Chalcogen Or Nitrogen Attached Indirectly To The Tricyclo Ring System By Acyclic Nonionic Bonding Patents (Class 548/444)
  • Publication number: 20030129513
    Abstract: Charge transport compounds are described that have a multiple number of hydrazone-bridged heterocyclic groups (especially julolidine, carbazole and/or triarylmethane groups) connected by a central bridging group.
    Type: Application
    Filed: September 24, 2001
    Publication date: July 10, 2003
    Applicant: Samsung Electronics Co., Ltd.
    Inventors: Nusrallah Jubran, Hwan Koo Lee, Kam W. Law
  • Publication number: 20030119893
    Abstract: The present invention is concerned with pseudopolymorphic forms of 1-(4-carbazolyloxy)-3-[2-(2-methoxyphenoxy)ethylamino]-2-propanole (carvedilol) or of optically active forms or pharmaceutically acceptable salts thereof, processes for the preparation thereof and pharmaceutical compositions containing them.
    Type: Application
    Filed: September 26, 2002
    Publication date: June 26, 2003
    Inventors: Andre Gerard Bubendorf, Rolf-Dieter Gabel, Michael Hennig, Siegfried Krimmer, Guenter Neugebauer, Walter Preis, Alexander Wirl
  • Publication number: 20030113132
    Abstract: A novel charge transport compound, a novel process using that novel compound and an organophotoreceptor includes:
    Type: Application
    Filed: August 9, 2002
    Publication date: June 19, 2003
    Applicant: Samsung Information Systems America
    Inventors: Kam W. Law, Nusrallah Jubran, Zbigniew Tokarski, Alan R. Katritzky, Ritu Jain, Rexiat Maimait
  • Publication number: 20030113644
    Abstract: This invention relates to an organophotoreceptor that includes:
    Type: Application
    Filed: October 31, 2002
    Publication date: June 19, 2003
    Applicant: SAMSUNG Electronics Co., Ltd.
    Inventors: Kam W. Law, Nusrallah Jubran, Zbigniew Tokarski
  • Patent number: 6566529
    Abstract: This invention pertains to DTT-based compounds having two-photon absorption property containing electron donors and/or electron acceptors and having cross section value &sgr; that is higher than compound AF-50.
    Type: Grant
    Filed: May 19, 2000
    Date of Patent: May 20, 2003
    Assignee: The United States of America as represented by the Secretary of the Navy
    Inventors: Oh-Kil Kim, Han Young Woo, Kie-Soo Kim, Kwang-Sup Lee
  • Publication number: 20030073846
    Abstract: A compound of the formula (I) wherein X1 ? is bond or —O(CH2)m— (in which m is an integral number of 1, 2 or 3); X2 is bond, —(CH2)n—, etc. (in which n is an integral number of 1, 2 or 3); R1 is hydrogen or amino protective group; R2 is hydroxy(lower)alkyl or (lower)alkoxy(lower)alkyl; A is phenyl, pyridyl, indolyl or carbazolyl, each of which may be substituted with one or two substituent(s) selected from the group consisting of halogen, hydroxy, lower alkyl, etc.; and B is phenyl or pyridyl, each of which may be substituted with one or two substituent(s) selected from the group consisting of halogen, hydroxy, nitro, etc.; and a pharmaceutically acceptable salt thereof which is useful as a medicament.
    Type: Application
    Filed: August 6, 2002
    Publication date: April 17, 2003
    Inventors: Kiyoshi Taniguchi, Hiroshi Kayakiri, Minoru Sakurai, Naokaki Fujii, Kenichi Washizuka, Hitoshi Hamashima, Yasuyo Tomishima, Kaori Hamada, Nobuhiro Yamamoto, Hirofumi Ishikawa, Naoko Unami, Toshiko Miura
  • Patent number: 6528657
    Abstract: The object of this invention is to provide an illuminant, which can easily be produced at low cost. This invention is a carbazole derivative luminescent compound having a carbazole ring skeleton, to the nitrogen atom of which is attached an electron-donating group, and to the carbon atom of which is attached an electron-attracting group at the third position to the nitrogen atom.
