Ring Nitrogen Is Shared By The Two Cyclos Patents (Class 548/154)
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Publication number: 20100184772Abstract: The present invention relates to substituted pyrazoline compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.Type: ApplicationFiled: October 10, 2007Publication date: July 22, 2010Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Helmut H. Buschmann, Antonio Torrens-Jover, Josef Mas-Prio, Susana Yenes-Minguez
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Publication number: 20100048555Abstract: Compounds of formula (I): are inhibitors of MARK, and hence useful for treatment of disorders involving 10 hyperphosphorylation of tau.Type: ApplicationFiled: July 20, 2007Publication date: February 25, 2010Inventors: Ian Churcher, Victoria Alexandra Doughty, Peter Hunt, Matthew Stanton
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Publication number: 20090259049Abstract: A compound represented by the following formula (I), or salt thereof exhibits excellent CRF receptor antagonism, and sufficient pharmacological activity, safety and pharmacokinetic properties as a drug. wherein R1 represents the formula -A11-A12; R2 represents tetrahydrofurylmethyl, tetrahydropyranylmethyl or tetrahydropyranyl; A11 represents a single bond, methylene or 1,2-ethylene; A12 represents C1-6 alkyl, C3-6 cycloalkyl or C3-6 cycloalkyl having methyl; R3 represents methoxy, cyano, cyclobutyloxymethyl, methoxymethyl or ethoxymethyl; and R4 represents methoxy or chlorine.Type: ApplicationFiled: April 9, 2009Publication date: October 15, 2009Applicant: Eisai R & D Management Co., Ltd.Inventors: Hisashi Shibata, Kodo Shikata, Akira Inomata, Kogyoku Shin, Taro Terauchi, Yoshinori Takahashi, Minako Hashizume, Kunitoshi Takeda
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Publication number: 20090221645Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof, exhibit 5-HT1A agonism in addition to noradrenaline reuptake inhibition and optionally also 5-HT reuptake inhibition are useful for the treatment of obesity.Type: ApplicationFiled: February 8, 2006Publication date: September 3, 2009Inventors: Oscar Barba, Graham John Dawson, Thomas Martin Krulle, Robert John Rowley, Donald Smyth, Gerard Hugh Thomas
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Patent number: 7563901Abstract: 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: GrantFiled: February 15, 2008Date of Patent: July 21, 2009Assignee: Meiji Seika Kaisha, Ltd.Inventors: 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: 20090163547Abstract: The present invention makes reference to new indene derivatives with general formula (I), as well as to their preparation procedures, their application as medicament and the pharmaceutical compositions containing them. 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: November 7, 2006Publication date: June 25, 2009Inventors: Maria De Las Ermitas Alcalde-Pais, Jordi Frigola-Constansa, Joerg Holenz, Ramon Merce-Vidal, Maria De Les Neus Mesquida-Estevez, Sara Lopez-Perez
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Publication number: 20090136448Abstract: Anti-viral agents of compounds of Formula (I): wherein A, R1, R2 and R3 are as defined in the specification, processes for their preparation and their use in HCV treatment are provided.Type: ApplicationFiled: December 20, 2006Publication date: May 28, 2009Inventors: John Andrew Corfield, Richard Martin Grimes, David Harrison, Charles David Hartley, Peter David Howes, Joelle Le, Malcolm Lees Meeson, Jacqueline Elizabeth Mordaunt, Pritom Shah, Martin John Slater, Gemma Victoria White
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Patent number: 7524951Abstract: 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: GrantFiled: December 15, 2003Date of Patent: April 28, 2009Assignee: Meiji Seika Kaisha, Ltd.Inventors: Toshiro Sasaki, Takashi Ando, Yasuo Yamamoto, Takahiro Imai, Dai Kubota, Katsuhiko Noguchi, Nobuyuki Hori, Eiki Shitara, Kunio Atsumi, Shohei Yasuda
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Patent number: 7498327Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.Type: GrantFiled: June 22, 2005Date of Patent: March 3, 2009Assignee: WyethInventors: Youchu Wang, Chia-Cheng Shaw, Ronald Charles Bernotas, Chung-Chiee Paul Wang, Ping Cai, Zhi Wang
