Nitro Bonded Directly To The Carbocyclic Ring Patents (Class 544/167)
  • Publication number: 20150093365
    Abstract: Provided herein are compositions containing photoactivatable caged tamoxifen and tamoxifen derivative molecules. Also provided are kits containing one of these compositions and a light source. Also provided are methods of optically inducing nuclear translocation of a fusion protein containing a mammalian estrogen receptor ligand binding domain in a eukaryotic cell and methods of optically inducing recombination in a eukaryotic cell that include contacting a eukaryotic cell with at least one of these compositions. Also provided are methods of treating breast cancer in a subject that include administering a photoactivatable caged tamoxifen or tamoxifen derivative molecule to a subject having breast cancer.
    Type: Application
    Filed: March 14, 2013
    Publication date: April 2, 2015
    Inventors: Xin Lu, Sarit S. Agasti, Ronald A. DePinho, Ralph Weissleder
  • Publication number: 20110251197
    Abstract: The presently disclosed subject matter provides compounds of the formula, formula (Ia): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, X, Y, and n are as defined herein. Also disclosed are methods for making the compounds of the formula as set forth hereinabove, their use in inhibiting acid ceramidase and ceramidase-related activity, and their use as drugs and prodrugs in the treatment and/or prevention of diseases associated with undesirable ceramidase or sphingosine kinase activity, including, but not limited to, cancer, cancer metastasis, atherosclerosis, stenosis, inflammation, asthma, and atopic dermatitis.
    Type: Application
    Filed: November 6, 2009
    Publication date: October 13, 2011
    Inventors: Alicja Bielawska, Aiping Bai, Zdzislaw M. Szulc, Yusef A. Hannun, James Norris, Liu Xiang
  • Publication number: 20110172421
    Abstract: An object of the present invention is to provide a novel photobase generator which can sensitively generate a base even by h-ray in place of a conventional 2-nitro-4,5-dimethoxybenzyloxycarbonylamine compound. Disclosed is an N-(?-aromatic group-substituted-2-nitro-4,5-dialkoxybenzyloxycarbonyl)amine compound represented by the following general formula (I). (In the above formula (I), R1 to R9 denote specific groups.
    Type: Application
    Filed: October 1, 2009
    Publication date: July 14, 2011
    Applicant: SHOWA DENKO K.K.
    Inventors: Isao Yamagami, Yoshihiko Maeda, Hiroshi Yasuda, Katsumi Murofushi
  • Publication number: 20080255124
    Abstract: This invention relates to non-steroidal compounds that are modulators of androgen, glucocorticoid, mineralocorticoid, and progesterone receptors, and also to the methods for the making and use of such compounds.
    Type: Application
    Filed: October 13, 2005
    Publication date: October 16, 2008
    Applicant: Smithkline Beecham Corporation
    Inventors: Philip Stewart Turnbull, Andrew Lamont Larkin, Istvan Kaldor, Rodolfo Cadilla, David John Cowan, Eugene Stewart
  • Patent number: 6953797
    Abstract: There is disclosed the use of a compound of formula (I), wherein R1, R2, X, Y, V, W and Z are as defined in the specification, and pharmaceutically acceptable salts, enantiomers or racemates thereof, in the manufacture of a medicament, for the treatment or prophylaxis of diseases or conditions in which inhibition of nitric oxide synthase activity is beneficial. Certain novel compounds of formula (Ia) and pharmaceutically acceptable salts thereof, and enantiomers and racemates thereof are disclosed; together with processes for their preparation, compositions containing them and their use in therapy.
    Type: Grant
    Filed: February 20, 2001
    Date of Patent: October 11, 2005
    Assignee: AstraZeneca AB
    Inventors: David Cheshire, Stephen Connolly, David Cox, Ian Millichip
  • Patent number: 6875764
    Abstract: The present invention relates to novel compounds, pharmaceutical compositions containing the same as well as a method for treatment of parasitic disorders, wherein said compounds are administered. The present compounds are especially well suited for treatment of coccidiosis, particularly in poultry, and they have general formula (I): where Y is S or O and R is as defined in the specification.
