary, Stéphane Carbonne, Ralf Dunkel, Arounarith Tuch, Jean-Pierre Vors
-
Publication number: 20110301203Abstract: This invention relates to non-steroidal compounds that are modulators of androgen receptor, and also to the methods for the making and use of such compounds.Type: ApplicationFiled: August 19, 2011Publication date: December 8, 2011Applicant: GLAXOSMITHKLINE LLCInventors: Philip Stewart Turnbull, Rodolfo Cadilla, Andrew Larkin, Huiquiang Zhou, Eugene L. Stewart, Katherine Stetson, Darryl Lynn McDougald, Amarjit Sab Randhawa, John A. Ray
-
Publication number: 20110294829Abstract: The present invention relates to hydroximoyl-heterocycle derivatives of formula (I) wherein T represents a substituted or non-substituted heterocyclyl group, Q represents a carbo or heterocyclic group, A represent a carbo or heterocyclic group or a carbo or hetero-polycylic group, and L1 represents various linking groups, their process of preparation, intermediate compounds for their 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: ApplicationFiled: December 8, 2009Publication date: December 1, 2011Inventors: Christian Beier, Jurgen Benting, David Bernier, Pierre-Yves Coqueron, Philippe Desbordes, Christophe Dubost, Stephanie Gary, Pierre Genix, Daniela Portz, Ulrike Wachendorff-Neumann
-
Patent number: 8063067Abstract: Compounds of the formula (I): in which R, R1, R2 and R3 are as defined in the description, the use thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes, pharmaceutical compositions comprising them, and processes for the preparation of these compounds.Type: GrantFiled: July 23, 2009Date of Patent: November 22, 2011Assignee: Merck Patent GmbHInventors: Jean Jacques Zeiller, Hervè Dumas, Valérie Guyard-Dangremont, Isabelle Berard, Francis Contard, Daniel Guerrier, Gérard Ferrand, Yves Bonhomme
-
Publication number: 20110269960Abstract: An object of the present invention is to provide a compound having an action of inhibiting binding between S1P and its receptor, Edg-1 (S1P1), and is useful as a pharmaceutical compound. A compound or a pharmaceutically acceptable salt thereof, which compound is represented by the formula below (where A represents an oxygen atom, a sulfur atom, a group represented by Formula —SO—, a group represented by Formula —SO2—, or the like, R1 represents a hydrogen atom, an alkyl group having 1-6 carbon atoms, or the like, R1A represents a hydrogen atom or the like, R2 represents an alkyl group having 1-6 carbon atoms, a cycloalkyl group having 3-6 carbon atoms, or the like, R3 represents an aryl group, R4 represents a hydrogen atom or an alkyl group having 1-6 carbon atoms and optionally substituted with a carboxyl group, and R5 represents an alkyl group having 1-10 carbon atoms, a cycloalkyl group having 3-8 carbon atoms, an aryl group which is optionally substituted, or the like).Type: ApplicationFiled: July 11, 2011Publication date: November 3, 2011Applicant: TAISHO PHARMACEUTICAL CO., LTD.Inventors: Naoya ONO, Tetsuo Takayama, Fumiyasu Shiozawa, Hironori Katakai, Tetsuya Yabuuchi, Tomomi Ota, Makoto Yagi, Masakazu Sato
-
Publication number: 20110263863Abstract: The invention deals with a preparation method of salts of 5-chloro-4-(2-imidazolin-2-yl-amino)-2,1,3-benzothiadiazole (tizanidine) of formula I, especially tizanidine hydrochloride, comprising preparation of a salt of tizanidine of formula I and a carboxylic acid as an intermediate, from which, after acidification with hydrogen chloride, tizanidine hydrochloride is obtained in a high yield and purity.Type: ApplicationFiled: December 18, 2009Publication date: October 27, 2011Inventors: Pavel Hradil, Lubomir Kvapil, Martin Grepl, Jan Novotny
-
Publication number: 20110237559Abstract: In its many embodiments, the present invention relates to a novel class of 6-substituted sulfonyl-1,3,3-trialkyl-6-azabicyclo[3.2.1]octane compounds useful to inhibit 11?-hydroxysteroid dehydrogenase type-I, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the expression of 11?-hydroxysteroid dehydrogenase type-I using such compounds or pharmaceutical compositions.Type: ApplicationFiled: August 12, 2008Publication date: September 29, 2011Applicant: Schering CorporationInventors: Craig D. Boyle, Samuel Chackalamannil, Unmesh Shah, Claire M. Lankin