    Type: Grant
    Filed: September 28, 2001
    Date of Patent: March 4, 2003
    Assignee: Taiho Industries Co., Ltd.
    Inventors: Tadao Nakaya, Takao Yamauchi, Akio Tajima, Hidemasa Mouri
  • Patent number: 6521667
    Abstract: The present invention features calcilytic compounds. “Calcilytic compounds” refer to compounds able to inhibit calcium receptor activity. Also described are the use of calcilytic compounds to inhibit calcium receptor activity and/or achieve a beneficial effect in a patient; and techniques which can be used to obtain additional calcilytic compounds.
    Type: Grant
    Filed: August 11, 1998
    Date of Patent: February 18, 2003
    Assignees: NPS Pharmaceuticals, Inc., SmithKline Beecham, PLC, SmithKline Beecham, Corp.
    Inventors: Eric G. Del Mar, Robert M. Barmore, Derek Sheehan, Bradford C. Van Wagenen, James F. Callahan, Richard M. Keenan, Nikesh R. Kotecha, Maria Amparo Lago, Linda Sue Southall, Mervyn Thompson
  • Patent number: 6515010
    Abstract: This invention relates to carvedilol methanesulfonate, compositions containing this compound and methods of using carvedilol methanesulfonate to treat hypertension, congestive heart failure and angina.
    Type: Grant
    Filed: May 15, 2002
    Date of Patent: February 4, 2003
    Assignee: SmithKline Beecham Corporation
    Inventors: Miriam Franchini, Gopadi M. Venkatesh
  • Patent number: 6514968
    Abstract: The present invention provides aminoalkoxy carbazole derivatives, and more specifically, provides compounds of formula (I) wherein R1, R2, R3, R4, R8 and R9 are described herein. These compounds are 5-HT ligands, and are useful for treating diseases wherein modulation of 5-HT activity is desired.
    Type: Grant
    Filed: August 31, 2000
    Date of Patent: February 4, 2003
    Assignee: Pharmacia & Upjohn Company
    Inventor: Ruth Elizabeth TenBrink
  • Publication number: 20030023099
    Abstract: The object of this invention is to provide an illuminant, which can easily be produced at low cost. This invention is a carbazole derivative luminescent compound having a carbazole ring skeleton, to the nitrogen atom of which is attached an electron-donating group, and to the carbon atom of which is attached an electron-attracting group at the third position to the nitrogen atom.
    Type: Application
    Filed: September 28, 2001
    Publication date: January 30, 2003
    Inventors: Tadao Nakaya, Takao Yamauchi, Akio Tajima, Hidemasa Mouri
  • Patent number: 6512123
    Abstract: Compounds of formula I wherein R1, R2, A, X, Y and Z have the meanings provided in the specification, and their enantiomers, diastereoisomers, racemates, pharmaceutically acceptable salts and mixtures thereof. These compounds have HDAC inhibitory activity for inhibiting cell proliferation. Also provided is a process of manufacturing these compounds.
    Type: Grant
    Filed: April 22, 2002
    Date of Patent: January 28, 2003
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Adelbert Grossmann, Wolfgang von der Saal, Tim Sattelkau, Ulrich Tibes
  • Patent number: 6495701
    Abstract: The present invention is directed to processes for the preparation of a compound useful for treating diabetes, obesity, hyperlipidemia and the like, which compound is represented by the formula (1): wherein R1 represents a lower alkyl group or a benzyl group; *1 represents an asymmetric carbon atom; R2 hydrogen atom, a halogen atom or a hydroxyl group; and A represents one of the following groups: wherein X represents NH, O or S; R6 represents a hydrogen atom, a hydroxyl group, an amino group or an acetylamino group; and *2 represents an asymmetric carbon atom when R6 is not a hydrogen atom, and to intermediates useful for the said processes. The processes of the present invention are convenient, practical preparing processes with low cost which comprise a small number of steps with good industrial work efficiency.