    Type: Grant
    Filed: October 27, 2000
    Date of Patent: April 5, 2005
    Assignee: New Pharma Research Sweden AB
    Inventors: Sabrina Muzi, ShoaĆ” Abdul Rahman
  • Publication number: 20040259868
    Abstract: Compounds of formula (I) 1
    Type: Application
    Filed: July 6, 2004
    Publication date: December 23, 2004
    Inventors: John Walter Liebeschuetz, Christopher William Murray, Stephen Clinton Young, Nicholas Paul Camp, Stuart Donald Jones, William Alexander Wylie, John Joseph Masters, Michael Robert Wiley, Scott Martin Sheehan, David Birenbaum Engel, Brian Morgan Watson
  • Publication number: 20040127494
    Abstract: There is provided a series of novel &agr;-(N-sulfonamido)acetamide compounds of the Formula (I) 1
    Type: Application
    Filed: December 20, 2002
    Publication date: July 1, 2004
    Inventors: Michael F. Parker, Katharine E. McElhone, Robert A. Mate, Joanne J. Bronson, Yonghua Gai, Carl P. Bergstrom, Lawrence R. Marcin, John E. Macor
  • Publication number: 20040110945
    Abstract: The present invention relates to a compound represented by the following formula (I): 1
    Type: Application
    Filed: June 30, 2003
    Publication date: June 10, 2004
    Inventors: Atsushi Nakayama, Nobuo Machinaga, Yoshiyuki Yoneda, Yuichi Sugimoto, Jun Chiba, Toshiyuki Watanabe, Shin Iimura
  • Publication number: 20040097500
    Abstract: Compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are provided as well.
    Type: Application
    Filed: August 27, 2003
    Publication date: May 20, 2004
    Inventors: Jun Liao, David Gschneider, John J. Weidner, Nai Fang Wang
  • Patent number: 6727360
    Abstract: The present invention relates to processes for the production of &agr;-aryl-&bgr;-ketonitriles, which serve as synthetic intermediates in the preparation of a series of biologically important molecules such as corticotropin releasing factor (CRF) receptor antagonists.
    Type: Grant
    Filed: March 13, 2003
    Date of Patent: April 27, 2004
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Jiacheng Zhou, Lynette May Oh, Philip Ma
  • Publication number: 20040077855
    Abstract: Invented are non-peptide TPO mimetics. Also invented is a method of treating thrombocytopenia, in a mammal, including a human, in need thereof which comprises administering to such mammal an effective amount of a selected hydroxy-1-azobenzene derivative.
    Type: Application
    Filed: August 28, 2003
    Publication date: April 22, 2004
    Inventors: Kevin J. Duffy, Juan I Luengo, Antony N Shaw
  • Patent number: 6693192
    Abstract: The present invention relates to the synthesis and the evaluation of the antioxidant, hypocholesterolemic and hypolipidemic activity of substituted morpholine derivatives of formula (I) in which R1=CH2CH3, R2=CH3, R3, R4=H, R5=C6H5 (compound 1) or R1=CH2CH2CH2ONO2, R2=CH3, R3, R4=H, R5=C6H5 (compound 2) or R1=H, R2—R3=(CH2)4, R4=H, R5=C6H5 (compound 3) or R1=CH2CH2CH3, R2—R3=(CH2)4, R4=H, R5=C6H5 (compound 4) or R1=CH2CH2CH2ONO2, R2—R3=(CH2)4, R4=H, R5=C6H5 (compound 5) or R1=H, R2=CH3, R3—R4=(CH2)4, R5=C6H5 (compound 6) or R1=CH2CH2CH3, R2=CH3, R3—R4=(CH2)4, R5=C6H5 (compound 7) or R1=CH2CH2CH2ONO2, R2=CH3, R3—R4=(CH2)4, R5=C6H5 (compound 8) or R1=CH2CH2CH2ONO2, R2=CH3, R3, R4=H, R5=C6H5 (compound 9) or R1=H, R2&equals
    Type: Grant
    Filed: October 11, 2001
    Date of Patent: February 17, 2004
    Assignee: Elpen S.A.