-
Publication number: 20110212968Abstract: The invention relates to novel phenethylamide derivatives and their wherein A, B, R1, R2 and R3 are as described in the application, and to the use of such compounds, or of pharmaceutically acceptable salts of such compounds, as medicaments, especially as orexin receptor antagonists.Type: ApplicationFiled: October 13, 2009Publication date: September 1, 2011Inventors: Hamed Aissaoui, Christoph Boss, Christine Brotschi, Ralf Koberstein, Romain Siegrist, Thierry Sifferlen, Daniel Trachsel, Jodi T. Williams
-
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
-
Patent number: 8003675Abstract: A 3,4-dihalogenoisothiazole derivative represented by the general formula [I] (wherein R1 is a halogen atom; A is an oxygen atom or a sulfur atom; and R is a C1-C6 alkyl group, a C2-C5 alkenyl group, a C2-C5 alkynyl group, a C3-C6 cycloalkyl group, a phenyl group or a 5- to 10-membered heterocyclic group containing at least one of oxygen atom, sulfur atom and nitrogen atom), or a salt thereof.Type: GrantFiled: July 6, 2007Date of Patent: August 23, 2011Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Toshihiro Nagata, Atsushi Kogure, Isao Kaneko, Norihisa Yonekura, Ryo Hanai
-
Patent number: 8003806Abstract: The invention relates to compounds of the Formula 1 and to pharmaceutically acceptable salts and solvates thereof, wherein A, X2, X4, X5 and X1 are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals by administering the compounds of Formula 1 and to pharmaceutical compositions for treating such disorders which contain the compounds of Formula 1.Type: GrantFiled: November 9, 2005Date of Patent: August 23, 2011Assignee: OSI Pharmaceuticals, LLCInventors: Jason Bloxham, Gary V. Borzillo, Eric William Collington, Shazia Sadiq, Colin Peter Sambrook Smith, Chris L. Waller, Graham M. Wynne
-
Publication number: 20110201603Abstract: The present invention relates to novel Acylaminobenzamide derivatives represented by the following formula (I) and use thereof as pesticides: wherein V represents an aromatic ring group of V1 to V5 described in the detailed description, Q represents an aromatic ring group of Q1 to Q7 described in the detailed description, G1 and G2 represent O or S, R1 represents hydrogen, alkyl, haloalkyl, alkoxy, haloalkoxy, phenyl or a heterocyclic group and R2 and R3 represent hydrogen, alkyl, haloalkyl, alkylcarbonyl, haloalkylcarbonyl, alkoxycarbonyl or haloalkoxycarbonyl.Type: ApplicationFiled: July 30, 2009Publication date: August 18, 2011Applicant: Bayer CropScience AGInventors: Jun Mihara, Tetsuya Murata, Kei Domon, Yukiyoshi Watanabe, Yasushi Yoneta, Takuma Mori, Eiichi Shimojo, Katsuhiko Shibuya, Teruyuki Ichihara, Masashi Ataka, Ulrich Görgens
-
Patent number: 7998959Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1 and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 such as obesity and diabetes.Type: GrantFiled: January 11, 2007Date of Patent: August 16, 2011Assignee: Incyte CorporationInventors: Wenqing Yao, David M. Burns, Lihua Chen, Jincong Zhuo, Chunhong He
-
Patent number: 7981925Abstract: 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: GrantFiled: August 26, 2009Date of Patent: July 19, 2011Assignee: CalciMedica, Inc.Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
-
Patent number: 7977332Abstract: Certain noel N-(heteroarylalkyl)alkanediamine derivatives have provided unexpected insecticidal and acaricidal activity. These compounds are represented by formula I: wherein Ar, a, r, R, Ra, Rb, Rc, Rd, b, c, Re, Rf, Rg, Rh, R5, d, e, U, V, X, WR6 and R7 are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.Type: GrantFiled: December 2, 2004Date of Patent: July 12, 2011Assignee: FMC CorporationInventors: David M. Roush, John F. Chiarello, Jianming Yu, Benjamin J. Dugan, George Theodoridis, Manorama M. Patel, Walter H. Yeager, Steven W. Szczepanski
-
