Benzene Ring Containing Patents (Class 564/155)
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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
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Publication number: 20110098504Abstract: The invention provides novel classes of HDAC inhibitors. Methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy are also provided as well as methods for treating cancer and methods for treating neurological diseases. Additionally, the invention further provides pharmaceutical compositions comprising an HDAC inhibitor of the invention, and kits comprising a container containing an HDAC inhibitor of the invention.Type: ApplicationFiled: October 25, 2010Publication date: April 28, 2011Applicant: Georgetown UniversityInventors: Alan P. Kozikowski, Anatoly Dritschilo, Mira Jung, Pavel A. Petukhov, Bin Chen
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Patent number: 7923576Abstract: The invention relates to tuned multifunctional linker molecules for charge transport through organic-inorganic composite structures. The problem underlying the present invention is to provide multifunctional linker molecules for tuning the conductivity in nanoparticle-linker assemblies which can be used in the formation of electronic networks and circuits and thin films of nanoparticles. The problem is solved according to the invention by providing a multifunctional linker molecule of the general structure CON1-FUNC1-X-FUNC2-CON2 in which X is the central body of the molecule, FUNC1 and FUNC2 independently of each other are molecular groups introducing a dipole moment and/or capable of forming intermolecular and/or intramolecular hydrogen bonding networks, and CON1 and CON2 independently of each other are molecular groups binding to nanostructured units comprising metal and semiconductor materials.Type: GrantFiled: January 3, 2006Date of Patent: April 12, 2011Assignee: Sony Deutschland GmbHInventors: Jurina Wessels, William Ford, Akio Yasuda
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Patent number: 7923577Abstract: Described is a new cooling agent represented by Structure I and compositions with known coolers having cooling properties and the application of Structure I in foodstuffs and chewing gum:Type: GrantFiled: April 27, 2009Date of Patent: April 12, 2011Assignee: International Flavors & Fragrances Inc.Inventors: Kathryn Anne Bardsley, Mark L. Dewis, Brian Trevor Grainger, Adam Jan Janczuk, Arkadiusz Kazimierski, Kenneth J. Kraut, John L. Sondrup, Ying Yang
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Patent number: 7902401Abstract: Compounds of Formula I are useful in the treatment of epilepsy, neuropathic pain, acute and chronic inflammatory pain, migraine, tardive dyskinesia and other related CNS disorders. wherein: A and R1 to R8 are defined in the specification.Type: GrantFiled: December 14, 2006Date of Patent: March 8, 2011Assignee: NPS Pharmaceuticals, Inc.Inventors: Guy A. Higgins, Methvin Issac, Abdelmalik Slassi, Tao Xin
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Publication number: 20110046128Abstract: A series of novel compounds showing anticonvulsant, chemical countermeasure(s), and analgesic activities is described. Such pharmaceutically active compounds may also show utility in the treatment of other central nervous system (“CNS”) diseases and disorders, such as anxiety, depression, insomnia, migraine headaches, schizophrenia, Parkinson's disease, spasticity, Alzheimer's disease, and bipolar disorder. Furthermore, such compounds may additionally find utility as analgesics (e.g., for the treatment of chronic or neuropathic pain) and as neuroprotective agents useful in the treatment of stroke(s), chronic neurodegenerative diseases (such as Alzheimer's disease and Huntington's disease), and/or traumatic brain and/or spinal cord injuries. Moreover, these/such compounds may also be useful in the treatment of status epilepticus and/or as chemical countermeasures.Type: ApplicationFiled: September 13, 2010Publication date: February 24, 2011Applicant: AURIMMED PHARMA, INC.Inventors: Amir Pesyan, Manuel F. Balandrin
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Publication number: 20110046138Abstract: A series of novel compounds showing anticonvulsant activity is described. Such pharmaceutically active compounds may also show utility in the treatment of other central nervous system (“CNS”) diseases and disorders, such as anxiety, depression, insomnia, migraine headaches, schizophrenia, Parkinson's disease, spasticity, Alzheimer's disease, and bipolar disorder. Furthermore, such compounds may additionally find utility as analgesics (e.g., for the treatment of chronic or neuropathic pain) and as neuroprotective agents useful in the treatment of stroke(s), chronic neurodegenerative diseases (such as Alzheimer's disease and Huntington's disease), and/or traumatic brain and/or spinal cord injuries. Moreover, these/such compounds may also be useful in the treatment of status epilepticus and/or as chemical countermeasures.Type: ApplicationFiled: March 18, 2009Publication date: February 24, 2011Inventors: Amir Pesyan, Manuel M. Balandrin
