Benzene Ring In A Substituent Attached To The Ring Nitrogen Of The Five Membered Hetero Ring By Nonionic Bonding Patents (Class 548/578)
  • Publication number: 20090170841
    Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are styrenyl derivative compounds, including but not limited to stilbene derivative compounds, and compositions comprising these compounds, that are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.
    Type: Application
    Filed: April 21, 2008
    Publication date: July 2, 2009
    Applicant: Acucela Inc.
    Inventors: Ian Leslie Scott, Vladimir Aleksandrovich Kuksa, Anna Gall, Mark W. Orme, Jennifer Gage, Thomas L. Little, JR., Qin Jiang, Lana Michele Rossiter, Kevin F. McGee, JR., Ryo Kubota
  • Publication number: 20090143397
    Abstract: The present invention provides a catechol-based derivative and a pharmaceutical acceptable salt therefrom and a solvate therefrom. A pharmaceutical composition for preventing or treating diabetics and ischemics, comprising a catechol-based derivative of formula (I) and at least one selected from the group consisting of a pharmaceutical excipient, a diluent and a carrier.
    Type: Application
    Filed: February 9, 2009
    Publication date: June 4, 2009
    Applicant: LOTUS PHARMACEUTICAL CO., LTD.
    Inventors: Yueh-Hsiung Kuo, Ming-Jai Su
  • Publication number: 20090137800
    Abstract: A compound represented by the following general formula (I), wherein ring A and ring B each independently represent a benzene, naphthalene, or heterocyclic ring which may be substituted; R1 and R2 each independently represent an alkyl group having 1 to 8 carbon atoms which may be substituted; R1 and R2 may be linked together to form a ring; a methylene group of the alkyl group having 1 to 8 carbon atoms may be replaced by —O— or —CH?CH—; Anq- represents a q-valent anion, where q is 1 or 2; p represents a coefficient to keep the charge neutral.
    Type: Application
    Filed: March 5, 2007
    Publication date: May 28, 2009
    Inventor: Satoshi Yanagisawa
  • Publication number: 20090099187
    Abstract: The present invention relates to new compounds of formula (I), wherein R1 to R12, P, X, Q and n are as defined as in formula I, or salts, solvates or solvated salts thereof, processes for their preparation and to new intermediates used in the preparation thereof, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.
    Type: Application
    Filed: May 22, 2006
    Publication date: April 16, 2009
    Applicant: AstraZeneca AB
    Inventors: Gunnar Nordvall, Carl Petersson, Laszlo Rakos, Daniel Sohn
  • Patent number: 7498447
    Abstract: Disclosed herein is a compound having a structure or a pharmaceutically acceptable salt, or a prodrug thereof. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: July 17, 2007
    Date of Patent: March 3, 2009
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Danny T. Dinh
  • Patent number: 7482475
    Abstract: Disclosed herein is a compound having a structure Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: August 9, 2007
    Date of Patent: January 27, 2009
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Robert M. Burk
  • Patent number: 7476747
    Abstract: A compound comprising or a pharmaceutically acceptable salt, prodrug, or a metabolite thereof is disclosed herein. Y, A, and B are as described herein. Methods, compositions, and medicaments related to these compounds are also disclosed.
    Type: Grant
    Filed: March 6, 2006
    Date of Patent: January 13, 2009
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Danny T. Dinh
  • Publication number: 20080300271
    Abstract: The present invention is directed to a procedure for making an enantidimerically enriched compound containing a hydronaphthalene ring structure. The process involves reacting oxabenzonorbornadienes with nuclophiles using rhodium as a catalyst and in the presence of a phosphine ligand. The compounds synthesized may be used in pharmaceutical preparations for the treatment of a variety of diseases and conditions.