    Inventors: Michael Chrysselis, Eleni Rekka, Panagiotis Kourounakis
  • Patent number: 6689882
    Abstract: A new improved process for synthesizing morpholinylbenzenes of the formula I by reacting morpholine of formula II with a substituted benzene of formula III, wherein morpholine is used as a reactant and as the only one solvent.
    Type: Grant
    Filed: November 12, 2002
    Date of Patent: February 10, 2004
    Assignee: AstraZeneca AB
    Inventor: Wei Tian
  • Publication number: 20030232811
    Abstract: The present invention relates to an anthranilic acid derivative expressed by the following formula (1) or the following formula (2), or its pharmacologically permissible salt or solvate.
    Type: Application
    Filed: January 31, 2003
    Publication date: December 18, 2003
    Applicant: TEIJIN LIMITED
    Inventors: Naoki Tsuchiya, Susumu Takeuchi, Takumi Takeyasu, Naoki Hase, Takao Yamori, Takashi Tsuruo
  • Publication number: 20030224940
    Abstract: The invention relates to novel pesticidally active &agr;-sulfin and &agr;-sulfonamino acid amides of the general formula (I) including the optical isomers thereof and mixtures of such isomers, wherein n is a number zero or one; R1, R2, R3, R4, R5, R6 and R7 have the meanings given in the specification, and R8 is either hydrogen, (a), (b), (c), (d) or (e) wherein R11, R12, R13, R15 and R17 are each independently hydrogen or C1-C4 alkyl, R13 is C4-C12 alkyl, C1-C12 halogenalkyl; C3-C8 cycloalkyl; optionally substituted aryl or optionally substituted heteroaryl, R16 is optionally substituted aryl or optionally substituted heteroaryl; and Z is oxygen, sulfur —CR18R19— or —NR2O—, wherein R18, R19 and R20 independently of each other are hydrogen or C1-C4 alkyl. The novel compounds possess plant-protecting properties and are suitable for protecting plants against infestation by phytopathogenic microorganisms.
    Type: Application
    Filed: May 6, 2003
    Publication date: December 4, 2003
    Inventors: Martin Zeller, Clemens Lamberth, Henry Szczepanski, Alain De Mesmaeker
  • Publication number: 20030220496
    Abstract: The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula 1
    Type: Application
    Filed: February 12, 2003
    Publication date: November 27, 2003
    Applicant: Merrell Pharmaceuticals, Inc.
    Inventors: Richard C. Krauss, Robert M. Strom, Carey L. Scortichini, William J. Kruper, Richard A. Wolf, Weishi W. Wu, Albert A. Carr, David A. Hay, Duane E. Rudisill, Gianbattista Panzone
  • Publication number: 20030212049
    Abstract: Compounds of the formula: 1
    Type: Application
    Filed: February 27, 2003
    Publication date: November 13, 2003
    Applicant: Wyeth
    Inventors: Jeremy I. Levin, James Ming Chen, Derek C. Cole, Mila T. Du, Leif M. Laakso
  • Publication number: 20030207871
    Abstract: The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.
    Type: Application
    Filed: February 19, 2003
    Publication date: November 6, 2003
    Inventors: Roger Dennis Tung, Michael Robin Hale, Christopher Todd Baker, Eric Steven Furfine, Istvan Kaldor, Wieslaw Mieczylaw Kazmierski, Andrew Spaltenstein
  • Publication number: 20030203898
    Abstract: The invention relates to novel diphenylmethane derivatives, processes for their preparation and their use in medicaments, in particular for the indications of arteriosclerosis and hypercholesterolaemia.
    Type: Application
    Filed: March 11, 2003
    Publication date: October 30, 2003
    Inventors: Helmut Haning, Gunter Schmidt, Josef Pernerstorfer, Hilmar Bischoff, Carsten Schmeck, Verena Vohringen, Michael Woltering, Axel Kretschmer, Christiane Faeste
  • Publication number: 20030199698
    Abstract: Novel compounds of the formula I 1
    Type: Application
    Filed: May 16, 2003
    Publication date: October 23, 2003
    Inventors: Horst Juraszyk, Dieter Dorsch, Werner Mederski, Christos Tsaklakidis, Christopher Barnes, Johannes Gleitz
  • Publication number: 20030195226
    Abstract: The present invention relates to novel oxime carbamyl derivatives and pharmaceutical compositions comprising said derivatives which inhibit fatty acid amide hydrolase. These pharmaceutical compositions are useful for the treatment of conditions which can be effected by inhibiting fatty acid amide hydrolase including, but not limited to, neuropathic pain, emesis, anxiety, altering feeding behaviors, movement disorders, glaucoma, brain injury, and cardiovascular disease.
