Polycyclo-carbocyclic Ring System Having At Least Three Cyclos Patents (Class 544/294)
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Publication number: 20110227053Abstract: The present invention relates to a novel chrysene derivative and an organic electronic device using the same. A chrysene according to the present invention may act as a hole injection, hole transport, electron injection and transport, or light emitting material in an organic light emitting device and an organic electronic device, and in particular, may be used alone as a light emitting host or a dopant.Type: ApplicationFiled: November 18, 2009Publication date: September 22, 2011Inventors: Jae-Soon Bae, Jeung-Gon Kim, Ji-Eun Kim, Hye-Young Jang, Jun-Gi Jang, Sang-Young Jeon
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Publication number: 20110144096Abstract: Novel compounds and methods for activating the TrkB receptor are provided. The methods include administering in vivo or in vitro a therapeutically effective amount of a compound containing four six-membered rings and a substituted or unsubstituted C5 or C6 heteroaryl or hetero-cycloalkyl ring and pharmaceutically acceptable salts, prodrugs, and derivatives thereof. Specifically, methods and compounds for the treatment of disorders including neurologic, neuropsychiatric, and metabolic disorders are provided. For example, a method is provided of treating or reducing the risk of depression, anxiety, or obesity in a subject, which includes selecting a subject with or at risk of developing depression, anxiety, or obesity, and administering to the subject a therapeutically effective amount of the described compounds.Type: ApplicationFiled: July 28, 2009Publication date: June 16, 2011Applicant: EMORY UNIVERSITYInventor: Keqiang Ye
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Patent number: 7943208Abstract: The invention provides materials and methods for making anisotropic solids which may be in the form of films, layers, shaped elements, and other shaped articles. The methods provide anisotropic solids without the need for rolling, rubbing, or stretching to impart orientational alignment of the molecules of the solid. The methods employ organic or organometallic compounds which are soluble orienting molecules. The solvent or solvent system must be sufficiently volatile to be removed without disruption of the molecular orientation. The soluble orienting molecules include those containing one or more hydrophilic and/or ionic groups and the solvent or solvent system can be a polar organic solvent or solvent system or an aqueous solvent or solvent system. The invention also provides novel compounds having quaterrylene, perylene and naphthalene ring systems carrying one or more hydrophilic and/or ionic groups.Type: GrantFiled: September 25, 2009Date of Patent: May 17, 2011Assignee: Board of Regents of the Nevada System of Higher Education, on behalf of the University of Nevada, RenoInventors: Travis D. Carson, Sean M. Casey, Isaac K. Iverson, Wonewoo Seo, Suk-Wah Tam-Chang
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Publication number: 20110020376Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.Type: ApplicationFiled: June 2, 2010Publication date: January 27, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Juan-Miguel Jimenez, Andrew Miller, Jeremy Green, Huai Gao, Gregory Henkel, Michael Liu, Timothy Neuberger
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Publication number: 20110009620Abstract: The present invention provides 4-amino-5-cyanopyrimidine derivatives of the formula: wherein R1, R2 and R3 are defined herein, or pharmaceutically acceptable salts thereof, having a safe and potent adenosine A2a receptor agonistic activity; and also provides an adenosine A2a receptor agonist, an intraocular pressure reducing agent, or a medicine for treating glaucoma, etc., which comprises the compound as an active ingredient.Type: ApplicationFiled: September 22, 2010Publication date: January 13, 2011Inventors: Masaya Kato, Norifumi Sato, Minoru Okada, Tetsuyuki Uno, Nobuaki Ito, Yasuhiro Takeji, Hisashi Shinohara, Masahiro Fuwa