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Patent number: 7893092Abstract: Compounds of formula (I) wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula (I) can be used as agrochemical active ingredients and can be prepared in a manner known per se.Type: GrantFiled: December 7, 2005Date of Patent: February 22, 2011Assignee: Syngenta Crop Protection, Inc.Inventors: Andre Jeanguenat, Anthony Cornelius O'Sullivan
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Publication number: 20110039908Abstract: Small molecules are used to inhibit specific receptor-ligand interaction between Alzheimer's amyloid-? peptide (A?) and Receptor for Advanced Gly-cation Endproducts (RAGE). Objectives include treating Alzheimer's disease and other pathologies involving cerebral amyloid angiopathy; improving blood flow to or within the brain; decreasing the level of A? in the brain; reducing neuropathology associated with Alzheimer's disease; reducing inflammation and/or oxidant stress in the brain; improving memory and/or learning; treating other conditions involving A?/RAGE interaction at the blood-brain barrier, RAGE-mediated transport of A? into the brain, or RAGE activation in brain vasculature and/or brain parenchyma (e.g., diabetic complications); or any combination thereof.Type: ApplicationFiled: January 26, 2007Publication date: February 17, 2011Inventors: Berislav V. Zlokovic, Rashid Deane, Benjamin L. Miller
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Publication number: 20110021448Abstract: Inhibitors of the soluble epoxide hydrolase (sEH) are provided that incorporate multiple pharmacophores and are useful in the treatment of diseases.Type: ApplicationFiled: December 4, 2009Publication date: January 27, 2011Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: BRUCE D. HAMMOCK, IN-HAE KIM, CHRISTOPHE MORISSEAU, TAKAHO WATANABE, JOHN W. NEWMAN
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Publication number: 20110009457Abstract: The invention relates to a composition comprising at least one aminobenzamide compound or a salt thereof for controlling animal parasites, veterinary pharmaceutical compositions comprising at least one aminobenzamide of formula (I) for preventing infection with diseases transmitted through parasites, its use for the preparation of a veterinary pharmaceutical for controlling animal parasites, and a method for preventing infection with diseases transmitted through parasites.Type: ApplicationFiled: December 9, 2008Publication date: January 13, 2011Applicant: BAYER CROPSCIENCE AGInventors: Ulrich Görgens, Katsuaki Wada, Yukiyoshi Watanabe, Jun Mihara, Koichi Araki
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Patent number: 7868204Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.Type: GrantFiled: March 25, 2005Date of Patent: January 11, 2011Assignee: MethylGene Inc.Inventors: Daniel Delorme, Soon Hyung Woo, Arkadii Vaisburg, Oscar Moradei, Silvana Leit, Stephane Raeppel, Sylvie Frechette, Giliane Bouchain
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Publication number: 20110004019Abstract: The present invention provides a parakeratosis inhibitor, a pore-shrinking agent, and a rough skin inhibiting or ameliorating agent comprising, as an active ingredient, a compound that has excellent effects and high safety without safety problems such as sensory irritation, and provides an external composition for skin containing the same. The compound is selected from the glutamic acid derivatives represented by formula (1) or (2) and the salts thereof: wherein A represents a carbamoyl group, a benzyloxycarbonyl group, an alkyl group having 1 to 3 carbon atoms, an allyl group, or an amidino group; wherein Z represents an alkyl group having 1 to 4 carbon atoms, an alkenyl group having 2 to 4 carbon atoms, etc.Type: ApplicationFiled: March 12, 2009Publication date: January 6, 2011Applicant: SHISEIDO COMPANY LTD.Inventors: Toshii Iida, Maki Kaneko, Mikiko Kaminuma, Masaru Suetsugu
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Publication number: 20100324056Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted phenyl or optionally substituted pyridinyl, and R2, R3, R4, R5, R6, R7, R8 and R9 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: June 22, 2010Publication date: December 23, 2010Inventors: Chris Allen Broka, Ronald Charles Hawley
