Tetramisole Per Se Or Salt Thereof (including Hydrogenated) Patents (Class 548/155)
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Patent number: 8889678Abstract: The present invention relates to acyl guanidine derivatives modulating the hedgehog protein signaling pathway to be used as drugs, in particular for treating diseases involving a tissue dysfunction associated with a deregulation of the hedgehog protein signaling pathway, as well as to pharmaceutical compositions containing same. The present invention also relates to novel acyl guanidine derivatives as such.Type: GrantFiled: July 19, 2010Date of Patent: November 18, 2014Assignees: Centre National de la Recherche Scientifique, Universite de StrasbourgInventors: Martial Ruat, Hélène Faure, Elisabeth Traiffort, Hermine Roudaut, André Mann, Angèle Schoenfelder, Maurizio Taddei, Fabrizio Manetti, Antonio Solinas
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Publication number: 20140315945Abstract: The present invention relates to azole compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.Type: ApplicationFiled: March 14, 2014Publication date: October 23, 2014Applicant: EPIZYME, INC.Inventors: John Emmerson Campbell, Kevin Wayne Kuntz
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Publication number: 20140221351Abstract: The present invention relates to novel bis-sulfonamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.Type: ApplicationFiled: April 8, 2014Publication date: August 7, 2014Applicant: ALLERGAN, INC.Inventors: HAIQING YUAN, RICHARD L. BEARD, XIAOXIA LIU, JOHN E. DONELLO, VEENA VISWANATH, MICHAEL E. GARST
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Publication number: 20140051682Abstract: The present invention relates to novel bis-sulfonamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.Type: ApplicationFiled: September 24, 2013Publication date: February 20, 2014Applicant: ALLERGAN, INC.Inventors: Haiqing Yuan, Richard L. Beard, Michael E. Garst, Xiaoxia Liu, John E. Donello, Veena Viswanath
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Patent number: 8586571Abstract: The present invention relates to wherein each symbol is as defined in the specification. The compound of the present invention has a superior RBP4-lowering action, and is useful as a medicament for the prophylaxis or treatment of disease and condition mediated by increased RBP4.Type: GrantFiled: October 17, 2008Date of Patent: November 19, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Shizuo Kasai, Tomohiro Kaku, Masahiro Kamaura
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Publication number: 20130296342Abstract: The present invention provides pharmaceutical compositions containing benzene compound(s) represented by General Formula (1) below and, particularly, LPL-activating compositions for use in hyperlipidemia therapeutic and preventive agents, anti-obesity agents, and the like: wherein R1, R2, R3 and R4 are as defined in the specification.Type: ApplicationFiled: June 28, 2013Publication date: November 7, 2013Applicant: OTSUKA PHARMACEUTICAL FACTORY, INC.Inventors: Irina NEAGU, Michael OHLMEYER, Vidyadhar M. PARADKAR, Kurt W. SAIONZ, Koushi IWATA, Takashi OKAMURA, Tadao SHIBUTANI
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Publication number: 20130225591Abstract: The present invention is directed to novel kinase inhibitors of general formula (I) and pharmaceutically acceptable salts thereof, and to the use of the kinase inhibitors of general formula (I) for treating diseases or disorders in which tau phosphorylation and cell cycle regulation is implicated, such as Alzheimer's Disease and cancer.Type: ApplicationFiled: September 14, 2010Publication date: August 29, 2013Inventors: Michelle R. Machacek, Sean P. Ahearn, Eric Romeo, Tony Siu, Stephanie Chichetti, Gabriela de Almeida, Alexey A. Rivkin
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Patent number: 8318928Abstract: The present invention provides transient receptor potential vanilloid (TRPV) modulators of formula (I). In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPV3.Type: GrantFiled: December 11, 2009Date of Patent: November 27, 2012Assignee: Glenmark Pharmaceuticals, S.A.Inventors: Sachin Sundarlal Chaudhari, Thomas Abraham, Ashok Bhausaheb Kadam, Sachin Vasantrao Dhone, Suresh Mahadev Kadam, Neelima Khairatkar-Joshi, Vidya Ganapati Kattige