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Publication number: 20110009391Abstract: The present invention relates to tetrahydroquinoxaline urea derivatives, to their preparation and to their therapeutic application.Type: ApplicationFiled: July 26, 2010Publication date: January 13, 2011Applicant: SANOFI-AVENTISInventors: Alain Jean BRAUN, Olivier CRESPIN, Claudie NAMANE, Eric NICOLAI, Francois PACQUET, Cecile PASCAL, Christophe PHILIPPO, Olivier VENIER
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Publication number: 20110002855Abstract: Piperazinyl oxoalkyl tetrahydro-beta-carbolines and related analogues of the formula (I): are provided, as are methods for their preparation and use. Such compounds may generally be used to modulate ligand binding to histamine H3 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and therapeutic methods are provided, as are methods for using such ligands for detecting histamine H3 receptors (e.g., receptor localization studies).Type: ApplicationFiled: June 25, 2008Publication date: January 6, 2011Applicant: NEUROGEN CORPORATIONInventors: Timothy M. Caldwell, Yang Gao, Linghong Xie, Yuelian Xu
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Publication number: 20100273775Abstract: Disclosed are compounds of Formulae 1 and 1a, N-oxides, and salts thereof, wherein R1, R1a, Y, and J are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention. Further disclosed is a method for preparing compounds of Formula 1 from compounds of Formula 1a.Type: ApplicationFiled: December 10, 2008Publication date: October 28, 2010Applicant: E.I. Du pont de Nemours and CompanyInventors: John Joseph Bisaha, Alvin Donald Crews, JR., Michael Henry Howard, JR., Paula Louise Sharpe, Thomas Martin Stevenson, Andrew Edmund Taggi
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Publication number: 20100210654Abstract: The present invention relates to novel P2Y12 receptor antagonists useful for treating, alleviating and/or preventing diseases and disorders related to P2Y12 receptor function as well as pharmaceutical compositions comprising such compounds and methods for preparing such compounds. The present invention is further directed to the use of these compounds, alone or in combination with other therapeutic agents, for the alleviation, prevention and/or treatment of diseases and disorders, especially the use as antithrombotic agents for inhibiting platelet aggregation.Type: ApplicationFiled: March 7, 2008Publication date: August 19, 2010Applicant: RHEINISCHE FRIEDRICH-WILHELMS UNIVERSITÄT BONNInventors: Christa E. Müller, Younis Baqi
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Publication number: 20100187505Abstract: The present invention relates to the compounds of the formula (1) and to organic electroluminescent devices, in particular blue-emitting devices, in which these compounds are used as host material or dopant in the emitting layer and/or as hole-transport material and/or as electron-transport material.Type: ApplicationFiled: April 29, 2008Publication date: July 29, 2010Inventors: Philipp Stoessel, Arne Buesing, Holger Heil
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Publication number: 20100160328Abstract: The present invention relates to the novel compounds of the general formula (I) possessing dipeptidyl peptidase IV enzyme inhibitory activity, pharmaceutical compositions thereof, methods of using said compounds, processes for their preparation and intermediates of the general formulae (II), (IV), (V), (VII), (VIII) and (IX).Type: ApplicationFiled: December 14, 2009Publication date: June 24, 2010Applicant: SANOFI-AVENTISInventors: Peter Aranyi, Imre BATA, Sandor Batori, Eva BORONKAY, Philippe BOVY, Zoltan Kapui, Edit SUSAN, Tibor SZABO, Katalin Urban-Szabo, Marton VARGA
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Publication number: 20090088570Abstract: An organic electroluminescent device, which has, between a pair of electrodes, at least one organic layer including a light-emitting layer, in which the organic layer contains a specific tetraphenylene compound, and in which the light-emitting layer contains a phosphorescent material; and a specific tetraphenylene compound that can be used in the device.Type: ApplicationFiled: November 20, 2008Publication date: April 2, 2009Applicant: FUJIFILM CORPORATIONInventors: Jun OGASAWARA, Tatsuya Igarashi, Satoshi Sano