    Type: Application
    Filed: July 28, 2008
    Publication date: December 4, 2008
    Inventors: Keith Fagnou, Mark Lautens
  • Patent number: 7408071
    Abstract: There is provided a series of substituted N-aryl pyrrolidine derivatives of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R5?, R6, R7, and p as defined herein, their pharmaceutical compositions and methods of use. These compounds inhibit the processing of amyloid precursor protein (APP) by ?-secretase and, more specifically, inhibit the production of A?-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to ?-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
    Type: Grant
    Filed: March 29, 2007
    Date of Patent: August 5, 2008
    Assignee: Bristol-Myers Squibb Company
    Inventors: Kenneth M. Boy, Shirong Zhu, John E. Macor, Shuhao Shi, Samuel Gerritz
  • Patent number: 7405262
    Abstract: A process for preparing a functionalized polymerization initiator, the process comprising combining a functionalized styryl compound and an organolithium compound.
    Type: Grant
    Filed: July 11, 2003
    Date of Patent: July 29, 2008
    Assignee: Bridgestone Corporation
    Inventors: Thomas Antkowiak, Christine Rademacher, Anthony Ramic, David F. Lawson
  • Patent number: 7381827
    Abstract: The invention relates to processes and compounds useful for producing modified aspartic acid derivatives, such as aspartic acid aldehyde moieties. Aspartic acid derivatives are useful for preparing caspase inhibitors and/or prodrugs thereof.
    Type: Grant
    Filed: March 11, 2005
    Date of Patent: June 3, 2008
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Gerald J. Tanoury, Minzhang Chen, Andrew D. Jones, Philip L. Nyce, Martin Trudeau, David J. Guerin, John R. Snoonian
  • Patent number: 7235544
    Abstract: The invention relates to compounds of formula (I): wherein substituents are as defined.
    Type: Grant
    Filed: June 17, 2004
    Date of Patent: June 26, 2007
    Assignee: Glaxo Group Limited
    Inventors: Alan David Borthwick, John David Harling, Wendy Rebecca Irving, Savvas Kleanthous, Nigel Stephen Watson, Robert John Young
  • Patent number: 7226917
    Abstract: Compounds of formula (I) as defined herein: are useful for treating behavioral disorders associated with dementia, psychoses, in particular schizophrenia (deficient form and productive form) and acute or chronic extrapyramidal symptoms induced by neuroleptics; for the treatment of various forms of anxiety, panic attacks, phobias, and compulsive obsessive disorders; for treating various forms of depression, including psychotic depression; for treating disorders caused by alcohol abuse or weaning from alcohol, sexual behavior disorders, eating disorders and for treating migraine.
    Type: Grant
    Filed: April 17, 2006
    Date of Patent: June 5, 2007
    Assignee: Sanofi-Aventis
    Inventors: Gihad Dargazanli, Genevieve Estenne-Bouhtou, Florence Medaisko, Nathalie Rakotoarisoa
  • Patent number: 7105507
    Abstract: The present invention relates compounds of formula (I), wherein ring A is a phenyl or pyridyl ring; X represents a linker selected from the group consisting of formulae: (a), (b), (c), (d), and (e); and R1, R2, R3, R4, R5, R6, R7, R13, R14, R15, R16, R17, R21a and R21b are as defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.
    Type: Grant
    Filed: May 16, 2001
    Date of Patent: September 12, 2006
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Jose Luis Castro Pineiro, Kevin Dinnell, Jason Matthew Elliott, Gregory John Hollingworth, Duncan Edward Shaw, Christopher John Swain
  • Patent number: 7005439
    Abstract: The invention provides compounds of general formula (I) wherein m, n, Z1, Z2, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined in the specification, process for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Grant
    Filed: June 14, 2001
    Date of Patent: February 28, 2006
    Assignee: AstraZeneca AB
    Inventors: Tomas Eriksson, Krister Henriksson
  • Patent number: 6943188
    Abstract: The invention provides compounds of general formula (I) wherein Q, R, R2, R3, R4, R5, R6, R7, and R8 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Grant
    Filed: February 23, 2001
    Date of Patent: September 13, 2005
    Assignee: AstraZeneca AB
    Inventors: Tomas Eriksson, Peter Hansen, Martin Hemmerling, Krister Henriksson, Tomas Klingstedt, Lars Pettersson, Michael Bodkin
  • Patent number: 6923835
    Abstract: The invention relates to novel bis-para-phenylenediamine derivatives containing a pyrrolidyl group substituted with a cationic radical, to dye compositions containing them and to the process of dyeing keratin fibres using these compositions. The present invention makes it possible to obtain a chromatic, powerful, sparingly selective and colourfast coloration of keratin fibres.