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Publication number: 20090048271Abstract: Novel compounds having a fused bicyclic heteroaromatic ring system substituted with a heteroaryl five-membered ring are disclosed. The compounds inhibit growth of a variety of types of cancer cells, and are thus useful for treating cancer. Efficacy of these compounds is demonstrated with a system for monitoring cell growth/migration, which shows they are potent inhibitors of growth and/or migration of cancer cells. In addition, compounds of the invention were shown to stop growth of tumors in vivo, and to reduce the size of tumors in vivo. Compositions comprising these compounds, and methods to use these compounds and compositions for treatment of cancers, are disclosed.Type: ApplicationFiled: July 17, 2008Publication date: February 19, 2009Inventors: Haoyun An, Biao Xi, Yama Abassi, Xiaobo Wang, Xiao Xu
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Publication number: 20090005417Abstract: The present invention relates to substituted indazolyl sulfonamide and 2,3-dihydroindolyl sulfonamide compounds of general formula I, a process for their preparation, medicaments comprising said substituted indazolyl sulfonamide and 2,3-dihydro-indolyl sulfonamide compounds as well as the use of said substituted indazolyl sulfonamide and 2,3-dihydro-indolyl sulfonamide compounds for the preparation of medicaments, which are particularly suitable for the prophylaxis and/or treatment of disorders or diseases that are at least partially mediated via 5-HT6 receptors.Type: ApplicationFiled: December 29, 2005Publication date: January 1, 2009Applicant: LABORATORIOS DEL DR. ESTEVE S.A.Inventors: Ramon Merce Vidal, Xavier Codony-Soler, Alberto Dordal-Zueras
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Publication number: 20080249146Abstract: The present invention relates to compounds of the formula (I), wherein R1, R2, A, B, D, E, F, G and Ar are as defined herein, and pharmaceutically acceptable salts thereof, useful in the prevention and treatment of hepatitis C infections.Type: ApplicationFiled: July 14, 2005Publication date: October 9, 2008Inventors: Immacolata Conte, Jose Ignacio Martin Hernando, Savina Malancona, Jesus Maria Ontoria Ontoria, Ian Stansfield
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Patent number: 7419993Abstract: The invention relates to triazolo-thiazole analogues of epothilone A and epothilone B.Type: GrantFiled: February 9, 2005Date of Patent: September 2, 2008Assignee: Helmholtz Center of Infection Research GmbHInventors: Gerhard Hoefle, Nicole Glaser
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Publication number: 20080114164Abstract: The present invention relates to compounds of formula (I) and a process for producing the same. In formula (I), X represents a halogen atom, and R1 represents group —COR2 wherein R2 represents group OM or C1-12 alkyloxy wherein M represents a hydrogen atom, an alkali metal, an alkaline earth metal, or quaternary ammonium. The use of this compound as a synthetic intermediate can realize the production of carbapenem derivatives having potent antimicrobial activity in an efficient and safe manner at low cost.Type: ApplicationFiled: January 19, 2006Publication date: May 15, 2008Inventors: Eiki Shitara, Kunio Atsumi, Keiichi Ajito, Shinya Ikeda, Tadashi Katoh, Munenori Inoue, Mari Nakatani
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Patent number: 7351481Abstract: The present invention is related to an imidazole ring-containing compound and an organic electroluminescence (EL) display device using the same. In particular, the imidazole ring-containing compound may be used alone or in combination with a dopant as a material for organic films such as an electroluminescent layer. The organic EL display device using an organic film made of the imidazole ring-containing compound has improved characteristics such as luminance, efficiency, driving voltage, and color purity.Type: GrantFiled: October 6, 2004Date of Patent: April 1, 2008Assignee: Samsung SDI Co., Ltd.Inventors: Seok-Jong Lee, Young-Kook Kim, Seok-Hwan Hwang, Seung-Gak Yang, Hee-Yeon Kim, Young-Rag Do, Joo-Han Song
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Patent number: 7351732Abstract: New cycloalkanedione derivatives that are serotonin (5-hydroxytriptamine, 5-HT) 5-HT1A receptor subtype agonists and, consequently, they are useful in the treatment of pathological states for which an agonist of these receptors is indicated. They are particularly useful as neuroprotective agents, of special interest in the treatment and prophylaxis of cerebral damage produced by traumatic or ischemic stroke.Type: GrantFiled: July 29, 2003Date of Patent: April 1, 2008Assignee: Schwarz Pharma S.L.Inventors: Joaquin Del Río Zambrana, Diana Frechilla Manso, M. Luz López Rodríguez, Bellinda Benhamú Salama, José Ángel Fuentes Cubero, Mercedes Delgado Wallace