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Publication number: 20080275048Abstract: Compounds of formula (I) Z-Ar1—Ar2 ??(I) wherein Z is a diazabicyclic amine, Ar1 is a 5- or 6-membered aromatic ring, and Ar2 is selected from the group consisting of an unsubstituted or substituted 5- or 6-membered heteroaryl ring; unsubstituted or substituted bicyclic heteroaryl ring; 3,4-(methylenedioxy)phenyl; carbazolyl; tetrahydrocarbazolyl; naphthyl; and phenyl; wherein the phenyl is substituted with 0, 1, 2, or 3 substituents in the meta- or para-positions. The compounds are useful in treating conditions or disorders prevented by or ameliorated by ?7 nAChR ligands. Also disclosed are pharmaceutical compositions comprising compounds of formula (I) and methods for using such compounds and compositions.Type: ApplicationFiled: June 3, 2008Publication date: November 6, 2008Applicant: ABBOTT LABORATORIESInventors: Jennifer M. Frost, Jianguo Ji, Tao Li, Diana L. Nersesian, Karin R. Tietje
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Patent number: 7432371Abstract: Nanofilms useful for filtration are prepared from oriented amphiphilic molecules and oriented macrocyclic modules. The amphiphilic species may be oriented on an interface or surface. The nanofilm may be prepared by depositing or attaching an oriented layer to a substrate. A nanofilm may also be prepared by coupling the oriented macrocyclic modules to provide a membrane.Type: GrantFiled: February 7, 2003Date of Patent: October 7, 2008Assignee: Covalent Partners, LLCInventors: Joshua W. Kriesel, Timothy B. Karpishin, Donald B. Bivin, Grant Merrill, Martin S. Edelstein, Thomas H. Smith, Jeffery A. Whiteford, Robert T. Jonas, Mark Micklatcher, Serena Joshi
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Publication number: 20080234292Abstract: The present invention relates to a series of novel compounds having the formula (I) wherein: X is NR3 or O; n is 1 or 2; A is a bicyclic carbocycle and R1 and R2 are as described herein. The compounds are useful as DPP-IV inhibitors, such as for the treatment of diabetes.Type: ApplicationFiled: July 21, 2005Publication date: September 25, 2008Inventors: Susan Marie Royalty, James Ford Burns, Jan Jozef Scicinski, Gunnar Erik Jagdmann, Jr., Robert James Foglesong, Kellee Griffin Ring, Tatyana Dyakonov, David Middlemiss
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Publication number: 20080152950Abstract: An anthracene derivative and an organic electroluminescent device using the same are provided. More specifically, provided are an anthracene derivative represented by Formula 1: wherein each R1 is aryl; and each R2 is independently C6-C20 aryl or C3-C19 heteroaryl, which are unsubstituted or substituted with one or more substituents selected from the group consisting of C1-C10 alkyl, C1-C10 alkoxy, cyano, C1-C10 alkylamino, C1-C10 alkylsilyl, halogen, C6-C10 aryl, C6-C10 aryloxy, C6-C10 arylamino, C6-C10 arylsilyl, C3-C19 heteroaryl and hydrogen; and an organic electroluminescent device using the same. The present invention can provide an organic electroluminescent device having excellent power and luminance efficiencies in conjunction with a long service life.Type: ApplicationFiled: November 30, 2007Publication date: June 26, 2008Applicant: SFC CO., LTD.Inventors: Jong-Tae JE, Sug-Kwang Hwang, Sung-Hoon Kim, Seung-Hyuck Choi, Seon-Keun Yoo
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Publication number: 20080125399Abstract: Compounds of structural formula (I) are modulators of the androgen receptor (AR) in a tissue selective manner. These compounds are useful in the enhancement of weakened muscle tone and the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid-induced osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, inflammatory arthritis and joint repair, HIV-wasting, prostate cancer, benign prostatic hyperplasia (BPH), cancer cachexia, Alzheimer's disease, muscular dystrophies, cognitive decline, sexual dysfunction, sleep apnea, depression, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.Type: ApplicationFiled: April 4, 2005Publication date: May 29, 2008Inventors: Jiabing Wang, Carol A. McVean