    Type: Grant
    Filed: September 9, 2003
    Date of Patent: August 2, 2005
    Assignee: L'Oreal S.A.
    Inventors: Stéphane Sabelle, Laure Ramos, Madeleine Leduc
  • Patent number: 6803462
    Abstract: This invention discloses a rubbery polymer which is comprised of repeat units that are derived from (1) at least one conjugated diolefin monomer, and (2) at least one functionalized monomer having of the structural formula: wherein R represents an alkyl group containing from 1 to about 10 carbon atoms or a hydrogen atom, and wherein R1 and R2 can be the same or different and represent hydrogen atoms or a moiety selected from the group consisting of wherein R3 groups can be the same or different and represent alkyl groups containing from 1 to about 10 carbon atoms, aryl groups, allyl groups, and alkyloxy groups of the structural formula —(CH2)y—O—(CH2)z—CH3, wherein Z represents a nitrogen containing heterocyclic compound, wherein R4 represents a member selected from the group consisting of alkyl groups containing from 1 to about 10 carbon atoms, aryl groups, and allyl groups, and wherein n, x, y and z represents integers from 1 to about 10, with the
    Type: Grant
    Filed: June 30, 2003
    Date of Patent: October 12, 2004
    Assignee: The Goodyear Tire & Rubber Company
    Inventors: Stephan Rodewald, Steven Kristofer Henning, Brian Earl Burkhart
  • Patent number: 6770463
    Abstract: There is provided a process for the preparation of a chiral insecticidal and acaricidal compound of formula I. Also provided are intermediate compounds useful in the process of the present invention.
    Type: Grant
    Filed: August 2, 2001
    Date of Patent: August 3, 2004
    Assignee: BASF Aktiengesellschaft
    Inventors: John Francis Chiarello, Brian Lee Buckwalter, Timothy Claude Barden
  • Patent number: 6753327
    Abstract: An amide of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings: A —(CH2)p—R1, where R1 can be pyrrolidine, morpholine, piperidine, —NR5R6 and  and R5, R6 and R7 can, independently of one another, be hydrogen, C1-C4-alkyl, CH2Ph, Ph, CH2CH2Ph, it also being possible for the phenyl rings to be substituted by R6, and p can be 1 and 2, and B can be phenyl, pyridyl, pyrimidyl and pyridazyl, it also being possible for the rings to be substituted by up to 2 R8 radicals, and D can be a bond, —(CH2)m, —CH═CH—, —C≡C—, and Y is phenyl, pyridine, pyrimidine and pyrazine and n is a number 0, 1 or 2, and m,q are, independently of one another, a number 0, 1, 2, 3 or 4.
    Type: Grant
    Filed: October 11, 2000
    Date of Patent: June 22, 2004
    Assignee: Abbott GmbH & Co. KG
    Inventors: Wilfried Lubisch, Achim Möller, Hans-Jörg Treiber, Monika Knopp
  • Patent number: 6750337
    Abstract: Couplers for hair coloring compositions for oxidative dyeing of hair are compounds of the formula (1): wherein X is selected from halogen and R5SO4 where the halogen is preferably Cl, Br or I; R, R1 and R2 are each individually selected from C1 to C22 alkyl and C1 to C22 mono or dihydroxyalkyl, or two of R, R1 and R2 together with the nitrogen atom to which they are attached form a C3 to C6 saturated or unsaturated ring optionally containing in the ring one or more additional hetero atoms selected from O, S and N atoms; R3 and R 4 are each individually selected from C1 to C6 alkyl, C1 to C6 hydroxyalkyl, C1 to C6 alkoxy, C1 to C6 aminoalkyl or R3 and R4 together form a C1 to C5 alkylene group; and R5 is selected from C1 to C22 alkyl and C1 to C22 mono or dihydroxyalkyl.