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Publication number: 20120196865Abstract: The present invention relates to acyl guanidine derivatives modulating the hedgehog protein signaling pathway to be used as drugs, in particular for treating diseases involving a tissue dysfunction associated with a deregulation of the hedgehog protein signaling pathway, as well as to pharmaceutical compositions containing same. The present invention also relates to novel acyl guanidine derivatives as such.Type: ApplicationFiled: July 19, 2010Publication date: August 2, 2012Applicants: UNIVERSITE DE STRASBOURG, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUEInventors: Martial Ruat, Hélène Faure, Elisabeth Traiffort, Hermine Roudaut, André Mann, Angèle Schoenfelder, Maurizio Taddei, Fabrizio Manetti, Antonio Solinas
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Publication number: 20120088771Abstract: This invention relates generally to the field of mineralization, and specifically to the role of TNAP in regulating the levels of extracellular inorganic pyrophosphate. The invention provides methods for modulating the activity of TNAP activity; methods for screening for modulators of TNAP activity; modulators of TNAP activity; and methods for treating pathologic conditions known of suspected to be affected by modulation of TNAP activity.Type: ApplicationFiled: October 11, 2011Publication date: April 12, 2012Inventor: Jose Luis Millan
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Publication number: 20120022254Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: September 29, 2011Publication date: January 26, 2012Applicant: Sirtris Pharmaceuticals, Inc.Inventors: Joseph J. Nunes, Jill Milne, Jean Bemis, Roger Xie, Chi B. Vu, Pui Yee Ng, Jeremy S. Disch
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Publication number: 20110263662Abstract: The invention relates to 1,2-diamido-ethylene derivatives of the formula (I) wherein R1, R2, R3, and A are as described in the description and their use as medicaments, especially as orexin receptor antagonists.Type: ApplicationFiled: August 14, 2008Publication date: October 27, 2011Inventors: Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, Thierry Sifferlen
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Patent number: 7994336Abstract: The invention relates to novel azetidine compounds of formula (I), wherein R1, R2, and X are as described in the description and their use as orexin receptor antagonists.Type: GrantFiled: August 15, 2007Date of Patent: August 9, 2011Assignee: Actelion Pharmaceuticals Ltd.Inventors: Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, Thierry Sifferlen
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Publication number: 20110150827Abstract: Provided herein are 5,5-fused heteroarylene hepatitis C virus inhibitor compounds, for example, of Formula I, IA, or IB, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.Type: ApplicationFiled: December 17, 2010Publication date: June 23, 2011Applicant: Idenix Pharmaceuticals, Inc.Inventors: Cyril B. Dousson, David Dukhan, Christophe Claude Parsy, Claire Pierra, Francois-Rene Alexandre, Guillaume Brandt, Daniel Da Costa, Houcine Rahali, Jean-Laurent Paparin, Michel Derock, Thierry Convard, Dominique Surleraux
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Patent number: 7960568Abstract: The present invention relates to heterocyclyl-substituted sulfonamides with 5-HT6 receptor affinity, and compositions thereof, and the use of said compounds for the treatment or prophylaxis of various disorders.Type: GrantFiled: January 30, 2008Date of Patent: June 14, 2011Assignee: Laboratorios Del Dr. Esteve, S.A.Inventor: José-Luis Diaz-Fernández
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Publication number: 20110065728Abstract: The present invention provides pharmaceutical compositions containing benzene compound(s) represented by General Formula (1) below and, particularly, LPL-activating compositions for use in hyperlipidemia therapeutic and preventive agents, anti-obesity agents, and the like: wherein R1, R2, R3 and R4 are as defined in the specification.Type: ApplicationFiled: May 14, 2008Publication date: March 17, 2011Applicant: OTSUKA PHARMACEUTICAL FACTORY, INC.Inventors: Irina Neagu, Michael Ohlmeyer, Vidyadhar M. Paradkar, Kurt W. Saionz, Koushi Iwata, Takashi Okamura, Tadao Shibutani