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Publication number: 20100324086Abstract: A compound of formula (1) as well as pharmaceutically acceptable salts thereof, and a pharmaceutical composition comprising the compound. The compound is useful for the treatment of disorder from pain, fever, inflammation and cancer.Type: ApplicationFiled: February 19, 2009Publication date: December 23, 2010Applicant: Novasaid ABInventors: Johan Wannberg, Mathias Alterman, Patric Stenberg, Jacob Westman
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Patent number: 7855308Abstract: The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.Type: GrantFiled: January 19, 2009Date of Patent: December 21, 2010Assignee: Abbott LaboratoriesInventors: Michael E. Brune, Peer B. Jacobson, James T. Link, Jyoti R. Patel, Jeffrey J. Rohde, Qi Shuai, Martin Winn, Vince S. Yeh, Hong Yong
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Patent number: 7851642Abstract: Disclosed are ?-amino-?-hydroxy-?-aryl-alkanoic acid amide compounds of formula (I) and the salts thereof, having renin-inhibiting properties. Also disclosed are pharmaceutical compositions comprising these compounds and methods of administering them for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.Type: GrantFiled: June 12, 2009Date of Patent: December 14, 2010Assignee: Novartis AGInventors: Daniel Kaspar Baeschlin, Juergen Klaus Maibaum, Holger Sellner
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Patent number: 7838520Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.Type: GrantFiled: March 15, 2005Date of Patent: November 23, 2010Assignee: MethylGene, Inc.Inventors: Daniel Delorme, Soon Hyung Woo, Arkadii Vaisburg, Oscar Moradei, Silvana Leit, Stephane Raeppel, Sylvie Frechette, Giliane Bouchain, Zhihong Zhou
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Patent number: 7838673Abstract: The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.Type: GrantFiled: October 16, 2007Date of Patent: November 23, 2010Assignee: Millennium Pharmaceuticals, Inc.Inventors: Edward J. Olhava, Mihaela Diana Danca
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Publication number: 20100286204Abstract: There is provided a compound having Formula I wherein each of R1, R2, R3, R4, R5, R6, R7, R8 and R9 are independently selected from (a) H, (b) R13, —OC(R13)3, —OCH(R13)2, —OCH2R13, C(R13)3, —CH(R13)2, or —CH2R13 wherein R13 is a halogen; (c) —CN; (d) optionally substituted alkyl, (e) optionally substituted heteroalkyl; (f) optionally substituted aryl; (g) optionally substituted heteroaryl; (h) optionally substituted arylalkyl; (i) optionally substituted heteroarylalkyl; (j) hydroxy; (k) alkoxy; (l) aryloxy; (m) —SO2-alkyl; and (n) —N(R14)C(O)R15, wherein R14 and R15 are independently selected from H and hydrocarbyl, wherein the optional substituents of (d) (e) (f) (h) and (i) are selected from the group consisting of: C1-6 alkyl, halo, cyano, nitro, haloalkyl, hydroxy, C1-6 alkoxy, carboxy, carboxyalkyl, carboxamide, mercapto, amino, alkylamino, dialkylamino, sulfonyl, sulfonamido, aryl and heteroaryl; wherein n and p are independently selected from 0 and 1; X is an optional group selected from O, S, S=0Type: ApplicationFiled: November 19, 2008Publication date: November 11, 2010Applicant: Sterix LimitedInventors: Nigel Vicker, Helen Victoria Bailey, Wesley Heaton, Joanna Mary Day, Atul Purohit, Barry Victor Lloyd Potter
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Publication number: 20100280108Abstract: A compound of general formula (I) wherein, R11, R12, R13, R14, R15, W, Y, R1, R2, R3, R4, R5, and R6 take various meanings for use in the treatment of cancer.Type: ApplicationFiled: December 19, 2008Publication date: November 4, 2010Applicant: Pharma Mar, S.A.Inventors: Alberto Rodriguez Vicente, Maria Garranzo García-Ibarrola, Carmen Murcia Pérez, Francisco Sánchez Sancho, Maria del Carmen Cuevas Marchante, Cristina Mateo Urbano, Isabel Digón Juárez
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Publication number: 20100278730Abstract: We disclose methods of detecting histone deacetylase activity in a mammal by administering to the mammal a compound comprising at least one atom having a nucleus detectable by magnetic resonance spectroscopy, wherein the compound is a substrate of histone deacetylase; and observing the compound or a cleavage product thereof in at least a portion of the body of the mammal by magnetic resonance spectroscopy (MRS). We also disclose methods of detecting histone deacetylase activity in a mammal by administering to the mammal a compound comprising at least one positron-emission-decaying radioisotope, wherein the compound is a substrate of histone deacetylase; and observing the compound or a cleavage product thereof in at least a portion of the body of the mammal by positron emission tomography (PET). We also disclose compounds useful as histone deacetylase substrates.Type: ApplicationFiled: April 8, 2008Publication date: November 4, 2010Inventors: Sabrina Ronen, Juri Gelovani, William Tong, Mian Alauddin, Uday Mukhopadhyay, Madhuri Sankaranatayanapillai, Ashutosh Pal