    Type: Grant
    Filed: January 18, 2002
    Date of Patent: June 15, 2004
    Assignee: The Procter & Gamble Company
    Inventors: Mu-Ill Lim, Yuh-Guo Pan, Gottfried Wenke
  • Publication number: 20040072854
    Abstract: A NK1 antagonist having the formula (I), with the variables defined herein, which is useful for treating a number of disorders, including emesis, depression, anxiety and cough: 1
    Type: Application
    Filed: March 12, 2003
    Publication date: April 15, 2004
    Applicant: Schering Corporation
    Inventors: Michelle Laci Wrobleski, Gregory A. Reichard, Neng-Yang Shih, Dong Xiao
  • Publication number: 20040030131
    Abstract: A compound of the formula in which R1 and R2 are each hydrogen or C1-4 alkyl, or R1 and R2 together with the nitrogen atom to which they are attached form an azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl or morpholino group, said group being optionally substituted with 1 to 3 substituents selected from C1-4 alkyl, hydroxymethyl, C1-4 alkoxymethyl and amido, R3 is a naphthyl, indolyl, benzothienyl, benzofuranyl, benzothiazolyl, quinolinyl or isoquinolinyl group, said group being optionally substituted, and n is 1 or 2; and m is 0 or 1, provided that when m is 1 then n is 1; or a salt or ester thereof.
    Type: Application
    Filed: September 3, 2003
    Publication date: February 12, 2004
    Inventors: Martine Keenan, Vincent Patrick Rocco, Kumiko Takeuchi, David Edward Tupper, Vincent Vivien
  • Publication number: 20040006061
    Abstract: There are described alkoxybenzylamines corresponding to formula 1
    Type: Application
    Filed: October 2, 2002
    Publication date: January 8, 2004
    Inventors: Wolfgang Haap, Werner Holzl, Karin Petzold
  • Patent number: 6608052
    Abstract: Disclosed are novel aromatic compounds of the formula(I) wherein G, E, W, Ar, X, Y and Z. The compounds are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.
    Type: Grant
    Filed: April 13, 2001
    Date of Patent: August 19, 2003
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Steffen Breitfelder, Pier F. Cirillo, John R. Regan
  • Patent number: 6605670
    Abstract: Methods of making low molecular weight methylene acceptors are provided. The methylene acceptors are prepared by reacting a polyhydric phenol with an aromatic olefinic compound in the presence of an acid catalyst, and then further reacting the products of the first reaction with an N-methylol lactam derivative. Derivatives made by the above method, as well as rubber compositions using these derivatives are also provided.
    Type: Grant
    Filed: November 6, 2001
    Date of Patent: August 12, 2003
    Assignee: Indspec Chemical Corporation
    Inventors: Raj B. Durairaj, Mark A. Lawrence
  • Publication number: 20030109560
    Abstract: Novel compounds of general formula (I), the use of these compounds as medicaments, pharmaceuticaly compositions comprising the compounds and methods of treatment employing these compounds and compostiones. The present compounds may be useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR). The compounds exert their effects by modulating the PPAR&ggr; response in a partial agonist manner.
    Type: Application
    Filed: July 29, 2002
    Publication date: June 12, 2003
    Inventors: Lone Jeppesen, Paul Stanley Bury, John Patrick Mogensen, Ingrid Pettersson, Per Sauerberg
  • Publication number: 20030100607
    Abstract: The present invention relates to new thiolalkyl benzoic acids, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-&bgr; activity, inhibiting angiogenesis, and treating glutamate abnormalities, neuropathy, pain, compulsive disorders, prostate diseases, cancers, glaucoma, retinal disorders, and cancer.