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Publication number: 20110009461Abstract: The invention relates to 2-aza-bicyclo[3.3.0]octane derivatives of Formula (I) wherein A, B, 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: July 25, 2008Publication date: January 13, 2011Inventors: Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, Thierry Sifferlen, Daniel Trachsel
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Publication number: 20110003806Abstract: This invention provides compounds of formula IA or IB: wherein R1, R2, G1 and HY are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: January 28, 2010Publication date: January 6, 2011Applicants: Millennium Pharmaceuticals, Inc., Takeda Pharmaceutical Company LimitedInventors: Masaaki Hirose, Steven P. Langston, Hirotake Mizutani, Stepan Vyskocil
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Publication number: 20100292206Abstract: The present invention relates to wherein each symbol is as defined in the specification. The compound of the present invention has a superior RBP4-lowering action, and is useful as a medicament for the prophylaxis or treatment of disease and condition mediated by increased RBP4.Type: ApplicationFiled: October 17, 2008Publication date: November 18, 2010Inventors: Shizuo Kasai, Tomohiro Kaku, Masahiro Kamaura
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Publication number: 20100261758Abstract: Compounds of Formula (I) wherein R1 is aryl, cyclohexyl or heterocyclyl, or (C1-4)alkyl substituted by aryl, cyclohexyl or heterocyclyl, R2 is defined heterocyclyl, R3 is alkyl, aryl, cyclohexyl or heterocyclyl, or (C1-4)alkyl substituted by aryl, cyclohexyl or heterocyclyl, R4 is H or alkyl, or R3 and R4 together with the carbon atom to which they are attached are cycloalkyl fused with aryl, and their use as pharmaceuticals.Type: ApplicationFiled: March 28, 2007Publication date: October 14, 2010Applicant: NOVARTIS AGInventors: Luca Arista, Klemens Hogenauer, Niko Schmiedeberg, Gudrun Werner, Herbert Jaksche
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Publication number: 20100152192Abstract: The present invention provides transient receptor potential vanilloid (TRPV) modulators of formula (I). In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPV3.Type: ApplicationFiled: December 11, 2009Publication date: June 17, 2010Applicant: Glenmark Pharmaceuticals S.AInventors: Sachin Sundarlal Chaudhari, Abraham Thomas, Ashok Bhausaheb Kadam, Sachin Vasantrao Dhone, Suresh Mahdadev Kadam, Neelima Khairatkar-Joshi, Vidya Ganapati Kattige
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Publication number: 20100076036Abstract: The present invention relates to heterocyclyl-substituted sulfonamides with 5-HT6 receptor affinity, and compositions thereof, and the use of said compounds for the treatment or prophylaxis of various disorders.Type: ApplicationFiled: January 30, 2008Publication date: March 25, 2010Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventor: Jose-Luis Diaz-Fernandez
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Publication number: 20100069378Abstract: The present invention refers to new indanyl sulphonamide compounds with general formula (I), as well as to their preparation procedure, their application as medicine and the pharmaceuticals composition which they are made up of. The new compounds of formula (I) show affinity for 5-HT6 receptors and are, therefore, effective for treating diseases mediated by these receptors.Type: ApplicationFiled: July 25, 2007Publication date: March 18, 2010Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Jordi Frigola-Constansa, Joerg Holenz, Ramon Merce-Vidal, Maria de las Ermitas Alcalde-Pais, Maria de les Neus Mesquida-Estevez, Sara Lopez-Perez
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Publication number: 20100004299Abstract: The present invention relates to derivatives of imidazo[2,1-b]thiazoles of formula I, in which R, R1 to R3 and n have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired.Type: ApplicationFiled: May 15, 2009Publication date: January 7, 2010Applicant: SANOFI-AVENTISInventors: Gerhard ZOLLER, Hartmut STROBEL, David William WILL, Paulus WOHLFART