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Publication number: 20100249424Abstract: Disclosed is a method for preparing a compound of Formula 1 wherein R1 is CHX2, CX3, CX2CHX2 or CX2CX3; each X is independently Cl or F; Z is optionally substituted phenyl; and Q is phenyl or 1-naphthalenyl, each optionally substituted as defined in the disclosure; comprising contacting a compound of Formula 2 with hydroxylamine in the presence of a base. The present invention also relates to novel compounds of Formula 2, useful as starting materials for the aforedescribed method.Type: ApplicationFiled: August 4, 2008Publication date: September 30, 2010Applicant: E.I.DuPont De Nemours and CompanyInventors: Gary David Annis, Brenton Todd Smith
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Patent number: 7803970Abstract: This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor.Type: GrantFiled: June 7, 2004Date of Patent: September 28, 2010Assignee: University of Tennessee Research FoundationInventors: James T. Dalton, Duane D. Miller, Mitchell S. Steiner, Karen A. Veverka, Dong Jin Hwang, Jiyun Chen
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Publication number: 20100240926Abstract: (R)—N-benzyl-2-(benzyloxycarbonylamino)-3-methoxypropionamide is an intermediate useful for preparing lacosamide. It can be prepared, for example, by combining (R)—N-benzyl-2-(benzyloxycarbonylamino)-3-hydroxypropionamide with dimethylsulfate, followed by mixing with an alkali or alkaline earth metal hydroxide at a temperature of about 25° C. to about ?15° C.Type: ApplicationFiled: March 18, 2010Publication date: September 23, 2010Applicant: PLIVA HRVATSKA D.O.O.Inventors: Gordana VRBANEC, Miroslava HARCA, Ana SUCEC, Damir SAHNIC, Amir AVDAGIC
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Patent number: 7799950Abstract: A diamine includes a structure of formula (I), wherein X and Y are independently a divalence group selected from the group consisting of: —O—, —(C?O)—O—, —O—(C?O)—, —(C?O)—NH—, and —NH—(C?O)—; and R has a structure of formula (II): wherein R1, R2, R3, R4, R5, m, and n are as defined in Claim 1. A polyamic acid is prepared by reacting a diamine reactant including the aforesaid diamine of formula (I) with a tetracarboxylic dianhydride reactant. A liquid crystal orienting film contains a polyimide converted from the aforesaid polyamic acid.Type: GrantFiled: May 9, 2007Date of Patent: September 21, 2010Assignee: Daily Polymer Co., Ltd.Inventors: Chuan-Ter Yan, Chih-Hsiung Huang, Chao-Ching Huang, Chin-Wang Kao, Tin-Hun Hung
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Publication number: 20100218414Abstract: The compounds of general formula (I) wherein: R1 is hydrogen, phenyl, C1-6 alkyl which can be further substituted with R3, R3 is 5- or 6-membered aromatic or heteroaromatic ring system which can be further substituted with benzyl or hydroxyl groups; R2 is OR4, NHR4, R4 is hydrogen, C1-6 alkyl or benzyl n is an integer from 1 to 12 or the salts of compounds mentioned which can form gels with commercial fuels, organic solvents and water.Type: ApplicationFiled: September 4, 2008Publication date: September 2, 2010Inventors: Mladen Zinic, Janja Makarevic
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Patent number: 7786046Abstract: The present invention relates to benzoyl-substituted serinamides of the formula I in which the variables R1 to R11 are as defined in the description, and to their agriculturally useful salts, to processes and intermediates for their preparation, and to the use of these compounds or of compositions comprising these compounds for controlling unwanted plants.Type: GrantFiled: March 29, 2006Date of Patent: August 31, 2010Assignee: BASF AktiengesellschaftInventors: Matthias Witschel, Cyrill Zagar, Eike Hupe, Toralf Kühn, William Karl Moberg, Liliana Parra Rapado, Frank Stelzer, Andrea Vescovi, Robert Reinhard, Bernd Sievernich, Klaus Groβmann, Thomas Ehrhardt
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Patent number: 7777077Abstract: The invention is directed to compounds of formula I: wherein Ar, r, R3, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds of formula I have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and a process and intermediates for preparing such compounds.Type: GrantFiled: January 31, 2008Date of Patent: August 17, 2010Assignee: Theravance, Inc.Inventors: Seok-Ki Choi, Paul R. Fatheree, Ryan Hudson, Keith Jendza, Robert M. McKinnell, Vivek Sasikumar