    Type: Application
    Filed: February 4, 2003
    Publication date: October 16, 2003
    Inventors: Sing-Yuen Sit, Kai Xie, Hongfeng Deng
  • Publication number: 20030195212
    Abstract: The present invention relates to novel aromatic amines of general formula (I) and to the use of these amines for the treatment of obesity, anorexia, inflammation, mental disorders an other diseases associated with the melanocortin receptors or related systems, e.g. the melanocyte stimulating hormones.
    Type: Application
    Filed: November 20, 2002
    Publication date: October 16, 2003
    Inventors: Torbjorn Lundstedt, Anna Skottner, Elisabeth Seifert, Igor Starchenkov, Peteris Trapencieris, Valerjans Kauss, Ivars Kalvins, Arne Boman
  • Publication number: 20030191189
    Abstract: Compounds of Formula I are disclosed which are useful as fungicides 1
    Type: Application
    Filed: November 25, 2002
    Publication date: October 9, 2003
    Inventors: Gregory S. Basarab, Lee Dalton Jennings, Dennis R. Rayner
  • Publication number: 20030181717
    Abstract: Novel chiral derivitaves of non-nucleoside inhibitors (NNI), particularly R-isomers of halopyridyl and thiazoyl thiourea compounds are provided as potent inhibitors of reverse transcriptase (RT), and particularly of retroviral RT, most particularly HIV RT. The stereospecific compounds and compositions of the invention inhibit replication of retrovirus, particularly human immunodeficiency virus-1 (HIV-1) and drug resistant strains.
    Type: Application
    Filed: January 21, 2003
    Publication date: September 25, 2003
    Applicant: Parker Hughes Institute located at Roseville, Minnesota
    Inventors: Fatih M. Uckun, Taracad K. Venkatachalam
  • Publication number: 20030171349
    Abstract: This invention relates to a novel class of partial or full muscarinic receptor agonists intermediates for their preparation, and pharmaceutical compositions and methods of use for the treatment or prevention of diseases the treatment or prevention of which is mediated by muscarinic receptor agonism.
    Type: Application
    Filed: February 28, 2003
    Publication date: September 11, 2003
    Inventors: Anabella Villalobos, Daniel Yohannes, Jolanta Nowakowski, Dane R. Liston
  • Publication number: 20030158180
    Abstract: A compound having the general formula (Ia) and methods of using such compounds for the treatment of diseases and pharmaceutical composition comprising such compounds.
    Type: Application
    Filed: October 3, 2002
    Publication date: August 21, 2003
    Inventor: Peter Bernstein
  • Publication number: 20030153559
    Abstract: The invention refers to novel propenecarboxylic acid amidoxime derivatives furthermore N-oxides and/or geometrical isomers and/or optical isomers and/or pharmaceutically suitable acid addition salts and/or quaternary derivatives thereof. The novel compounds are suitable for the treatment of a state connected with oxygen deficit and/or energy deficit, or a disease based on PARP inhibition, especially an autoimmune or neurodegenerative disease, and/or a viral disease, and/or a disease caused by a toxic effect.
    Type: Application
    Filed: November 20, 2002
    Publication date: August 14, 2003
    Inventors: Peter Literati Nagy, Balazs Sumegi, Kalman Takacs
  • Publication number: 20030152600
    Abstract: The invention concerns novel compounds of the N-acylamino-amide family, compositions, in particular cosmetic or pharmaceutical, containing them, and their use for treating body or face skin ageing, whether chronobiologic or light-induced, and in particular skin ageing caused by decrease of skin elasticity and/or by collagen degradation in the structure of tissues.