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Publication number: 20090312310Abstract: There is provided a novel compound that inhibits interaction between murine double minute 2 (Mdm2) protein and p53 protein and exhibits anti-tumor activity. The present invention provides an imidazothiazole derivative represented by the following formula (1) having various substituents that inhibits interaction between Mdm2 protein and p53 protein and exhibits anti-tumor activity: wherein R1, R2, R3, R4, and R5 in the formula (1) each has the same meaning as defined in the specification.Type: ApplicationFiled: June 11, 2009Publication date: December 17, 2009Inventors: Haruko Kawato, Masaki Miyazaki, Yuuichi Sugimoto, Hiroyuki Naito, Tooru Okayama, Tsunehiko Soga, Kouichi Uoto
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Publication number: 20090291948Abstract: Acyl sulfonamide, peri-substituted, fused bicyclic ring compounds useful for the treatment or prophylaxis of a prostaglandin-mediated disease or condition are disclosed.Type: ApplicationFiled: August 3, 2009Publication date: November 26, 2009Applicant: DECODE GENETICS EHFInventors: Jasbir Singh, Mark E. Gurney, Georgeta Hategan, Peng Yu, David Zembower, Nian Zhou
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Publication number: 20090142347Abstract: This invention relates generally to the field of mineralization, and specifically to the role of TNAP in regulating the levels of extracellular inorganic pyrophosphate. The invention provides methods for modulating the activity of TNAP activity; methods for screening for modulators of TNAP activity; modulators of TNAP activity; and methods for treating pathologic conditions known of suspected to be affected by modulation of TNAP activity.Type: ApplicationFiled: September 29, 2005Publication date: June 4, 2009Applicant: THE BURNHAM INSTITUTE FOR MEDICAL RESEARCHInventor: José Luis Millan
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Publication number: 20090011975Abstract: The invention provides a method of inhibiting cell death in a mammal. The method comprises administering to a mammal an effective amount of a composition comprising a cell protection factor covalently linked to a bone targeting agent via a linkage that is cleaved under physiological conditions, whereby the cell protection factor is released from the bone targeting agent in vivo to inhibit cell death. The invention further provides a compound comprising a cell protection factor covalently attached to a bone targeting agent via a linker that is cleaved under physiological conditions.Type: ApplicationFiled: July 31, 2008Publication date: January 8, 2009Applicant: Semafore Pharmaceuticals Inc.Inventors: Joseph R. Garlich, Donald L. Durden, Tim C. Smith
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Publication number: 20090005399Abstract: Substituted imidazo[2,1-b]thiazole compounds corresponding to formula I, a method for producing them, pharmaceutical compositions containing them, and the use thereof for regularing mGluR5 receptors, or for treating or inhibiting disorders or disease states at least partially mediated by mGluR5 receptor such as pain, anxiety attacks, drug or alcohol dependency, and others.Type: ApplicationFiled: September 9, 2008Publication date: January 1, 2009Applicant: Gruenenthal GmbHInventors: Sven KUEHNERT, Saskia ZEMOLKA, Michael HAURAND, Klaus SCHIENE
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Publication number: 20080287511Abstract: The present invention relates to the novel anthelmintic compound tetrahydro-furan-2-carboxylic acid-[3-(2,3,5,6-tetrahydro-imidazo[2,1-b]thiazol-6-yl)-phenyl]-amide and the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, as well as pharmaceutical compositions comprising said novel compound, processes for preparing said compound and compositions, and the use thereof as a medicine, in particular in treatment, control and prevention of endo- and ectoparasite infections in warm-blooded animals.Type: ApplicationFiled: January 26, 2006Publication date: November 20, 2008Inventors: Jan Heeres, Paulus Joannes Lewi, Paul Adriaan Jan Janssen, Kathleen Marie Jeanne Alice Vlaminck, Pierre Josef Hektor Valere Ottevaere, Oscar Franz Joseph Vanparijs, Frank Xavier Jozef Herwig Arts