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Publication number: 20080119492Abstract: The present invention relates to compositions and methods for treating cancer and other disease states characterized by abnormal cell proliferation. In particular, the present invention relates to certain novel non-nucleoside pharmacologically active compounds that alter telomere and telomerase functions, regulate cell proliferation and/or treat cancer and other diseases characterized by abnormal cell proliferation. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit telomerase, to regulate cell proliferation, and to treat cancer or to inhibit the proliferation of the rumor cells, and to treat other proliferative conditions.Type: ApplicationFiled: July 28, 2006Publication date: May 22, 2008Inventors: Jean-Marie Lehn, Jean-Louis Mergny, Anne Petitjean, Maia-Paule Teulade-Fichou, Andrei Tchirkov, Pierre Verrelle
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Patent number: 7321033Abstract: The invention is directed to 3-?-D-ribofuranosylthiazolo[4,5-d]pyridimine nucleosides and pharmaceutical compositions containing such compounds that have immunomodulatory activity. The invention is also directed to the therapeutic or prophylactic use of such compounds and compositions, and to methods of treating diseases and disorders described herein, by administering effective amounts of such compounds.Type: GrantFiled: June 7, 2004Date of Patent: January 22, 2008Assignee: Anadys Pharmaceuticals, Inc.Inventors: Devron R. Averett, Stephen E. Webber, Joseph R. Lennox, Erik J. Rueden, David Louis Clark, Alan Xin Xiang
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Publication number: 20070254879Abstract: The instant invention provides for compounds which comprise substituted triazoloquinazolinones that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting CHK1 activity by administering the compound to a patient in need of treatment of cancer.Type: ApplicationFiled: April 24, 2007Publication date: November 1, 2007Inventors: Kenneth L. Arrington, Edward J. Brnardic, Vadim Y. Dudkin, Mark E. Fraley, Shaei Y. Huang, Cheng Wang
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Patent number: 7279575Abstract: Pyrimidylpyrrole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.Type: GrantFiled: August 5, 2004Date of Patent: October 9, 2007Assignee: Pfizer Italia S.r.l.Inventors: Ermes Vanotti, Roberto D'Alessio, Marcellino Tibolla, Mario Varasi, Alessia Montagnoli, Corrado Santocanale, Paolo Orsini, Antonio Pillan
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Patent number: 7226926Abstract: A class of 8-fluoroimidazo[1,2-?]pyridine derivatives, substituted at the 3-position by an optionally substituted five-membered or six-membered heteroaromatic ring, being selective ligands for GABAA receptors, in particular having high affinity for the ?2 and/or ?3 and/or ?5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.Type: GrantFiled: May 23, 2003Date of Patent: June 5, 2007Assignee: Merck Sharp & Dohme Ltd.Inventors: Wesley Peter Blackaby, Jose Luis Castro Pineiro, Simon Charles Goodacre, David James Hallett, Alexander Charles Humphries, Philip Jones, Kevin John Merchant, Michael Reader
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Patent number: 7205304Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicineType: GrantFiled: March 11, 2003Date of Patent: April 17, 2007Assignee: Janssen Pharmaceutica N.V.Inventors: Kristof Van Emelen, Janine Arts, Leo Jacobus Jozef Backx, Hans Louis Jos De Winter, Sven Franciscus Anna Van Brandt, Marc Gustaaf Celine Verdonck, Lieven Meerpoel, Isabelle Noëlle Constance Pilatte, Virginie Sophie Poncelet, Alexey Borisovich Dyatkin, Jimmy Arnold Viviane Van heusden