    Type: Application
    Filed: May 30, 2002
    Publication date: May 29, 2003
    Inventors: Takashi Tsukamoto, Doris Stoermer, Dilrukshi Vitharana
  • Publication number: 20030078428
    Abstract: Phenylamino benzhydroxamic acid derivatives of formula (I) where R1, R2, R3, R4, R5, and R6 are hydrogen or substituent groups such as alkyl, and where R7 is hydrogen or an organic radical, are potent inhibitors of MEK and, as such, are effective in treating cancer and other proliferative diseases such as psoriasis and restenosis.
    Type: Application
    Filed: June 4, 2002
    Publication date: April 24, 2003
    Inventors: Stephen Douglas Barrett, Alexander James Bridges, Annette Marian Doherty, David Thomas Dudley, Alan Robert Saltiel, Haile Tecle
  • Publication number: 20030078249
    Abstract: Compounds that selectively inhibit the binding of ligands to &agr;4&bgr;1 integrin (VLA-4) and methods for their preparation are disclosed.
    Type: Application
    Filed: December 28, 2001
    Publication date: April 24, 2003
    Applicant: Daiichi Pharmaceutical Co., LTD.
    Inventors: John J. Baldwin, Edward McDonald, Kevin Joseph Moriarty, Christopher Ronald Sarko, Nobuo Machinaga, Atsushi Nakayama, Jun Chiba, Shin Iimura, Yoshiyuki Yoneda
  • Publication number: 20030073833
    Abstract: Phenyl acetamide compounds are described, including compounds of Formula I: 1
    Type: Application
    Filed: October 3, 2002
    Publication date: April 17, 2003
    Applicant: 3-Dimensional Pharmaceuticals, Inc.
    Inventors: Wenxi Pan, Tianbao Lu, Thomas P. Markotan, Bruce E. Tomczuk
  • Patent number: 6544982
    Abstract: A thrombin receptor antagonist having the formula useful for inhibiting the aggregation of blood platelets. The compounds can be used in a method of acting upon a thrombin receptor which comprises administering a therapeutically effective but non-toxic amount of such compound to a mammal, preferably a human.
    Type: Grant
    Filed: October 27, 2000
    Date of Patent: April 8, 2003
    Assignee: Merck & Co., Inc.
    Inventors: Harold G. Selnick, Philippe G. Nantermet, James C. Barrow, Roger M. Freidinger, Thomas Connolly
  • Publication number: 20030060624
    Abstract: The present invention relates to processes for the preparation of any of the intermediate 1,3-substituted indenes of the formulae (Ia), (Ib) and (Ic) or a mixture thereof: 1
    Type: Application
    Filed: April 17, 2002
    Publication date: March 27, 2003
    Inventor: Robert A. Singer
  • Publication number: 20030045712
    Abstract: The present invention relates to new substituted aryl and heteroaryl derivatives of general formula 1
    Type: Application
    Filed: May 10, 2002
    Publication date: March 6, 2003
    Applicant: Boehringer Ingelheim Pharma KG
    Inventors: Henning Priepke, Uwe Ries, Herbert Nar, Wolfgang Wienen, Jean-Marie Stassen
  • Publication number: 20030032802
    Abstract: This invention relates to the novel use of dianilino squarates in the treatment of disease states mediated by the chemokine, Interteukin-8 (IL-8).
    Type: Application
    Filed: August 30, 2002
    Publication date: February 13, 2003
    Inventors: Michael R. Palovich, Joseph Weinstock, Katherine L. Widdowson
  • Publication number: 20030032808
    Abstract: This invention provides an amido ligand and its synthesis. Use of the amide ligand in a variety of metal complexes, and transition metals in particular, is also provided.
    Type: Application
    Filed: April 2, 2002
    Publication date: February 13, 2003
    Inventors: Jonas C. Peters, Steven D. Brown, Seth B. Harkins
  • Patent number: 6476063
    Abstract: Method for the prevention or treatment of pruritus with anti-pruritic compounds is provided. The compounds of formulae I, II, IIA, III, IIIA, IV and IVA have the structure: wherein R1, R2, R3, R4; and X, X4, X5, X7, X9; Y, Z and n are as described in the specification.