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Publication number: 20080167475Abstract: The present invention relates to compounds represented by formula (1) and a process for producing the same. The use of these compounds can realize the production of carbapenem derivatives having potent antimicrobial activity and a wide antimicrobial spectrum in a safe and cost-effective manner.Type: ApplicationFiled: February 15, 2008Publication date: July 10, 2008Inventors: Toshiro Sasaki, Takashi Ando, Yasuo Yamamoto, Takahiro Imai, Dai Kubota, Katsuhiko Noguchi, Nobuyuki Hori, Eiki Shitara, Kunio Atsumi, Shohei Yasuda
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Publication number: 20080161341Abstract: The present invention is directed to novel compounds of formula (I) wherein the variables are as defined herein. The compounds of formula (I) are useful as kinase inhibitors and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, cancers.Type: ApplicationFiled: October 5, 2007Publication date: July 3, 2008Inventors: David J. Calderwood, Kristine E. Frank, David W. Borhani, Heather M. Davis, Nathan S. Josephsohn, Barbara S. Skinner
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Patent number: 7288559Abstract: The present invention is directed to compounds that are antagonists of CGRP receptors and that are useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: March 10, 2004Date of Patent: October 30, 2007Assignee: Merck + Co, Inc.Inventors: Ian M. Bell, Steven N. Gallicchio, Craig A. Stump, C. Blair Zartman
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Patent number: 7153873Abstract: Salts of a bicyclic, N-acylated imidazo-3-amine or an imidazo-5-amine of the formula: addition products thereof with acids, and methods for preparing the salts and addition products. Also disclosed are pharmaceutical compositions comprising the same and methods using the pharmaceutical compositions for the treatment or prophylaxis of pain, drug or alcohol abuse, diarrhoea, gastritis, ulcers, urinary incontinence, depression, narcolepsy, overweight, asthma, glaucoma, tinnitus, itching, hyperkinetic syndrome, epilepsy, or schizophrenia, for inducing anesthesia, and for anxiolysis.Type: GrantFiled: June 6, 2006Date of Patent: December 26, 2006Assignee: Gruenenthal GmbHInventors: Matthias Gerlach, Corinna Sundermann
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Patent number: 6177454Abstract: An amide derivative represented by the following general formula (I) or a salt thereof and a pharmaceutical composition containing the amide derivative and a pharmaceutically acceptable vehicle. The symbols in the formula have the following meanings wherein A: heteroarylene; X: bond, O, S, —NR5—, —NR5CO—, —NR5CONH—, —NR5SO2— or —NR5C(═NH)NH—; R1: —H, -optionally substituted lower alkyl, -optionally substituted aryl, -optionally substituted heteroaryl or -optionally substituted cycloalkyl; R2a, R2b: —H or -lower alkyl, which may be the same or different; R3: —H or -lower alkyl; R4a, R4b: —H or —OH, which may be the same different, or R4a and R4b are taken together to form ═O or ═N—O—lower alkyl; and R5: —H or -lower alkyl.Type: GrantFiled: February 29, 2000Date of Patent: January 23, 2001Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Tatsuya Maruyama, Kenichi Onda, Masahiko Hayakawa, Takumi Takahashi, Takayuki Suzuki, Tetsuo Matsui
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Patent number: 5384325Abstract: Compounds based on heterobicyclic derivatives displaying fungicidal activity, having the general formula (I): ##STR1##Type: GrantFiled: April 25, 1994Date of Patent: January 24, 1995Assignee: Isagro S.r.l.Inventors: Giovanni Camaggi, Lucio Filippini, Marilena Gusmeroli, Raul Riva, Carlo Garavaglia, Ernesto Signorini, Mario Ferri
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Patent number: 5008390Abstract: 6-Aryl-2,3-dihydroimidazo[2,1-b]thiazoles and corresponding thiazines act as nucleophiles, either directly or in the form of Grignard reagents, with N-acylpyridinium salts to produce new 6-aryl-5-(N-acyl-1,4-dihydro-4-pyridyl)-2,3-dihydroimidazo-[2,1-b]thiazole s and corresponding thiazines. These are oxidized to give the corresponding pyridyl-substituted imidazo[2,1-b]thiazoles and thiazines, which are active as inhibitors of the 5-lipoxygenase pathway of arachidonic acid metabolism.Type: GrantFiled: November 3, 1988Date of Patent: April 16, 1991Assignee: SmithKline Beckman CorporationInventors: Paul E. Bender, Ivan Lantos, Michael A. McGuire, Lendon N. Pridgen, Herbert B. Winicov