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Patent number: 7176310Abstract: This invention is directed to compound of the following formula (I): wherein R1, R2, R3 and R4 are as described herein. These compounds and pharmaceutical compositions containing the compounds are useful in treating inflammatory disorders in mammals.Type: GrantFiled: April 4, 2003Date of Patent: February 13, 2007Assignee: UCB SAInventors: Theodore A. Baughman, Jim P. Boyce, Ihab S. Darwish, J. Jeffry Howbert, Nathan C. Ihle, Randy W. Jackson, Scott C. Jeffrey, Dean Maeda, Kraig M. Yager
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Patent number: 7125996Abstract: The invention provides methods relating to a novel screening assay format that can be applied to broad members of the protein kinase gene family. The assay uses a series of labeled, active site probes described herein that can be displaced by an inhibitor agent. The Kd for the inhibitor compound is derived based on the Kd of the probe for the kinase and the dose response of the inhibitor agent. The invention also provides active site probes suitable for use with the screening method.Type: GrantFiled: September 30, 2004Date of Patent: October 24, 2006Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Anthony S. Prokopowicz, III, Martha Priscilla Brown, Jessi Marie Wildeson, Scott Jakes, Mark E. Labadia
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Patent number: 7087598Abstract: This invention provides compounds of Formula I, their N-oxides and agriculturally suitable salts wherein A and B are independently O or S; J is an optionally substituted 5- or 6-memebered nonaromatic heterocyclic ring; K is taken together with the two contiguous linking carbon atoms to form a phenyl ring or a 5- or 6-membered heteroaromatic ring, each ring optionally substituted; and R1, R2, and R3 are as defined in the disclosure. Also disclosed are methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound of Formula I, an N-oxide thereof or a suitable salt of the compound (e.g., as a composition described herein).Type: GrantFiled: May 21, 2002Date of Patent: August 8, 2006Assignee: E. I. du Pont de Nemours and CompanyInventor: David Alan Clark
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Patent number: 7087599Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restinosis, gynacomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.Type: GrantFiled: February 14, 2001Date of Patent: August 8, 2006Assignee: Merck & Co., Inc.Inventors: Dann LeRoy Parker, Jr., Ronald W. Ratcliffe, Robert R. Wilkening, Kenneth J. Wildonger
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Patent number: 7018685Abstract: The invention relates to fluorinated aromatics of the formula (I) where X is CH2, C?O, CF2, O or S, Y is H or F, with the proviso that Y has to be F when X is CH2, and where the other parameters are as defined in claim 1, and also to their use in liquid-crystal mixtures, and also to liquid-crystal mixtures comprising these compounds and to liquid-crystal displays comprising these mixtures.Type: GrantFiled: January 10, 2002Date of Patent: March 28, 2006Assignee: Merck Patent GmbHInventors: Wolfgang Schmidt, Rainer Wingen, Barbara Hornung
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Patent number: 6972297Abstract: 2-(S)-hydroxymutilin carbamate derivatives of formula (I), in which R1 is a 5- or 6-membered optionally substituted heteroaryl group; and R2 is vinyl or ethyl, are useful in the treatment of bacterial infectionsType: GrantFiled: March 29, 2001Date of Patent: December 6, 2005Assignee: SmithKline Beecham p.l.c.Inventors: Gerald Brooks, Eric Hunt, Steven Howard
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Patent number: 6949557Abstract: The invention relates to the use of novel anthracene based compounds for the inhibition or prevention of the growth or multiplication of cancer cells, and to therapeutic compositions containing such compounds. The invention relates more specifically to the use of hydroanthracene based compounds for the inhibition and/or prevention of cancer of the colon, pancreas, prostate, lung, larynx, ovary, breast, glioblastoma, oral cavity, endothelial cells and leukemias. The agents of the invention form a distinct class, distinct from the anthracene, anthrone or anthraquinone derivatives.Type: GrantFiled: April 29, 2003Date of Patent: September 27, 2005Assignee: Dabur Research FoundationInventors: Asish Kumar Banerjee, Venkatachalam Sesha Giri, Rama Mukherjee, Kamal K. Kapoor, Gautam Desiraju, Manu Jaggi, Anu T. Singh, Sankar Kumar Dutta, Kalapatapu V. V. M. Sairam