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Patent number: 7345178Abstract: 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 benfit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: GrantFiled: August 4, 2006Date of Patent: March 18, 2008Assignee: 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: 20070299113Abstract: The invention relates to imidazothiazole derivatives as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are group I mGluR modulators and are therefore useful for the control and prevention of various disorders, including acute and/or chronic neurological disorders.Type: ApplicationFiled: June 22, 2007Publication date: December 27, 2007Applicant: MERZ PHARMA GMBH & CO. KGAAInventors: Ivars Kalvinsh, Larisa Kaulina, Valerjans Kauss, Ronalds Zemribo, Wojciech Danysz, Markus Henrich, Christopher Graham Raphael Parsons, Tanja Weil, Elina Erdmane
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Patent number: 7205316Abstract: Compounds of formula (I) wherein R1 or R2 is a tricyclic or bicyclic ring, each of which contains at least two heteroatoms, and R1, R2, R3, R3a, R3b, R4, R5, L, X, X?, Y, Y?, Z, and Z? are as defined herein, are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).Type: GrantFiled: May 6, 2005Date of Patent: April 17, 2007Assignee: Abbott LaboratoriesInventors: Robert J. Altenbach, Lawrence A. Black, Marlon D. Cowart, Huaqing Liu
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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: 7125863Abstract: Compounds according to formula (1), wherein R1 is H or CN, X1 is S, O, SO2 or CH2, X2 is CO, CH2 or a covalent bond, Het is a nitrogen-containing heterocycle and n is 1–5 are new. The compounds of the invention are inhibitors of dipeptidyl peptidase IV.Type: GrantFiled: April 26, 2001Date of Patent: October 24, 2006Assignee: Ferring BVInventors: David Michael Evans, Gary Robert William Pitt
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Patent number: 7112582Abstract: The present invention provides a compound of formula I, pharmaceutical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof. wherein one of A and B denotes hydrogen and the other an optionally substituted fused bicyclic heteroaryl group; and X is S.Type: GrantFiled: May 1, 2003Date of Patent: September 26, 2006Assignee: WyethInventors: Aranapakam Mudumbai Venkatesan, Tarek Suhayl Mansour, Takao Abe, Itsuki Yamamura, Tsuyoshi Takasaki, Atul Agarwal, Osvaldo dos Santos, Fuk-Wah Sum, Yang-I Lin
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Patent number: 7022701Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.Type: GrantFiled: April 20, 2004Date of Patent: April 4, 2006Assignee: WyethInventors: Derek Cecil Cole, Joseph Raymond Stock, William Joseph Lennox, Ping Zhou
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Patent number: 6900160Abstract: The invention relates to triazolo-thiazole analogues of epothilone A and epothilone B.Type: GrantFiled: September 21, 2001Date of Patent: May 31, 2005Assignee: Gesellschaft fuer Biotechnologische Forschung mbHInventors: Gerhard Hoefle, Nicole Glaser
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Patent number: 6875765Abstract: The novel arylsulfonamide ether compounds, pharmaceutical compositions and uses thereof as inhibitors of interleukin-1? converting enzyme and other cysteine proteases in the ICE family are described. In one embodiment, the compound is described by the generalized structure: and pharmaceutically acceptable salts, esters, amides, and prodrugs thereof. In addition, methods of treating stroke, inflammatory diseases, septic shock, repurfusion injury, Alzheimer's disease, and shigellosis, using a compound of the invention or a pharmaceutical composition thereof, are described.Type: GrantFiled: May 10, 2002Date of Patent: April 5, 2005Assignee: Warner-Lambert CompanyInventors: James Knobelsdorf, Sheryl Hays, Charles J. Stankovic, Kimberly S. Para, Michael K. Connolly, Paul Galatsis, William Harter, Aurash B. Shahripour, Mark Stephen Plummer, Beth Lunney, Bernd Janssen, Jay Bradford Fell