Publication number: 20110160176Abstract: The invention relates to compounds of the formula (I) wherein n is 0, 1 or 2; G is CH2 or CHR3; R1 is H, C,-C6-alkyl, C,-C6-alkyl substituted by C3-C6-cycloalkyl, C1-C6-hydroxyalkyl, fluorinated C,-C6-alkyl, C3-C6-cycloalkyl, fluorinated C3-C6-cycloalkyl, C3-C6 alkenyl, fluorinated C3-C6-alkenyl, formyl, acetyl or propionyl; R2, R3 and R4 are, independently of each other, H, methyl, fluoromethyl, difluoromethyl, or trifluoromethyl; A is phenylene, pyridylene, pyrimidylene, pyrazinylene, pyridazinylene or thiophenylene, which can be substituted by one or more substituents selected from halogen, methyl, methoxy and CF3; E is NR5 or CH2, wherein R5 is H or C1-C3-alkyl; Ar is a cyclic radical selected from the group consisting of phenyl, a 5- or 6-membered heteroaromatic radical comprising as ring members 1, 2 or 3 heteroatoms selected from N, O and S and a phenyl ring fused to a saturated or unsaturated 5- or 6-membered carbocyclic or heterocyclic ring, where the heterocyclic ring comprises as ring members 1, 2Type: ApplicationFiled: August 25, 2010Publication date: June 30, 2011Applicant: Abbott GmbH & Co. KGInventors: Karla Drescher, Andreas Haupt, Liliane Unger, Sean C. Turner, Wilfried Braje, Roland Grandel, Christophe Henry, Gisela Backfisch, Armin Beyerbach, Wilfried Lubisch
-
Patent number: 7968591Abstract: 1,3-disubstituted 4-methyl-1H-pyrrole-2-carboxamides corresponding to formula I methods for their production, pharmaceutical compositions containing them, and the use thereof for noradrenalin receptor regulation, particularly for inhibiting noradrenalin reuptake, and/or for 5-HT receptor regulation, particularly for inhibiting 5-hydroxy tryptophan reuptake, and/or for opioid receptor regulation and/or for batrachotoxin (BTX) receptor regulation and/or for treating or inhibiting pain and other conditions.Type: GrantFiled: December 9, 2008Date of Patent: June 28, 2011Assignee: Gruenenthal GmbHInventors: Stefan Oberboersch, Bernd Sundermann, Corinna Sundermann, Edward Bijsterveld, Hagen-Heinrich Hennies
-
ACYLAMINO-SUBSTITUTED FUSED CYCLOPENTANECARBOXYLIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS
Publication number: 20110152290Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: ApplicationFiled: November 4, 2010Publication date: June 23, 2011Applicant: SANOFI-AVENTISInventors: Matthias SCHAEFER, Josef PERNERSTORFER, Dieter KADEREIT, Hartmut STROBEL, Werngard CZECHTIZKY, L. Charlie CHEN, Alena SAFAROVA, Aleksandra WEICHSEL, Marcel PATEK -
Patent number: 7964735Abstract: Novel 3-acylaminobenzanilides of the formula (I) wherein R1 represents phenyl which may be substituted or a 5-member or 6-member heterocyclic ring group, which may be substituted, containing at least one hetero-atom selected from the group consisting of N, O, and S; R2 represents halogen, C1-6 alkyl, or C1-6 haloalkyl; R3 represents C1-6 haloalkyl, C1-6 haloalkoxy, C1-6 haloalkylthio, C1-6 haloalkylsulfinyl, or C1-6 haloalkylsulfonyl; R4 represents halogen, C1-6 alkyl, or C1-6 haloalkyl; X represents halogen, C1-6 alkyl, or C1-6 haloalkyl; and n represents 0 or 1 and the compounds are used as insecticides, and a use of the new compounds as insecticides.Type: GrantFiled: July 21, 2006Date of Patent: June 21, 2011Assignee: Bayer Cropscience AGInventors: Akihiko Yanagi, Yukiyoshi Watanabe, Katsuaki Wada, Tetsuya Murata, Jun Mihara, Katsuhiko Shibuya, Eiichi Shimojo, Akira Emoto
-
Patent number: 7956185Abstract: Compounds of formula (I) where X1, C1, and D1 are defined herein, are inhibitors of polo-like kinases. The compounds of formula (I) are useful for treatment of diseases of cellular proliferation, such as, for example, cancer.Type: GrantFiled: May 24, 2007Date of Patent: June 7, 2011Assignee: Abbott LaboratoriesInventors: Robert B. Diebold, Stevan W. Djuric, Vincent L. Giranda, Laura A. Hexamer, Nan-Horng Lin, Julie M. Miyashiro, Thomas D. Penning, Magdalena Przytulinska, Thomas J. Sowin, Gerard M. Sullivan, Zhi-Fu Tao, Yunsong Tong, Anil Vasudevan, Le Wang, Keith W. Woods, Zhiren Xia, Henry Q. Zhang
-
Publication number: 20110130409Abstract: The present invention relates to certain substituted 1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid derivatives of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1 receptor-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, microbial infections or diseases and viral infections or diseases.Type: ApplicationFiled: July 22, 2009Publication date: June 2, 2011Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Robert M. Jones, Daniel J. Buzard, Sangdon Han, Sun Hee Kim, Juerg Lehmann, Brett Ullman, Jeanne V. Moody, Xiuwen Zhu, Scott Stirn