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Publication number: 20100196502Abstract: One aspect of the invention relates to isoform-selective HDAC inhibitors. Also provided are methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy. The invention also provides methods for treating cancer, methods for treating neurological diseases and methods for treating malaria. Additionally, the invention provides pharmaceutical compositions comprising an HDAC inhibitor of the invention; and kits comprising a an HDAC inhibitor of the invention.Type: ApplicationFiled: August 2, 2007Publication date: August 5, 2010Applicant: Georgetown UniversityInventors: Alan P. Kozikowski, Mira Jung, Anatoly Dritschilo, Arsen Gaysin, Pavel A. Petukhov, Werner Tueckmantel, Hongbin Yuan
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Patent number: 7754919Abstract: The present invention provides for compounds useful for treating an HIV-1 infection, or preventing an HIV-1 infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein R1, R2, R3, R4, R5 and X are as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds.Type: GrantFiled: October 18, 2006Date of Patent: July 13, 2010Assignee: Roche Palo Alto LLCInventors: Tania Silva, Zachary Kevin Sweeney
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Publication number: 20100144707Abstract: The present invention relates to inhibitors of ROCK1 and ROCK2 and methods of modulating the pharmacokinetic and/or pharmacodynamic properties of such compounds. Also provided are methods of inhibiting ROCK1 and or ROCK2 that are useful for the treatment of disease.Type: ApplicationFiled: March 27, 2006Publication date: June 10, 2010Inventors: Alessandra Bartolozzi, Stewart Campbell, Hope Foudoulakis, Brian Kirk, Siya Ram, Paul Sweetnam
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Patent number: 7718684Abstract: A modest (2-5 fold) increase in androgen receptor (AR) mRNA is the only expression change consistently associated with developing resistance to antiandrogen therapy. Increased levels of AR confer resistance to anti-androgens by amplifying signal output from low levels of residual ligand and altering the normal response to antagonists. This invention provides cell based assays for use in the examination of new therapeutic modalities and provides for the design of novel antiandrogen compounds.Type: GrantFiled: February 23, 2005Date of Patent: May 18, 2010Assignee: The Regents of the University of CaliforniaInventors: Michael E. Jung, Samedy Ouk, Charles L. Sawyers, Charlie D. Chen, Derek Welsbie
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Patent number: 7714167Abstract: The present invention relates to the synthesis of chiral epoxides via a catalytic asymmetric oxidation of olefins. Additionally, the methodology provides a method of asymmetrically oxidizing sulfides and phosphines. This asymmetric oxidation employs a catalyst system composed of a metal and a chiral bishydroxamic acid ligand, which, in the presence of a stoichiometric oxidation reagent, serves to asymmetrically oxidize a variety of substrates.Type: GrantFiled: January 22, 2007Date of Patent: May 11, 2010Assignees: University of Chicago, Japan Science & Technology AgencyInventors: Hisashi Yamamoto, Arindrajit Basak, Wei Zhang
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Publication number: 20100113829Abstract: The present invention provides a pharmaceutical composition or crystalline composition with a specific dissolution profile, which comprises suberoylanilide hydroxamic acid or a pharmaceutically acceptable salt or hydrate thereof as an active ingredient. The present invention provides a process of producing said crystalline composition or pharmaceutical composition. The present invention also provides compositions with a specific particle size distribution.Type: ApplicationFiled: January 13, 2010Publication date: May 6, 2010Inventors: Aaron S. Cote, Erik A. Dienemann, Hsien-Hsin Tung, Benjamin Max Cohen, Vincent R. Capodanno, Thomas A. Miller
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Patent number: 7705182Abstract: This invention provides androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor.Type: GrantFiled: February 24, 2003Date of Patent: April 27, 2010Assignee: University of Tennessee Research FoundationInventors: James T. Dalton, Duane D. Miller, Mitchell S. Steiner, Karen A. Veverka, Dong Jin Hwang, Jiyun Chen