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Patent number: 6838462Abstract: The present invention relates to novel heterocyclic compounds of formula (I) where A, R1, R2, Y, Z, and n are defined in the disclosure, to processes for their preparation, and to their use as crop protection agents, in particular for controlling animal pests.Type: GrantFiled: April 16, 2002Date of Patent: January 4, 2005Assignee: Bayer CropScience LPInventors: Peter Jeschke, Michael Beck, Wolfgang Krämer, Detlef Wollweber, Angelika Lubos-Erdelen, Andreas Turberg, Olaf Hansen, Hans-Dieter Martin, Piet Sauer, Christoph Erdelen
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Publication number: 20040242874Abstract: There is provided a process for the preparation of bicyclicheteroaryl carboxaldehydes having the structural Formula I where X and Y are defined in the specification 1Type: ApplicationFiled: May 12, 2004Publication date: December 2, 2004Applicant: Wyeth Holdings CorporationInventors: Michael William Winkley, Anita Wai-Yin Chan, Ivo L. Jirkovsky, Kenneth Alfred Martin Kremer, Joseph Zeldis, Antonia Aristotelevna Nikitenko, Henry Lee Strong, Tarek Mansour, Gulnaz Khafizova, Aranapakam M. Venkatesan
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Publication number: 20040209896Abstract: The present application relates to novel heterocyclic compounds of formula (I) 1Type: ApplicationFiled: May 3, 2004Publication date: October 21, 2004Inventors: Peter Jeschke, Michael Beck, Wolfgang Kramer, Detlef Wollweber, Christoph Erdelen, Andreas Turberg, Olaf Hansen, Hans-Dieter Martin, Piet Sauer, Angelika Lubos-Erdelen
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Patent number: 6784293Abstract: The present invention provides a process for the efficient assembly of Boc-protected 3-aminohydantoins/thiohydantoins and 3-aminodihydrouracils/dihydrothiouracils via a one-pot solution phase or solid phase synthesis from readily available starting materials.Type: GrantFiled: June 25, 2002Date of Patent: August 31, 2004Assignee: The Procter & Gamble CompanyInventors: Shengde Wu, John Michael Janusz
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Patent number: 6770642Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.Type: GrantFiled: December 19, 2002Date of Patent: August 3, 2004Assignee: WyethInventors: Derek Cecil Cole, Joseph Raymond Stock, William Joseph Lennox, Ping Zhou
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Publication number: 20040122002Abstract: The present invention relates to fused pyrrole compounds of the formula 1.Type: ApplicationFiled: September 27, 2002Publication date: June 24, 2004Inventors: Hans Guenter Striegel, Stefan Laufer, Karola Tollmann, Susanne Tries
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Publication number: 20040063580Abstract: The present invention provides a bicyclic triazolone derivative represented by the formula:Type: ApplicationFiled: June 26, 2003Publication date: April 1, 2004Inventors: Takashi Kuragano, Yasushi Tanaka
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Publication number: 20040048879Abstract: Heterocyclic compound represented by the formula I 1Type: ApplicationFiled: July 29, 2003Publication date: March 11, 2004Inventors: Seiichiro Kawashima, Toshiyuki Matsuno, Naoki Fukuda, Kenichi Saitoh, Yoshima Yamaguchi, Masaya Higashi
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Publication number: 20040014982Abstract: The invention relates to triazolo-thiazole analogues of epothilone A and epothilone B.Type: ApplicationFiled: August 18, 2003Publication date: January 22, 2004Inventors: Gerhard Hoefle, Nicole Glaser
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Patent number: 6657064Abstract: A novel bicyclic imidazo-5-yl-amine derivative of Formula I, wherein X denotes CR5, N or S, and Y in the case where X denotes S, denotes CR6 or N and in all other cases denotes N, and methods for preparation thereof are disclosed. Also disclosed are methods for treating pain using the compound of Formula I, and pharmaceutical compositions comprising the compound of Formula I.Type: GrantFiled: April 8, 2002Date of Patent: December 2, 2003Assignee: Gruenenthal GmbHInventors: Matthias Gerlach, Corinna Maul
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Publication number: 20030191309Abstract: The present invention relates to a novel class of organic molecules capable of inhibiting C-proteinase, and to their use to regulate, modulate and/or inhibit abnormal collagen formation as a therapeutic approach towards the treatment of fibrotic disorders.Type: ApplicationFiled: November 12, 2002Publication date: October 9, 2003Inventor: Wen-Bin Ho