-
Publication number: 20110130305Abstract: Provided are dyes and compositions which are useful in a number of applications, such as the detection and monitoring protein aggregation, kinetic studies of protein aggregation, neurofibrillary plaques analysis, evaluation of protein formulation stability, protein thermal stability shift assay and analysis of molecular chaperone activity. These dyes and compositions are also useful as probes in nucleic acid and protein detection.Type: ApplicationFiled: November 30, 2009Publication date: June 2, 2011Inventors: Wayne Forrest Patton, Sergiy M. Yarmoluk, Praveen Pande, Vladyslava Kovalska, Lijun Dai, Kateryna Volkova, Jack Coleman, Mykhaylo Losytskyy, Anthony Ludlum, Anatoliy Balanda
-
Publication number: 20110130391Abstract: The invention encompasses ureido substituted benzoic acid compounds, compositions comprising the compounds and methods for treating or preventing diseases associated with nonsense mutations of mRNA by administering these compounds or compositions.Type: ApplicationFiled: December 29, 2010Publication date: June 2, 2011Inventors: Richard G. Wilde, James J. Takasugi, Seongwoo Hwang, Ellen M. Welch, Guangming Chen
-
Publication number: 20110124636Abstract: The invention relates to novel 2-aza-bicyclo[3.1.0]hexane derivatives of Formula (I) wherein A, B, n and R1 are as described in the description, and to the use of such compounds, or of pharmaceutically acceptable salts of such compounds, as medicaments, especially as orexin receptor antagonists.Type: ApplicationFiled: December 28, 2007Publication date: May 26, 2011Applicant: Actelion Pharmaceuticals Ltd.Inventors: Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, Thierry Sifferlen, Daniel Trachsel
-
Publication number: 20110123586Abstract: Methods are provided for identifying molecules that can be used to positively and negatively manipulate quorum-sensing-mediated communication to control bacterial behavior. Small-molecule antagonists that disrupt quorum-sensing-mediated activities are identified. Methods are provided for disrupting detection of acyl-homoserine lactone autoinducer in Gram-negative bacteria by contacting the bacteria with the antagonists. Methods of inhibiting quorum sensing-mediated activity in Gram-negative bacteria are provided wherein the activity is pathogenicity, bioluminescence, siderophore production, type III secretion, or metalloprotease production.Type: ApplicationFiled: June 2, 2009Publication date: May 26, 2011Inventors: Bonnie Bassler, Lee Swem
-
Publication number: 20110112110Abstract: Inhibitors of the oncogenic tyrosine kinase ALK and of the Bcr-Abl mutant T315I Bcr-Abl, pharmaceutical compositions containing the same and their use for the treatment of hyper-proliferative diseases.Type: ApplicationFiled: March 30, 2009Publication date: May 12, 2011Applicants: UNIVERSITA' DEGLISTUDI DI MILANO- BICOCCA, UNIVERSITE ' DE GENEVE, UNIVERSITE ' CLAUDE BERNARD DE LYON 1Inventors: Carlo Gambacorti Passerini, Rosalind Helen Gunby, Alfonso Zambon, Leonardo Scapozza, Shaheen Ahmed, Peter G. Goekjian, David Gueyrard, Florence Popowycz, Cerric Schneider
-
Patent number: 7939528Abstract: The present invention relates to novel compounds which are antagonist or inverse agonists at an opioid receptor. Such compounds are useful in the treatment of obesity and related diseases and/or conditions in mammals, particularly humans. Methods of making and using such compounds are also disclosed.Type: GrantFiled: October 12, 2006Date of Patent: May 10, 2011Assignee: GlaxoSmithKline LLCInventors: Kevin Karl Barvian, Jason Daniel Speake, David John Cowan, Andrew Lamont Larkin, Jerzy Ryszard Szewczyk
-
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
-
Publication number: 20110105447Abstract: Disclosed are novel calcium release-activated calcium (CRAC) channel inhibitors, methods for preparing them, pharmaceutical compositions containing them, and methods of treatment using them. The present disclosure also relates to methods for treating non-small cell lung cancer (NSCLC) with CRAC inhibitors, and to methods for identifying therapeutics for treating and of diagnosing cancer.Type: ApplicationFiled: October 6, 2010Publication date: May 5, 2011Applicants: Incozen Therapeutics Pvt. Ltd., Rhizen Pharmaceuticals SAInventors: Meyyappan Muthuppalaniappan, Srikant Viswanadha, Gayatri S. Merikapudi, Swaroop Kumar V.S. Vakkalanka