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Patent number: 7687435Abstract: The present invention relates to benzoyl-substituted phenylalanineamides of the formula I in which the variables R1 to R15 are as defined in the description, and to their agriculturally useful salts, to processes and intermediates for their preparation and to the use of these compounds or of compositions comprising these compounds for controlling unwanted plants.Type: GrantFiled: December 17, 2004Date of Patent: March 30, 2010Assignee: BASF AktiengesellschaftInventors: Matthias Witschel, Michael Puhl, Gerhard Hamprecht, Liliana Parra Rapado, Ulf Misslitz, CyrilL Zagar, Peter Plath, Robert Reinhard, Bernd Sievernich, Rex Liebl
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Publication number: 20100056522Abstract: An object of the present invention is to find a novel pharmacological effect of a compound having an HDAC inhibitory effect. The compound having an HDAC inhibitory effect of the invention has an excellent effect of cell morphological change on trabecular meshwork cells and/or effect of intraocular pressure reduction, and is therefore useful as a preventive and/or therapeutic agent for a disease considered to be associated with aqueous humor circulation and/or intraocular pressure, particularly as a preventive and/or therapeutic agent for glaucoma or ocular hypertension.Type: ApplicationFiled: March 28, 2008Publication date: March 4, 2010Applicant: Santen Pharmaceutical Co., Ltd.Inventors: Shinji Yoneda, Koushi Fujisawa, Katsuhiko Watanabe, Junko Fujikawa, Atsushi Shimazaki, Tomoko Kirihara, Hisashi Tajima
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Publication number: 20100048652Abstract: A compound of formula (I): wherein A1, A2, A3, A4, R1, R2, R3, R4, G1, G2, Q1, Y1, Y2, and Y4 are as defined in claim 1; or salts or N-oxides thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising them and to methods of using them to combat and control insect, acarine, mollusc and nematode pests.Type: ApplicationFiled: July 19, 2007Publication date: February 25, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Peter Renold, Peter Maienfisch, William Lutz, Werner Zambach
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Publication number: 20100036132Abstract: The present invention is directed to novel processes for the preparation of opioid modulators (agonists and antagonists) and intermediates in their synthesis. The opioid modulators are useful for the treatment and prevention of as pain and gastrointestinal disorders.Type: ApplicationFiled: October 16, 2009Publication date: February 11, 2010Inventors: Chaozhong Cai, Wei He
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Publication number: 20100035991Abstract: The present invention provides amine base salts of SAHA, polymorphs and pharmaceutical compositions thereof. The invention provides a method of treating cancer by administering the pharmaceutical composition. The invention also provides a crystalline composition comprising the amine base and SAHA. The invention also provides methods of obtaining the amine base salt and crystalline composition.Type: ApplicationFiled: September 24, 2007Publication date: February 11, 2010Inventors: Arlene McKeown, Fuh-Rong Tsay
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Publication number: 20100022585Abstract: Disclosed are beta and gamma-amino isoquinoline amide compounds and substituted benzamide compounds. In particular, the invention provides compounds that affect the function of kinases in a cell and that are useful as therapeutic agents or with therapeutic agents. The compounds of the invention are useful in the treatment of a variety of diseases and conditions including eye diseases such as glaucoma, cardiovascular diseases, and diseases characterized by abnormal growth, such as cancers. The invention further provides compositions containing the beta or gamma-amino isoquinoline amide compounds or substituted benzamide compounds.Type: ApplicationFiled: July 25, 2008Publication date: January 28, 2010Inventors: Mitchell A. deLong, Jill Marie Sturdivant, Susan M. Royalty
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Publication number: 20090288768Abstract: The invention generally relates to di-cinnamyl compounds useful in a variety of adhesive applications. More specifically, the invention provides chain-extended bismaleimides and methods for generating them by reaction with di-cinnamyl compounds, including particular di-cinnamyl compounds disclosed herein. Invention di-cinnamyl compounds can also be used as co-monomers in a Diels-Alder type cure, and can act as a co-monomer in a thermoset composition with a maleimide monomer.Type: ApplicationFiled: April 9, 2009Publication date: November 26, 2009Inventor: Stephen M. Dershem