    Type: Grant
    Filed: March 13, 2001
    Date of Patent: November 5, 2002
    Assignee: Adolor Corporation
    Inventors: Wei Yuan Zhang, Alan L. Maycock, Anthony Michael Marella, Virendra Kumar, Forrest Gaul, Deqi Guo
  • Publication number: 20020151534
    Abstract: Antithrombotic compounds of general formula 1
    Type: Application
    Filed: January 16, 2002
    Publication date: October 17, 2002
    Inventors: Uwe Joerg Ries, Henning Priepke, Herbert Nar, Jean-Marie Stassen, Wolfgang Wienen
  • Publication number: 20020147347
    Abstract: Aromatic methylidene compounds of the following general formula 1
    Type: Application
    Filed: January 24, 2002
    Publication date: October 10, 2002
    Applicant: Matsushita Electirc Industrial Co., Ltd.
    Inventor: Mitsuru Hashimoto
  • Publication number: 20020137742
    Abstract: Compound of formula (I): 1
    Type: Application
    Filed: March 14, 2002
    Publication date: September 26, 2002
    Inventors: Gilbert Lavielle, Bernard Cimetiere, Tony Verbeuren, Serge Simonet, Jean-Jacques Descombes
  • Patent number: 6417353
    Abstract: Amines are prepared by reacting aldehydes or ketones at elevated temperature under elevated pressure with nitrogen compounds selected from the group of ammonia, primary and secondary amines, and with hydrogen in the presence of a catalyst containing copper, wherein the catalytically active mass of the catalyst contains, before the reduction with hydrogen, 20 to 85% by weight of oxygen-containing compounds of zirconium, calculated as ZrO2, 1 to 30% by weight of oxygen-containing compounds of copper, calculated as CuO, 14 to 70% by weight of oxygen-containing compounds of nickel, calculated as NiO, 0 to 5% by weight of oxygen-containing compounds of molybdenum, calculated as MoO3, and 0 to 10% by weight of oxygen-containing compounds of aluminum, calculated as Al2O3.
    Type: Grant
    Filed: March 7, 2000
    Date of Patent: July 9, 2002
    Assignee: BASF Aktiengesellschaft
    Inventors: Frank Funke, Joachim Wulff-Döring, Gerhard Schulz, Wolfgang Siegel, Andreas Kramer, Johann-Peter Melder, Arthur Höhn, Philipp Buskens, Wolfgang Reif, Jan Nouwen
  • Patent number: 6413987
    Abstract: The present invention relates to new aminoindane piperidine compounds, the method of using aminoindane compounds as local anesthetics, said compounds having particularly valuable properties as dermal and topical anesthetics in mammals, including man, as well as compositions containing said compounds.
    Type: Grant
    Filed: June 6, 2000
    Date of Patent: July 2, 2002
    Assignee: Bridge Pharma, Inc.
    Inventors: A. K. Gunnar Aberg, George E. Wright, Jan L. Chen
  • Patent number: 6403585
    Abstract: &agr;- and &bgr;-amino acid hydroxyethylamino sulfonyl urea derivative compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: December 8, 2000
    Date of Patent: June 11, 2002
    Assignee: G. D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
  • Patent number: 6391910
    Abstract: Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics are provided. The compounds of formulae I, II, IIA, III, IIIA, IV and IVA have the structure: wherein R1, R2, R3, R4; and X, X4, X5, X7, X9; Y, Z and n are as described in the specification.