    Type: Application
    Filed: December 6, 2002
    Publication date: August 14, 2003
    Inventors: Maria Dalko, Yann Mahe, Lionel Breton
  • Publication number: 20030149015
    Abstract: Phenylamino benzoic acid, benzamides, and benzyl alcohol derivatives of the formula 1
    Type: Application
    Filed: December 10, 2002
    Publication date: August 7, 2003
    Inventors: Stephen Douglas Barrett, Alexander James Bridges, Donna Reynolds Cody, Annette Marian Doherty, David Thomas Dudley, Alan Robert Saltiel, Mel Conrad Schroeder, Haile Tecle
  • Publication number: 20030149043
    Abstract: NHE-1 inhibitors, methods of using such NHE-1 inhibitors and pharmaceutical compositions containing such NHE-1 inhibitors. The NHE-1 inhibitors are useful for the reduction of tissue damage resulting from tissue ischemia.
    Type: Application
    Filed: December 9, 2002
    Publication date: August 7, 2003
    Applicant: Pfizer Inc.
    Inventors: Ernest S. Hamanaka, Angel Guzman-Perez, Christian J. Mularski, Roger B. Ruggeri, Ronald T. Wester
  • Publication number: 20030144505
    Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof: 1
    Type: Application
    Filed: January 16, 2003
    Publication date: July 31, 2003
    Applicant: SmithKline Beecham p.l.c.
    Inventors: Steven Mark Bromidge, Francis David King, Paul Adrian Wyman
  • Patent number: 6479491
    Abstract: The present invention relates to compounds of formula (I), any of it enantiomers, or any mixture thereof, or a pharmaceutically acceptable acid addition salt thereof, wherein R1, R2, R3, R4, R11, R12, R13, R14 and R15 each independently are hydrogen, alkyl, alkoxy, halogen, trifluoromethyl, nitro, cyano, amino, acyl, alkylamino, dialkylamino, aminocarbonyl, or acylamino; R5 is hydrogen, alkyl, alkoxyalkyl, or phenylalkyl; X is —CH2—Z—, Z—CH2—, NH—CO—, —CO—NH—, or —CH═CH—; wherein Z is O, S, CH2, or NH; Y is O, —CH2—W—, —W—CH2—; wherein W is O, or S; and n is 0, 1 or 2. The compounds are useful in the treatment of psychotic disorders.
    Type: Grant
    Filed: November 13, 2000
    Date of Patent: November 12, 2002
    Assignee: Neurosearch A/S
    Inventors: Oskar Axelsson, Dan Peters, Jorgen Scheel-Kruger, Elsebet Ostergaard Nielsen
  • Patent number: 6100428
    Abstract: An improved method for guanylating amines is provided. Broadly, the amines are reacted with a guanylating agent in the presence of a nickel catalyst. Preferably, the nickel catalyst comprises nickel in the zero oxidation state. Suitable nickel(0) catalysts are derived from nickel-boride alloys, nickel-phosphide alloys, aluminum-nickel alloys, nickel on kieselguhr, and nickel on silica/alumina catalysts. Preferred guanylating agents are thioureas and isothioureas. In one embodiment, protecting groups are selectively attached to the guanylating agents to yield particular substituted guanidines. The preferred protecting groups are Boc groups, Cbz groups, and arylsulfonyl groups. The reactions are particularly well suited for guanylating primary and secondary amines. The methods of the invention can be carried out under ambient conditions to provide high yields of the corresponding guanidines, with the nickel catalyst being essentially completely recoverable for reuse.
    Type: Grant
    Filed: October 6, 1999
    Date of Patent: August 8, 2000
    Assignee: The University of Kansas
    Inventors: Laxminarayan Bhat, Gunda I. Georg
  • Patent number: 5972939
    Abstract: The compounds of formula I are useful in treating gastrointestinal disorders associated with antagonizing the motilin receptor disorders. The compounds compete with erythromycin and motilin for the motilin receptor. In addition the compounds are antagonists of the contractile smooth muscle response to those ligands.