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Patent number: 6872824Abstract: A fluorene-based pyrimidine-containing conjugated oligomer applied in six different layers in an OLED, respectively, used as an electron-transport emitting layer, an emitting layer, a host in the emitting layer, the ETL, a host in the electron-transport emitting layer, and a hole-blocking layer to upgrade light-emitting efficiency and regulate emitting color of the OLED.Type: GrantFiled: January 20, 2004Date of Patent: March 29, 2005Assignee: Echem Hightech Co., Ltd.Inventors: Ken Tsung Wong, Yuan Li Liao, Chung Chih Wu, Yu Ting Lin, Huo Hsien Chiang
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Publication number: 20040220197Abstract: The invention relates to the use of novel anthracene based compounds for the inhibition or prevention of the growth or multiplication of cancer cells, and to therapeutic compositions containing such compounds. The invention relates more specifically to the use of hydroanthracene based compounds for the inhibition and/or prevention of cancer of the colon, pancreas, prostate, lung, larynx, ovary, breast, glioblastoma, oral cavity, endothelial cells and leukemias. The agents of the invention form a distinct class, distinct from the anthracene, anthrone or anthraquinone derivatives.Type: ApplicationFiled: April 29, 2003Publication date: November 4, 2004Applicant: DABUR RESEARCH FOUNDATIONInventors: Asish Kumar Banerjee, Venkatachalam Sesha Giri, Rama Mukherjee, Kamal K. Kapoor, Gautam Desiraju, Manu Jaggi, Anu T. Singh, Sankar Kumar Dutta, Kalapatapu V.V.M. Sairam
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Publication number: 20040171628Abstract: The invention provides a compound of formula I wherein A, B, X, Y and R1 are as defined in the description, and a process for preparing them. The compounds of formula I are useful as pharmaceutical agents for the treatment of glaucoma and myopia.Type: ApplicationFiled: January 8, 2004Publication date: September 2, 2004Inventors: Rudolf Markstein, Peter Gull, Esteban Pombo Villar
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Publication number: 20040162430Abstract: This invention provides compounds and methods using them to provide neuroprotection and prevent or limit processes of neurodegeneration in mammals, including Alzheimer's Disease, Huntington's Disease, Parkinson's Disease, AIDS dementia, retinal disease, diabetic peripheral neuropathy, multiple sclerosis, stroke, acute thromboembolic stroke, focal ischemia, global ischemia, transient ischemic attack, ischemia resulting from surgery, head trauma, spinal trauma, hypoxia, fetal hypoxia, and neuroprotection.Type: ApplicationFiled: February 20, 2004Publication date: August 19, 2004Applicant: WyethInventors: Wayne E. Childers, Horace Fletcher, Magid A. Abou-Gharbia, John P. Yardley
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Patent number: 6756375Abstract: The invention provides for a non-steroidal compound having the formula wherein Re and ′Re are OH, optionally independently etherified or esterified; Z is —CH2— or —CH2CH2—; R1 is H, halogen, CF3, or (1C-4C)alkyl; R2, R3 and R4 are independently H, halogen, —CF3, —OCF3, (1C-8C)Alkyl, hydroxy, (1C-8C)alkyloxy, aryloxy, aryl(1C-8C)alkyl, halo(1C-8C)alkyl, —O(CH2)mX, wherein X is halogen or phenyl and m=2-4; —O(CH2)mNRaRb, —S(CH2)mNRaRb or —(CH2)mNRaRb, wherein m=2-4 and Ra, Rb are independently (1C-8C)alkyl, (2C-8C)alkenyl, (2C-8C)alkynyl, or aryl, optionally substituted with halogen, —CF3, —OCF3, —CN, —NO2, —OH, (1C-8C)alkoxy, aryloxy, carboxyl, (1C-8C)alkylthio, carboxylate, (1C-8C)alkyl, aryl, aryl(1C-8C)alkyl, halo(1C-8C)alkyl or Ra and Rb form a 3-8 membered ring structure, optionally substituted with halogen, —CF3, —OCF3, —CN, —NO2, hydroxy, hydroxy(1C-4C)aType: GrantFiled: July 24, 2003Date of Patent: June 29, 2004Assignee: Akzo Nobel N.V.Inventors: Gerrit Herman Veeneman, Hubert JanJozef Loozen, Jordi Mestres, Eduard Willem De Zwart