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Publication number: 20030166628Abstract: The present invention relates to certain novel substituted dihydroimidazo[2,1-b]thiazole and dihydro-5H-thiazolo[3,2-a]pyrimidine compounds of Formula (I) including pharmaceutically acceptable salts thereof in which have affinity for 5-HT1A receptors and which inhibits neuronal reuptake of 5-hydroxytryptamine and/or noradrenaline, to processes for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, obesity, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, obsessive-compulsive behaviour, panic attacks, social phobias, eating disorders such as bulimia, anorexia, snacking and binge eating, non-insulin dependent diabetes mellitus, hyperglycaemia, hyperlipidaemia, stress, as an aid to smoking cessation and in the treatment and/or prophylaxis of seizures, neurological disorders such as epilepsy and/or in which there is neurological damage such asType: ApplicationFiled: January 16, 2003Publication date: September 4, 2003Inventors: Kevin James Doyle, Frank Kerrigan, John Paul Watts
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Patent number: 6586452Abstract: The present invention relates to novel nodulosporic acid derivatives, which are acaricidal, antiparasitic, insecticidal and anthelmintic agents.Type: GrantFiled: July 9, 2001Date of Patent: July 1, 2003Assignee: Merck & Co., Inc.Inventors: Thomas Shih, Steven L. Colletti, Michael H. Fisher, Peter T. Meinke, Howard C. H. Kuo, Prasun K. Chakravarty, Matthew J. Wyvratt, Sriram Tyagarajan, Richard Berger
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Patent number: 6534506Abstract: The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.Type: GrantFiled: April 6, 2001Date of Patent: March 18, 2003Assignee: Merck & Co., Inc.Inventors: Diem N. Nguyen, Craig A. Stump, Theresa M. Williams
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Patent number: 6486328Abstract: A novel route has been developed for substituted 2-[-6-benzyl-5-oxo-3-phenyl-(3s,7s,7aR)-perhydroimidazol[1,5-c][1,3]thiazol] compounds; crucial intermediates for D(+)-biotin of formula (7) which involves simple, efficient, practical and cost effective protocol. These are crucial intermediates for commercially important D(+)-biotin preparation. These compounds are more stable and are produced by non-hazardous methods.Type: GrantFiled: October 12, 2000Date of Patent: November 26, 2002Assignee: Council of Scientific and Industrial ResearchInventors: Subhash Prataprao Chavan, Amar Gopal Chittiboyina, Subhash Krishnaji Kamat, Uttam Ramrao Kalkote, Thotapallil Ravindranathan
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Patent number: 6395724Abstract: Disclosed are multibinding compounds which inhibit cyclooxygenase-2 (COX-2), an enzyme which catalyzes the first committed step in the biosynthesis of prostaglandins. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is a moiety capable of binding to COX-2. The multibinding compounds of this invention are useful in the treatment inflammation, pain, fever and the like.Type: GrantFiled: June 7, 1999Date of Patent: May 28, 2002Assignee: Advanced Medicine, Inc.Inventors: J. Kevin Judice, Deborah L. Higgins, John H. Griffin
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Patent number: 6380228Abstract: The present invention is directed to peptidomimetic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.Type: GrantFiled: April 6, 2001Date of Patent: April 30, 2002Assignee: Merck & Co., Inc.Inventors: Craig A. Stump, Theresa M. Williams
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Patent number: 6350881Abstract: This invention provides a process for the preparation of 5-methoxy-4-(methylthioalkyl)-1,3-bis(phenylmethyl)-2-imidazolidone having general formula (2a-d) [wherein R═—CH2COCH2CH2CH2COOMe (2a); —CH2CH(OMe)2(2b); —CH2COOMe(2c); —H (2d)] which comprises reacting a reducing agent with 6-benzyl-7-methoxy-3-phenylperhydroimidazo[1,5-c][1.3]thiozol-5-one in the presence of an organic solvent for a period ranging from 0.5 to 2 hrs at a temperature ranging from −78° C. to 80° C., evaporating the solvent and reacting the residue with an alkylating reagent, optionally in the presence of a phase transfer catalyst and an inorganic base in an organic solvent for a period ranging from 10-12 hrs at room temperature, evaporating the solvent followed by purification to obtain the desired compound of general formula 2 a-d.Type: GrantFiled: November 28, 2000Date of Patent: February 26, 2002Assignee: Council of Scientific and Industrial ResearchInventors: Subhash Prataprao Chavan, Subhash Krishnaji Kamat, Beena Rai, Latha Sivadasan, Kamalam Balakrishnan, Ramalingam Sadyandi, Amar Gopal Chittiboyina, Vishnu Hari Deshpande