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Patent number: 4803279Abstract: 6-Aryl-2,3-dihydroimidazo[2,1-b]thiazoles and corresponding thiazines act as nucleophiles, either directly or in the form of Grignard reagents, with N-acylpyridinium salts to produce new 6-aryl-5-(N-acyl-1,4-dihydro-4-pyridyl)-2,3-dihydroimidazo-[2,1-b]thiazole s and corresponding thiazines. These are oxidized to give the corresponding pyridyl-substituted imidazo[2,1-b]thiazoles and thiazines, which are active as inhibitors of the 5-lipoxygenase pathway of arachidonic acid metabolism.Type: GrantFiled: April 28, 1986Date of Patent: February 7, 1989Assignee: SmithKline Beckman CorporationInventors: Paul E. Bender, Ivan Lantos, Michael A. McGuire, Lendon N. Pridgen, Herbert B. Winicov
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Patent number: 4672126Abstract: A process for isolating levamisole or a therapeutically acceptable acid addition salt thereof from tetramisole or an acid addition salt thereof by precipitating levamisole. L-N-[(4-methoxyphenyl)sulfonyl]-glutamic acid (salt) and converting the diastereomeric salt into levamisole or a suitable acid addition salt thereof.Type: GrantFiled: October 1, 1984Date of Patent: June 9, 1987Assignee: Janssen Pharmaceutica, N.V.Inventors: Guido J. L. Van der Veken, Eric J. Guns, Albert L. A. Willemsens
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Patent number: 4632927Abstract: A class of bicyclic nitrogen heterocyclic ether and thioether compounds exhibiting pharmacological activity including cytoprotective, H.sub.2 -antagonist, anti-secretory and anti-ulcerogenic activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions are disclosed.Type: GrantFiled: March 20, 1984Date of Patent: December 30, 1986Assignee: William H. Rorer, Inc.Inventors: Henry F. Campbell, Donald E. Kuhla, William L. Studt, Stuart A. Dodson
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Patent number: 4620009Abstract: A process for the manufacture of 1-(2-alkoxyethyl)-4-phenyl-4-imidazolin-2-ones, 1-(2-alkoxyethyl)-4-phenyl-2-imidazolidones, 1-(2-alkoxyethyl)-4-phenyl-imidazolidine-2-thiones, certain of the corresponding 1-(2-hydroxyethyl) derivatives and their 3-acylated derivatives, and certain related compounds which are all useful as intermediates in a new process for the manufacture of tetramisole, dl-2,3,5,6-tetrahydro-6-phenylimidazo-[2,1-b]thiazole, and its derivatives. The compound tetramisole is useful as an anthelmintic.Type: GrantFiled: October 1, 1981Date of Patent: October 28, 1986Assignee: Cyanamid Agricultural de Puerto Rico, Inc.Inventors: Sivaraman Raghu, Arthur K. Hoffmann, Balwant Singh
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Patent number: 4618618Abstract: The invention concerns novel compounds selected from D,L-2,3,5,6-tetrahydro-6-phenylimidazo[2,1-b]-thiazolium 4-cyano-2-iodo-6-nitrophenoxide and L-2,3,5,6-tetrahydro-6-phenylimidazo[2,1-b]thiazolium 4-cyano-2-iodo-6-nitrophenoxide. The compounds are anthelmintics effective against both nematodes and trematodes and in further embodiments the invention provides processes for the preparation of the compounds of the invention, compositions comprising as active ingredient the compounds of the invention and processes for killing helminths using the compounds of the invention.Type: GrantFiled: December 28, 1984Date of Patent: October 21, 1986Inventor: Errol J. McGarry
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Patent number: 4376769Abstract: Disclosed herein are novel tetrahydro imidazo thiazoles, tetrahydro imidazo thiazines, hexahydro imidazo thiazepines and hexahydro imidazo thiazocines, intermediates for the preparation thereof, methods of using the compounds as anti-inflammatory agents and methods of using an intermediate thereof as anti-secretory agents to relieve the symptoms of gastric distress.Type: GrantFiled: June 19, 1981Date of Patent: March 15, 1983Assignee: Schering CorporationInventor: Sherlock Margaret H.