    Type: Grant
    Filed: October 26, 1998
    Date of Patent: October 26, 1999
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Robert H. Chen, Min Xiang, John B. Moore, Jr., Mary Pat Beavers
  • Patent number: 5514819
    Abstract: The present invention provides a dye-donor element for use according to thermal dye sublimation transfer, said dye-donor element comprising a support provided with a dye layer containing a dye and a polymeric binder, characterized in that said dye corresponds to the following formula: ##STR1## wherein R.sup.1 to R.sup.12 are as set out in the claims and the description.
    Type: Grant
    Filed: September 20, 1994
    Date of Patent: May 7, 1996
    Assignee: Agfa-Gevaert N.V.
    Inventor: Luc Vanmaele
  • Patent number: 5453517
    Abstract: The invention relates to fluorescent and/or reactive derivatives of 1,2-bis-(2-aminophenoxyethane)-N,N,N',N'-tetraacetic acid (BAPTA) according to the formula: ##STR1## where at least one of W and X is a functional group, with or without a spacer, that terminates in an alcohol or phenol, a thiol, a haloacetamide, an alkyl halide, an amine or aniline, a carboxylic acid, an anhydride, an isocyanate, an isothiocyanate, a maleimide, or an activated ester. The BAPTA-like molecule may be further substituted, one or more times, by additional functional groups with or without spacers or by CH.sub.3, NO.sub.2, CF.sub.3, F, Cl, Br, I, or carboxylic acid derivatives or pharmaceutically acceptable salts thereof, or by indolyl or benzofuran fluorophores. The functional groups allow for subsequent covalent attachment of one or more oxygen heterocycle fluorophores (e.g. fluorescein, coumarin, rhodamine); or polymolecular assemblies (e.g.
    Type: Grant
    Filed: February 25, 1992
    Date of Patent: September 26, 1995
    Assignee: Molecular Probes, Inc.
    Inventors: Michael A. Kuhn, Richard P. Haugland
  • Patent number: 5389653
    Abstract: Catechol derivatives of the formula ##STR1## wherein Ra, Rb and Rc have the significance given herein, the ester and ether derivatives thereof which are hydrolyzable under physiological conditions and the pharmaceutically acceptable salts thereof are described and possess valuable pharmacological properties. In particular, they inhibit the enzyme catechol-O-methyltransferase (COMT), a soluble, magnesium-dependent enzyme which catalyses the transference of the methyl group of S-adenosylmethionine to a catechol substrate, whereby the corresponding methyl ethers are formed. Suitable substrates which can be O-methylated by COMT and which can thus be deactivated are, for example, extraneuronal catecholamines and exogeneously-administered therapeutically active substances having a catechol structure.Formula Ia above embraces not only compounds which form part of the invention, but also known compounds; the compounds which form part of the invention can be prepared according to known methods.
    Type: Grant
    Filed: April 16, 1993
    Date of Patent: February 14, 1995
    Assignee: Hoffman-La Roche Inc.
    Inventors: Karl Bernauer, Janos Borgulya, Hans Bruderer, Mose Da Prada, Gerhard Zurcher
  • Patent number: 5290756
    Abstract: Compounds of the formula: ##STR1## wherein X is hydrogen, halo, trihalomethyl, alkyl, nitroor cyano; X.sup.1 is hydrogen, halo, or trihalomethyl; R.sup.1 and R.sup.2 are hydrogen, alkyl phenyl or benzyl; n is 1 to 5, and Z is halo, cyano, nitro, trihalomethyl, methylthio, methylsulfinyl, methylsulfonyl, acetyl, phenyl, or heterocycle, and compositions containing these compounds exhibit herbicidal activity.
    Type: Grant
    Filed: June 8, 1982
    Date of Patent: March 1, 1994
    Assignee: Rohm and Haas Company
    Inventors: Colin Swithenbank, Ted Fujimoto
  • Patent number: 5283352
    Abstract: Catechol compounds of formula I ##STR1## where R.sub.1, R.sub.2, R.sub.3 and X are as described herein are effective Catechol-O-methyltransferase inhibitors.