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Publication number: 20040110762Abstract: This invention provides compounds of formula 1, having the structure 1Type: ApplicationFiled: July 10, 2003Publication date: June 10, 2004Applicant: WYETHInventors: Dan M. Berger, Minu D. Dutia, Frenel F. DeMorin, Diane H. Boschelli, Dennis W. Powell, Hwei-Ru Tsou, Allan Wissner, Nan Zhang, Fei Ye, Biqi Wu
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Publication number: 20040106798Abstract: The invention relates to fluorinated fluorene derivatives of negative DC anisotropy, of the formula IType: ApplicationFiled: September 29, 2003Publication date: June 3, 2004Inventors: Matthias Bremer, Detlef Pauluth, Melanie Klasen-Memmer
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Patent number: 6737423Abstract: Substituted heterocyclo-norbornylaminoderivatives having: a) an exo-configuration nitrogen and an endo-fused five-membered ring or six-membered ring of the formula (I) or b) an exo-configuration nitrogen and an exo-fused five-membered ring or six-membered ring of the formula (I a), wherein Rn, Het, A, B and T have the meanings given in the claims. These compounds have a variety of uses. They can be used as antihypertensives, for the reduction or prevention of is chemically induced damage, as pharmaceuticals for surgical interventions, for the treatment of ischemia of the nervous system, including stroke and cerebral edema, for the treatment of ischemia due to shock and disturbed respiratory drive, for the treatment of snoring, as a laxative, as an agent against ectoparasites, for the prevention of gallstone formation, as an antiatherosclerotic, as an agent against diabetic late complications, cancers, fibrotic disorders, endothelial dysfunction, organ hypertrophy, and organ hyperplasia.Type: GrantFiled: December 18, 2001Date of Patent: May 18, 2004Assignee: Aventis Pharma Deutschland GmbHInventors: Uwe Heinelt, Hans-Jochen Lang, Klaus Wirth, Hans-Willi Jansen
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Publication number: 20040053943Abstract: The present invention is directed to novel compounds of Formula (I) for use in the treatment of diseases in a mammal, in which inappropriate, excessive or undesirable angiogenesis has occurred and/or where excessive Tie2 receptor activity has occurred.Type: ApplicationFiled: May 20, 2003Publication date: March 18, 2004Inventors: Jerry L. Adams, Deborah L. Bryan
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Publication number: 20040039006Abstract: (2S)-2-(Adamantan-1-ylmethoxycarbonylamino)-3-(4-(2-(1,4,5,6-tetrahydropyrimidin-2-ylcarbamoyl)ethyl)benzoylamino)propionic acid isopropyl ester, its preparation and its useType: ApplicationFiled: July 30, 2003Publication date: February 26, 2004Inventors: Aunschirwan Peyman, Theodor Wollmann, Gerhard Brejpohl, Jean-Francois Gourvest, Jean-Marie Ruxer, Thomas Gadek, Robert McDowell
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Publication number: 20040034223Abstract: The present invention relates to the preparation of synthons that are used to form modules that, in turn, are used to form two-dimensional close-packed planar arrays, referred to as nanomembranes. In a presently preferred embodiment, a nanomembrane herein constitutes a filter.Type: ApplicationFiled: February 7, 2002Publication date: February 19, 2004Applicant: CoValent Partners, LLC.Inventors: Timothy B. Karpishin, Josh Kriesel, Grant Merrill, Donald B. Bivin, Thomas H. Smith, Martin Stuart Edelstein
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Publication number: 20040014971Abstract: Polyarylcarboxamide compounds of formula (I) 1Type: ApplicationFiled: February 28, 2003Publication date: January 22, 2004Inventors: Lieven Meerpoel, Peter Walter Maria Roevens, Leo Jacobus Jozef Backx, Louis Jozef Elisabeth Van der Veken, Marcel Viellevoye