-
Publication number: 20110092553Abstract: The present invention provides azole derivatives of Formula (I), methods of their preparation, pharmaceutical compositions comprising the compounds of Formula (I), and their use in treating human or animal disorders. The compounds of the invention can be useful as inhibitors of protein tyrosine phosphatases and thus can be useful for the management, treatment, control, or the adjunct treatment of diseases mediated by PTPase activity. Such diseases include Type I diabetes and Type II diabetes.Type: ApplicationFiled: November 19, 2010Publication date: April 21, 2011Applicant: TransTech Pharma, Inc.Inventors: Adnan M.M. Mjalli, Dharma R. Polisetti, Govindan Subramanian, James C. Quada, JR., Murty N. Arimilli, Ravindra R. Yarragunta, Robert C. Andrews, Rongyuan Xie
-
Publication number: 20110077265Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds having the general formula U1-M-U2 wherein M is a linking group covalently joining R2, R3, R4 or R5 of U1 to an R2, R3, R4 or R5 group of U2; U1 and U2 have the general formula (I) and G, X1, X2, R2, R3, R3?, R4, R4? and R5, are as described herein.Type: ApplicationFiled: April 29, 2008Publication date: March 31, 2011Applicant: Genentech, Inc.Inventors: John A. Flygare, Frederick Cohen, Kurt Deshayes, Michael F. T. Koehler, Lewis J. Gazzard, Lan Wang, Chudi Ndubaku
-
Publication number: 20110046182Abstract: Aspirin is one of the most widely used drugs in the treatment of inflammation, pain and fever. It has more recently found application in the prevention of heart attacks and stroke and is being studied as a cancer chemopreventative agent. Despite its value aspirin continues to be underutilized because it causes gastric bleeding. The technology under development potentially removes this problem. It is designed to reduce contact between the drug and the intestinal lining. An isosorbide aspirinate prodrug compound is thus provided. The compound has the general structure as shown in general formula (I) wherein Y is a C1-C8 alkyl ester, a C1-C8 alkoxy ester, a C3-C10 cycloalkyl ester, an arylester, a C1-C8 alkylaryl ester or —C(O)ORring, wherein Rring is a 5-membered aromatic or nonaromatic 5-member ring having at least one heteroatom substituted for a carbon of the ring system, which can be unsubstituted or substituted with at least one nitric oxide releasing group.Type: ApplicationFiled: December 19, 2008Publication date: February 24, 2011Applicant: The Provost, Fellows and Scholars of the College of the Holy and Undivided Trinity of Queen ElizabeInventors: John Francis Gilmer, Louise Clune-Moriarty, Maeve Lally
-
Publication number: 20110046129Abstract: 2-Phenylethylamino substituted carboxamide derivatives and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies are presented.Type: ApplicationFiled: September 9, 2010Publication date: February 24, 2011Applicant: Newron Pharmaceuticals S.p.A.Inventors: Florian Thaler, Mauro Napoletano, Cibele Sabido-David, Ermanno Moriggi, Carla Caccia, Laura Faravelli, Alessandra Restivo, Patricia Salvati
-
Publication number: 20110046387Abstract: Invention is related to novel compounds -5-aryl-4-(5-substituted 2,4-dihydroxyphenyl)-1,2,3-thiadiazoles with general formula (I). The compounds can be used in biomedicine as active ingredients in pharmaceutical formulations, because they inhibit Hsp90 chaperone which participate in cancer progression. This invention is also related to new intermediate compounds which are used for the synthesis of thiadiazoles of general formula (I).Type: ApplicationFiled: June 18, 2008Publication date: February 24, 2011Inventors: Daumantas Matulis, Inga Cikotiene, Egidijus Kazlauskas, Jurgita Matuliene
-
Publication number: 20110039819Abstract: The present invention relates to substituted phenoxybenzamide compounds of general formula (I): in which R1, R2, R3, R4, R5, X, R6 and q are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: April 9, 2009Publication date: February 17, 2011Inventors: Marion Hitchcock, Ingo Hartung