    Type: Grant
    Filed: December 7, 1992
    Date of Patent: February 1, 1994
    Assignee: Orion-yhtyma Oy
    Inventors: Reijo J. Backstrom, Kalevi E. Heinola, Erkki J. Honkanen, Seppo K. Kaakkola, Pekka J. Kairisalo, Inge-Britt Y. Linden, Pekka I. Mannisto, Erkki A. O. Nissinen, Pentti Pohto, Aino K. Pippuri, Jarmo J. Pystynen
  • Patent number: 5140026
    Abstract: Compounds of this invention are represented by the formula: ##STR1## wherein Z is a C.sub.1 -C.sub.6 alkylene group and R is an alkyl or substituted alkyl group. Class III antiarrhythmic activity is determined in vitro using an electrophysiological test where prolongation of the action potential duration is an indication of activity.
    Type: Grant
    Filed: May 9, 1991
    Date of Patent: August 18, 1992
    Assignee: A. H. Robins Company, Incorporated
    Inventors: Mark R. Hellberg, James R. Shanklin, Jr.
  • Patent number: 5053504
    Abstract: A process is disclosed for providing benzazepine intermediates of the formulae ##STR1## wherein R.sub.3, R.sub.4 and Y are as defined herein, which intermediates are useful in a process for the preparation of pharmaceutically useful benzazepine derivatives.
    Type: Grant
    Filed: November 29, 1989
    Date of Patent: October 1, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Wen-Sen Li, John K. Thottathil, Michael Murphy
  • Patent number: 5026401
    Abstract: There are described dyeing compositions for keratin fibres, and in particular for human hair, containing a dyestuff of the formula: ##STR1## in which A denotes an alkylene group, an alkylene group substituted by one or more OH groups, or an alkylene group interrupted by a hetero-atom such as oxygen or by an --NH-- group, R.sub.1 and R.sub.2, which are identical or different, denote hydrogen, alkyl, monohydroxyalkyl or polyhydroxyalkyl, or R.sub.1 and R.sub.2 can together form a heterocyclic ring chosen from among piperidino or morpholino groups, Y denotes alkoxy or NO.sub.2, R denotes hydrogen or lower alkyl, and if Y denotes alkoxy, Z denotes NO.sub.2 and is located in the para-position to the amine group, and if Y denotes NO.sub.2, (a) Z denotes alkoxy or OH and is located in the para-position to the NO.sub.2 group, or alternatively (b) Z denotes OH and is located in the para-position to the amine group, and also their cosmetically acceptable salts. Many of these dyestuff are novel.
    Type: Grant
    Filed: September 13, 1989
    Date of Patent: June 25, 1991
    Assignee: L'Oreal
    Inventors: Andree Bugaut, Herve Borowiak
  • Patent number: 4959366
    Abstract: A series of [N-alkyl-N-(nitro-, alkylsulphonamido, or amino-phenalkyl)amino]-alkyl, alkoxy or alkylthio phenyl derivatives having utility as anti-arrhythmic agents.
    Type: Grant
    Filed: April 29, 1987
    Date of Patent: September 25, 1990
    Assignee: Pfizer Inc.
    Inventors: Peter E. Cross, Geoffrey N. Thomas, John E. Arrowsmith
  • Patent number: 4935421
    Abstract: Novel compounds of the general formula ##STR1## wherein Ar represents a substituted or unsubstituted aromatic or heterocyclic group; W represents alkylene of from 1 to about 10 carbon atoms; and B represents --NR.sub.2 COR.sub.1, --NR.sub.2 CONR.sub.1 R.sub.3, --NR.sub.2 SO.sub.2 R.sub.1, --NR.sub.2 SO.sub.2 NR.sub.1 R.sub.3, or --NR.sub.2 COOR.sub.1 wherein R.sub.1, R.sub.2 and R.sub.3 may be the same or different and may be hydrogen, alkyl, alkoxyalkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, or aralkyl, except that R.sub.1 is not hydrogen when B is --NR.sub.2 SO.sub.2 R.sub.1 or --NR.sub.2 COOR.sub.1, or R.sub.1 and R.sub.3 may together with N form a 5 to 7 membered heterocyclic group; and the pharmaceutically acceptable salts thereof. These compounds exhibit .beta.-adrenergic blocking activity and are also useful in the treatment of glaucoma.