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Publication number: 20030222243Abstract: Fluorinated indenes and 1,7-dihydroindacenes of the general formulae (I) and (II) of negative dielectric anisotropy (&Dgr;&egr;<0) 1Type: ApplicationFiled: April 4, 2003Publication date: December 4, 2003Applicant: Merck Patent GmbHInventors: Lars Lietzau, Melanie Klasen-Memmer, Matthias Bremer
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Publication number: 20030166637Abstract: The present invention relates to substituted piperazine derivatives of general formula 1Type: ApplicationFiled: October 9, 2002Publication date: September 4, 2003Inventors: Thorsten Lehmann-Lintz, Armin Heckel, Leo Thomas, Michael Mark
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Publication number: 20030114674Abstract: 1 2-(S)-hydroxymutilin carbamate derivatives of formula (I), in which R1 is a 5- or 6-membered optionally substituted heteroaryl group; and R2 is vinyl or ethyl, are useful in the treatment of bacterial infections.Type: ApplicationFiled: October 4, 2002Publication date: June 19, 2003Inventors: Gerald Brooks, Eric Hunt, Steven Howard
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Publication number: 20030008889Abstract: The present invention provides novel aminoadamantane derivatives, methods of making the derivatives, compositions including the novel aminoadamantane derivatives, and methods for the treatment and prevention of neurological diseases using the derivatives and compositions.Type: ApplicationFiled: July 19, 2002Publication date: January 9, 2003Inventors: Yuqiang Wang, Wenqing Ye, James W. Larrick, Jonathan S. Stamler, Stuart A. Lipton
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Patent number: 6492355Abstract: The invention provides compounds of general formula in which m, A, R1 and Ar have the meanings defined in the specification; a process for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy.Type: GrantFiled: June 1, 2000Date of Patent: December 10, 2002Assignee: AstraZeneca ABInventors: Lilian Alcaraz, Mark Furber, Michael P. Mortimore
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Patent number: 6399620Abstract: There are described cycloalkyl derivatives of the formula (I) R1—Y—A—B—D—E—F—G (I) in which R1, Y, A, B, D, E, F and G have the meaning indicated herein, their preparation and their use as medicaments. The compounds according to the invention can be used as vitronectin receptor antagonists and as inhibitors of bone resorption.Type: GrantFiled: June 29, 2000Date of Patent: June 4, 2002Assignee: Aventis Pharma S.A.Inventors: Volkmar Wehner, Jochen Knolle, Hans Ulrich Stilz, Jean-Francois Gourvest, Denis Carniato, Thomas Richard Gadek, Robert McDowell, Robert Maurice Pitti, Sarah Catherine Bodary
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Patent number: 6288123Abstract: The present invention provides therapeutically useful substituted guanidines, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.Type: GrantFiled: June 5, 1995Date of Patent: September 11, 2001Assignee: Cambridge NeuroSciences, Inc.Inventors: Stanley M. Goldin, James B. Fischer, Andrew Gannett Knapp, N. Laxma Reddy, David Berlove, Graham J. Durant, Subbarao Katragadda, Lain-Yen Hu, Sharad Magar, Wenhong Fan, Elizabeth Yost, Jun Qing Guo
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Patent number: 6211189Abstract: There are provided novel compounds of formula (I) wherein A represents an aromatic carbocyclic ring or a 5- or 6-membered heterocyclic aromatic ring containing 1 to 3 heteroatoms which may be the same or different and are selected from O, N and S; X represents —(CH2)n— wherein n represents zero or 1; and R1, R2 and R3 are as defined in the specification, and pharmaceutically acceptable salts thereof, and enantiomers and tautomers thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of nitric oxide synthase and are thereby particularly useful in the treatment or prophylaxis of inflammatory disease and pain.Type: GrantFiled: May 31, 2000Date of Patent: April 3, 2001Assignee: AstraZeneca UK LimitedInventors: Peter Hamley, Austen Pimm, Alan Tinker