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Patent number: 7622610Abstract: The invention is directed to the Form A polymorph of N-benzyl-N?-(2,6-diisopropyl-phenyl)-N-isopropyl-malonamide and its use as a therapeutic/cosmetic agent.Type: GrantFiled: February 15, 2006Date of Patent: November 24, 2009Assignee: Graceway Pharmaceuticals, LLCInventor: Rita Mayur Lodaya
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Publication number: 20090286990Abstract: A process for preparing irbesartan comprises pentanoylation of cycloleucine in the presence of sodium hydroxide to form n-pentanoyl cycloleucine, condensing this product with 2-(4-aminomethyl phenyl) benzonitrile using dicyclohexyl carbodiimide and 1-hydroxy benzotriazole as a catalyst to form the 4-(&quest-N-pentanoyl amino) cyclopentamido methyl-2?-cyano biphenyl compound, and then cyclizing using trifluoroacetic acid in the presence of an aromatic solvent to form cyano irbesartan. Cyano irbesartan is converted to irbesartan by reaction with tributyltin chloride and sodium azide in the presence of an aromatic solvent.Type: ApplicationFiled: May 20, 2005Publication date: November 19, 2009Inventors: Reguri Buchi Reddy, Sunkari Sudhakar, Chaganti Sridhar, Somisetti Narender Rao, Sundaram Venkataraman, Padi Pratap Reddy, Bollikonda Satyanarayana
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Publication number: 20090278087Abstract: The instant invention concerns a composition comprising a base polymer, at least one compound of the formula E-(L-E)x wherein: E is formula (I) or formula (II) and L is a linking group; and at least one transition metal in a positive oxidation state. The invention also concerns packages containing walls comprising such compositions, methods of forming such packages, and methods of packaging an oxygen-sensitive item within such a package.Type: ApplicationFiled: February 15, 2006Publication date: November 12, 2009Applicant: Constar International, IncInventors: Girish Nilkanth Deshpande, Venkat Govindarajan, John M. Rost, Alan Silverman
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Publication number: 20090270338Abstract: Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type and/or T-type calcium channel activity are disclosed. Specifically, a series of compounds of substituted or unsubstituted N-cyclylalkyl-diphenylpropanamide derivatives as shown in formula (1).Type: ApplicationFiled: April 28, 2009Publication date: October 29, 2009Inventors: Robert Galemmo, JR., Richard Holland, Gabriel Hum
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Publication number: 20090264533Abstract: The present invention is directed to methods and compositions methods and compositions for determining and inhibiting gene transcription in mammalian cells. The invention relates to novel inhibitors of rho-mediated gene transcription and to compounds that may be used as therapeutic agents.Type: ApplicationFiled: March 21, 2006Publication date: October 22, 2009Inventors: Richard Neubig, Chris Evelyn
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Patent number: 7601872Abstract: Disclosed are compounds capable of facilitating transport of biologically active agents or substances into cells having the general structure: wherein Q is selected from the group consisting of N, O and S; L is any bivalent organic radical capable of linking each Q, such as C, CH, (CH2)l, or {(CH2)i-Y—(CH2)j}k, wherein Y is selected from the group consisting of CH2, an ether, a polyether, an amide, a polyamide, an ester, a sulfide, a urea, a thiourea, a guanidyl, a carbamoyl, a carbonate, a phosphate, a sulfate, a sulfoxide, an imine, a carbonyl, and a secondary amino group and wherein Y is optionally substituted by —X1-L?-X2-Z or -Z; R1-R6, independently of one another, are selected from the group consisting of H, —(CH2)p-D-Z, an alkyl, an alkenyl, an aryl, and an alkyl or alkyl ether optionally substituted by one or more of an alcohol, an aminoalcohol, an amine, an amide, an ether, a polyether, a polyamide, an ester, a mercaptan, an alkylthio, a urea, a thiourea, a guanidyl, or a carbamoyl group, and wType: GrantFiled: January 21, 2005Date of Patent: October 13, 2009Assignee: Life Technologies CorporationInventors: Yongliang Chu, Malek Masoud, Gulilat Gebeyehu
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Publication number: 20090247506Abstract: Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.Type: ApplicationFiled: August 20, 2007Publication date: October 1, 2009Inventors: Niels H. Andersen, Jason Bowman, Alice L. Erwin, Eric A. Harwood, Toni Kline, Khisimuzi E. Mdluli, Simon Ng, Keith B. Pfister, Ribhi Shawar, Allan S. Wagman, Asha Yabannavar