    Type: Grant
    Filed: March 1, 1989
    Date of Patent: June 19, 1990
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Sheung T. Kam, William L. Matier
  • Patent number: 4933367
    Abstract: This invention relates to carboxylic acid derivatives and their use thereof. The compounds are useful in treatment of various diseases such as diabetes, prediabetic conditions, adipositas ailments or atherosclerosis.
    Type: Grant
    Filed: March 12, 1987
    Date of Patent: June 12, 1990
    Assignee: Boehringer Mannheim GmbH
    Inventors: Hans P. Wolff, Ernst-Christian Witte, Hans-Frieder Kuhnle
  • Patent number: 4923863
    Abstract: Compounds are disclosed of formula (I): ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and are C.sub.1-6 alkyl or C.sub.3-6 alkenyl; or --NR.sub.1 R.sub.2 forms a 5-membered (optionally containing an oxygen atom adjacent to the nitrogen) or a 6-membered ring, which ring optionally contains one unit of unsaturation and which is unsubstituted or substituted by hydroxy, oxo, optionally substituted methylidene, --COR.sub.3 (where R.sub.6 represents C.sub.1-6 alkyl, OR.sub.4 or --NHR.sub.4, and R.sub.4 represents hydrogen, C.sub.1-6 alkyl, aryl, ar(C.sub.1-6)alkyl) or .dbd.NOR.sub.5 (where R.sub.5 represents C.sub.1-6 alkyl);X represents a direct bond, --CH.sub.2 -- or --CH.sub.2 O--;Ar represents a substituted phenyl moiety;and physiologically acceptable salts thereof.The compounds are indicated as useful for the treatment of pain and cerebral ischaemia.Processes and intermediates for their preparation and pharmaceutical compositions containing them are also disclosed.
    Type: Grant
    Filed: June 6, 1989
    Date of Patent: May 8, 1990
    Assignee: Glaxo Group Limited
    Inventors: David I. C. Scopes, David E. Bays
  • Patent number: 4910200
    Abstract: Compounds of the formula ##STR1## wherein A is ##STR2## B is ##STR3## R.sup.1 is hydrogen; halogen, cyano or optionally substituted C.sub.1-4 alkyl; andQ is NR.sup.8 R.sup.9 or ##STR4## where R.sup.2 to R.sup.11 are substituents of various types. The compounds are useful as fungicides.
    Type: Grant
    Filed: October 9, 1986
    Date of Patent: March 20, 1990
    Assignee: Celamerck GmbH & Co. KG
    Inventors: Jurgen Curtze, Helmut Pieper, Josef Nickl, Heinz-Manfred Becher, Guido Albert, Christo Drandarevski, Sigmund Lust, Ludwig Schroder
  • Patent number: 4889953
    Abstract: Compounds of the formula: ##STR1## wherein R.sup.1 is a higher alkyl group which may be substituted; R.sup.2 is a hydrogen, a lower alkyl group which may be substituted, a lower alkanoyl group which may be substituted or a lower alkylthiocarbamoyl group; R.sup.3 is a primary to tertiary amino group or a quaternary ammonium group; and n is 2 or 3, and salts thereof, have antitumor activity and platelet activating factor inhibitory activity.
    Type: Grant
    Filed: July 22, 1987
    Date of Patent: December 26, 1989
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Keizo Inoue, Hiroaki Nomura, Tetsuya Okutani
  • Patent number: 4859206
    Abstract: This invention encompasses compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 independently are hydrogen, C.sub.1-4 alkyl, or C.sub.2-4 hydroxyalkyl; one of R.sup.3 to R.sup.7 is --SO.sub.3 H or --COOH; and the remaining of R.sup.3 to R.sup.7 independently are hydrogen, chlorine, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, or --NR.sup.8 R.sup.9, where R.sup.8 and R.sup.9 independently are hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkoxy, or where --NR.sup.8 R.sup.9 is piperidine, morpholine, piperazine, or pyrrolidone; or a water soluble salt thereof; hair dye preparation containing these compounds, and methods for dyeing hair using such preparation.
    Type: Grant
    Filed: February 26, 1988
    Date of Patent: August 22, 1989
    Assignee: Henkel Kommanditgesellschaft auf Aktien
    Inventors: David Rose, Edgar Lieske, Horst Hoeffkes, Norbert Maak