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Patent number: 6340372Abstract: A compostion for the dyeing of keratinous fibres comprising, in a medium appropriate for dyeing keratinous fiber contains: as coupler, at least one compound of formula: in which R1 denotes in particular hydrogen, halogen, aryloxy, alkoxy, acyloxy, arylthio, alkylthio, acetamido; an NRIIIRIV radical with RIII and RIV representing a C1-C4 alkyl, and the like; Za, Zb, and Zc represent, independently of one another, a nitrogen atom or else a carbon atom carrying an R2, R3 or R4 radical; provided that: when Za denotes a carbon atom carrying an R2 radical, Zb represents a nitrogen atom and Zc denotes a carbon atom carrying an R3 radical; when Za denotes a nitrogen atom, Zb represents a carbon atom carrying an R4 radical and Zc dentoes a nitrogen atom; R2, R3 or R4=H, C1-4 alkyl, aryl; n is 1 or 2: and at least one oxidation base.Type: GrantFiled: February 26, 1999Date of Patent: January 22, 2002Assignee: L'Oreal S.A.Inventors: Laurent Vidal, Gèrard Malle
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Patent number: 6191124Abstract: The present invention relates to compounds of formula (I) which are imidazo[2,1-b]benzothiazole-3-methanol and imidazo[2,1-b]thiazole-5-methanol derivatives useful for inhibiting a retrovirus in a mammalian cell infected with said retrovirus, wherein R1 is —H or —CH3; wherein R2 is —H or —CH3; or wherein R1 and R2 taken together are (a) formula (II), or (b) formula (III).Type: GrantFiled: April 7, 1997Date of Patent: February 20, 2001Assignee: Pharmacia & Upjohn CompanyInventor: Herman W. Smith
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Patent number: 6187802Abstract: Compounds of Formula I including pharmaceutically acceptable salts thereof in the form of individual enantiomers, racemates, or other mixtures of enantiomers, in which Ar is phenyl, naphthyl or benzo[b]thiophenyl, each of which may be optionally substituted; R1 and R2, which may be the same or different, independently are a) H, b) an alkyl group containing 1 to 6 carbon atoms, c) an alkenyl group containing 3 to 6 carbon atoms, d) a cycloalkyl group containing 3 to 7 carbon atoms, e) a cycloalkylmethyl group in which the ring contains 3 to 7 carbon atoms, f) an aryl or heteroaryl group optionally substituted g) an arylalkyl or heteroarylalkyl group each optionally substituted; or R1 and R2 form an alkylene chain optionally substituted by one or more alkyl groups each containing 1 to 3 carbon atoms, such that, together with the atoms to which they are attached, they form a 5 or 6 membered ring; R3 is a) H, b) an aryl or heteroaryl group each optionally substituted c) an optionallyType: GrantFiled: September 14, 1999Date of Patent: February 13, 2001Assignee: Knoll AktiengesellschaftInventors: Sharon Crawford Cheetham, Frank Kerrigan, Colin Gerhart Pryce Jones
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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: 6159995Abstract: Compounds of formula (I) ##STR1## are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved.Type: GrantFiled: May 8, 1998Date of Patent: December 12, 2000Assignee: Aventis Pharma Deutschland GmbHInventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase, Bernhard Neises, Gunter Billen
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Patent number: 6037469Abstract: Compounds of formula (I) in which: R.sup.1 is hydrogen or an organic substituent group; R.sup.2 is a fused bicyclic heterocyclic ring system of general formula (a) wherein R.sup.4 and R.sup.5 are independently hydrogen or one or more substituents replacing hydrogen atoms in the ring system shown; m is 2 or 3; p is 0, 1 or 2; and R.sup.3 is hydrogen, a salt-forming cation or an ester-forming group; and the symbol .dbd./.dbd.Type: GrantFiled: May 24, 1995Date of Patent: March 14, 2000Assignee: SmithKline Beecham plcInventors: Nigel John Perryman Broom, Frank Peter Harrington
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Patent number: 5994380Abstract: This invention refers to new analogs of strobilurine, having the general formula (I): ##STR1## The compounds of formula (I) are endowed with good stability and high fungicidal activity against phytopathogenous fungi, combined with good selectivity for the vegetable it is designed to apply to.Type: GrantFiled: October 19, 1998Date of Patent: November 30, 1999Assignee: Isagro Ricerca S.r.L.Inventors: Lucio Filippini, Isabella Venturini, Laura Colombo, Luigi Mirenna