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Patent number: 4370482Abstract: A process for the manufacture of 1-(2-alkoxyethyl)-4-phenyl-4-imidazolin-2-ones, 1-(2-alkoxyethyl)-4-phenyl-2-imidazolidones, 1-(2-alkoxyethyl)-4-phenyl-imidazolidine-2-thiones, certain of the corresponding 1-(2-hydroxyethyl) derivatives, and their 3-acylated derivatives, and certain related compounds which are all useful as intermediates in a new process for the manufacture of the anthelmintic levamisole, (-)-2,3,5,6-tetrahydro-6-phenylimidazo-[2,1-b]thiazols, and its derivatives through conventional resolution procedures. The new process also permits the direct manufacture of optically active 1-(2-alkoxyethyl)-4-phenyl-2-imidazolidone and their 3-acylated derivatives, optically active 1-(2-alkoxyethyl)-4-phenylimidazolidine-2-thiones, and levamisole, the levorotatory isomer of tetramisole, using catalytic amounts of a chiral reducing agent, with the elimination of conventional resolution procedures.Type: GrantFiled: October 28, 1981Date of Patent: January 25, 1983Assignee: American Cyanamid Co.Inventors: Sivaraman Raghu, Arthur K. Hoffmann, Balwant Singh
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Patent number: 4314079Abstract: Processes for reacting arylvinyl oxides and alkoxyethylamines to provide novel N-substituted alkoxyethylamines; processes for reacting the novel N-substituted amines with nitriles to provide novel amidoamines; processes for preparing novel diamines from the amidoamines, together with the novel nitrogen-containing products so produced, such products being useful for the preparation of various imidazothiazoles including tetramisole.Type: GrantFiled: May 21, 1980Date of Patent: February 2, 1982Assignee: American Cyanamid CompanyInventor: Sivaraman Raghu
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Patent number: 4310672Abstract: A process for the manufacture of 1-(2-alkoxyethyl)-4-phenyl-4-imidazolin-2-ones, 1-(2-alkoxyethyl)-4-phenyl-2-imidazolidones, 1-(2-alkoxyethyl)-4-phenyl-imidazolidine-2-thiones, certain of the corresponding 1-(2-hydroxyethyl) derivatives and their 3-acylated derivatives, and certain related compounds which are all useful as intermediates in a new process for the manufacture of tetramisole, di-2,3,5,6-tetrahydro-6-phenylimidazo-[2,1-b]thiazole, and its derivatives. The compound tetramisole is useful as an anthelmintic.Type: GrantFiled: March 17, 1980Date of Patent: January 12, 1982Assignee: American Cyanamid Co.Inventors: Sivaraman Raghu, Arthur K. Hoffmann, Balwant Singh
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Patent number: 4282225Abstract: Thiazole derivatives of general formula (I) ##STR1## in which n is 1 or 2 and Ar represents a phenyl radical unsubstituted or substituted by one or more substituents selected from halogen atoms, the radical CF.sub.3, the phenyl radical straight or branched chain alkyl radicals having 1 to 4 carbon atoms, and cycloalkyl radicals having 3 to 6 carbon atoms, and their pharmaceutically acceptable acid addition salts are useful in therapy as anti-depressive agents. They are prepared by reacting the thiazole ##STR2## with a ketone X--CH.sub.2 --CO--CH.sub.2 O--Ar (III) (X is a leaving group, such as halogen).Type: GrantFiled: February 4, 1980Date of Patent: August 4, 1981Assignee: SynthelaboInventor: Dennis C. H. Bigg
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Patent number: 4267339Abstract: There are disclosed certain novel imidazo(2,1-b)thiazoles, their physiologically acceptable acid addition--or quaternary ammonium salts and a process for their preparation. Said compounds show a good anti-diabetic activity.Type: GrantFiled: December 28, 1976Date of Patent: May 12, 1981Assignee: Plantex Ltd.Inventor: Enzo Tedeschi
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Patent number: 4245102Abstract: Processes for reacting aryl vinyl compounds, nitriles, and halogens to provide imidoyl halides; processes for preparing amidine hydrohalides from the imidoyl compounds; processes for producing novel imidazolines from the amidine hydrohalides; processes for preparing novel amidoamines from the imidazolines; processes for preparing novel diamines from the amidoamines, together with novel nitrogen-containing products so produced, such products being useful for the production of various imidazothiazoles including tetramisole.Type: GrantFiled: August 2, 1979Date of Patent: January 13, 1981Assignee: American Cyanamid CompanyInventor: Sivaraman Raghu
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Patent number: 4245103Abstract: Processes for reacting arylvinyl oxides and alkoxyethylamines to provide novel N-substituted alkoxyethylamines; processes for reacting the novel N-substituted amines with nitriles to provide novel amidoamines; processes for preparing novel diamines from the amidoamines, together with the novel nitrogen-containing products so produced, such products being useful for the preparation of various imidazothiazoles including tetramisole.Type: GrantFiled: August 2, 1979Date of Patent: January 13, 1981Assignee: American Cyanamid CompanyInventor: Sivaraman Raghu