    Type: Grant
    Filed: January 6, 2000
    Date of Patent: May 21, 2002
    Assignee: Adolor Corporation
    Inventors: Wei Yuan Zhang, Alan L. Maycock, Michael Anthony Marella, Virendra Kumar, Forrest Gaul, An-Chih Chang, Deqi Guo
  • Publication number: 20020058811
    Abstract: Compounds of formula (1) where R1 is of formulae (II), (III), or (IV), or (V); R2 is —R4, —O—R4, —O—S(O)2—R4, —NR4R5, R4—(CH2)b—NH(C═X)—(CH2)c—, R4—(CH2)b—O(C—O)NH—(CH2)c—(C═O)NH—, R4—(C═O)NH—(C═O)NH—, —(CH2)b—NH(C═X)—(CH2)c—R4, R4—(CH2)b—O(C═O)CH2)c—, —(CH2)b—O(C═O)—(CH2)c—R4, —NH(C═X)NH—R4, R4—O(C═O)O—, —O(C═O)NH—R4, R4—O(C═O)NH—, —(CH2)b—(C═O)—(CH2)c—R4, —NH—S(O)2—R4, —C(OH)R4R5, —CH(OH)—R4, —(C═O)—NR4, —CN, —NO2, substituted C1 to C6 alkyl, substituted or unsubstituted C1 to C6 alkenyl, or substituted or unsubstituted C1 to C6 alkynyl, said substituted moieties substituted with a moiety of the formulae —R4, —R4R5, &md
    Type: Application
    Filed: December 3, 2001
    Publication date: May 16, 2002
    Inventors: Bertrand L. Chenard, John E. Macor, Barbara E. Segelstein
  • Patent number: 6380397
    Abstract: A process for preparing 1H-indole-3-glyoxamides useful for inhibiting SPLA2 and novel intermediates useful in the preparation of such compounds.
    Type: Grant
    Filed: March 19, 2001
    Date of Patent: April 30, 2002
    Assignee: Eli Lilly and Company
    Inventors: Benjamin Alan Anderson, Nancy Kay Harn, Richard Duane Miller, Edward Francis Plocharczyk
  • Publication number: 20020042524
    Abstract: This invention provides an improved process for cis-1-{2-[4-(6-methoxy-2-phenyl-1,2,3,4-tetrahydronaphthalen-1-yl)phenoxy]ethyl}pyrrolidine which is an intermediate for the preparation of (−)cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydronaphthalene-2-ol which is useful for the treatment of osteoporosis.
    Type: Application
    Filed: October 9, 2001
    Publication date: April 11, 2002
    Inventor: Charles K.F. Chiu
  • Publication number: 20020037885
    Abstract: The present invention relates to certain novel benzylamine derivatives, to processes for their preparation, to pharmaceutical formulations containing them and to their use in medical therapy, particularly in the treatment of depression.
    Type: Application
    Filed: August 20, 2001
    Publication date: March 28, 2002
    Inventors: Fredericus Antonius Dijcks, Diark Leysen, Joannes Theodorus Maria Linders, Gerardus Stephanus Franciscus Ruigt, Ian Craig Carlyle, Simon James Anthony Grove, Duncan Robertson Rae, Simon N. Thorn
  • Publication number: 20020032351
    Abstract: There is provided a process for the preparation of a chiral insecticidal and acaricidal compound of formula I.
    Type: Application
    Filed: August 2, 2001
    Publication date: March 14, 2002
    Applicant: BASF Aktiengesellschaft
    Inventors: John Francis Chiarello, Brian Lee Buckwalter, Timothy Claude Barden
  • Patent number: RE39667
    Abstract: The invention relates to 3,3-diphenylpropylamines of formula (I), wherein R1 signifies hydrogen or methyl, R2 and R3 independently signify hydrogen, methyl, methoxy, hydroxy, carbamoyl, sulphamoyl or halogen, and X represents a tertiary amino group of formula (II), wherein R4 and R5 signify non-aromatic hydrocarbyl groups, which may be the same or different and which together contain at least three carbon atoms, and wherein R4 and R5 may form a ring together with the amine nitrogen, their salts with physiologically acceptable acids and, when the compounds can be in the form of optical isomers, the racemic mixture and the individual enantiomers.
    Type: Grant
    Filed: November 5, 1993
    Date of Patent: May 29, 2007
    Assignee: Pfizer Health AB
    Inventors: Rolf A. Johansson, Pinchas Moses, Lisbeth Nilvebrant, Bengt A. Sparf