    Type: Grant
    Filed: September 26, 2001
    Date of Patent: December 17, 2002
    Assignee: Asahi Kasei Kabushiki Kaisha
    Inventors: Koki Matsubara, Hitoshi Kida
  • Publication number: 20020188123
    Abstract: Novel polydentate asymmetric nitrogen-oxygen-containing binaphthyl derivatives of the formulae (I) and (II), and metal complexes of these compounds may be used as catalysts for enantioselective transformations.
    Type: Application
    Filed: May 2, 2002
    Publication date: December 12, 2002
    Applicant: DEGUSSA AG
    Inventors: Axel Monsees, Carsten A. Schneider, Thomas Riermeier, Uwe Dingerdissen
  • Publication number: 20020143045
    Abstract: This invention relates to an improved process of preparing carvedilol, as well as a new crystalline hydrate and solvate and forms of carvedilol, processes for the manufacture thereof, and pharmaceutical compositions thereof.
    Type: Application
    Filed: June 28, 2001
    Publication date: October 3, 2002
    Inventors: Jean Hildesheim, Sergey Finogueev, Judith Aronhime, Ben-Zion Dolitzky, Shoshana Ben-Valid, Ilan Kor
  • Publication number: 20020115869
    Abstract: The present invention provides a lambda-shaped carbazole based chromophore, and a main-chain NLO polyurethane containing the same. The lambda-shaped structure reduces the plasticization to the main-chain polymers caused by the chromophore and increases temporal stability of the NLO coefficients of the main-chain NLO polyurethane. The NLO coefficients of the main-chain NLO polyurethane are stable because the efficiency of dipole alignment in electric field is increased due to the dipole thereof being perpendicular to the main chain of the polyurethane.
    Type: Application
    Filed: September 5, 2001
    Publication date: August 22, 2002
    Inventors: Ging-Ho Hsiue, Wen-Jang Kuo, Ru-Jong Jeng
  • Publication number: 20020107405
    Abstract: The present invention features substituted carbazole compounds of formula (I): 1
    Type: Application
    Filed: November 21, 2001
    Publication date: August 8, 2002
    Inventors: Jiann T?apos;Suen Lin, K. R. Justin Thomas, Yu-Tai Tao, Chung-Wen Ko
  • Patent number: 6413991
    Abstract: Disclosed herein are selective beta 3 adrenergic agonists represented by the following structural formula: The variables in the structural formula shown above are defined in the specification. Also disclosed are methods of using these compounds for agonizing the beta 3 adrenergic receptor in patients in need of such treatment, for example, patients in need of treatment for obesity or Type II diabetes.
    Type: Grant
    Filed: June 30, 2000
    Date of Patent: July 2, 2002
    Assignee: Eli Lilly and Company
    Inventors: Thomas A. Crowell, Deborah A. Evrard, Charles D. Jones, Brian S. Muehl, Christopher J. Rito, Anthony J. Shuker, Andrew J. Thorpe, Kenneth J. Thrasher
  • Patent number: 6399631
    Abstract: Carbazoles of the formula which are effective in treating conditions associated with neuropeptide Y-5 neurotransmission.
    Type: Grant
    Filed: July 21, 2000
    Date of Patent: June 4, 2002
    Assignee: Pfizer Inc.
    Inventors: Richard L. Elliott, David A. Griffith, Marlys Hammond
  • Publication number: 20020065422
    Abstract: The present invention relates to methods for using a maleimide of formula (I) 1
    Type: Application
    Filed: May 21, 2001
    Publication date: May 30, 2002
    Inventors: Kazuhiko Kunimoto, Junji Otani, Kunihiko Kodama, Hiroshi Yamamoto, Patrick Verhoustraeten, Sonia Megert, Adalbert Braig
  • Patent number: 6340548
    Abstract: Organic photoreceptors that include a charge transport compound, a charge generating compound, and an electroconductive support in which the charge transport compound is a novel aryl hydrazone-functional carbazole compound.
    Type: Grant
    Filed: March 16, 2000
    Date of Patent: January 22, 2002
    Assignee: Imation Corp.
    Inventors: Nusrallah Jubran, Zbigniew Tokarski, Terrance P. Smith
  • Patent number: 6258954
    Abstract: The present invention relates to compounds of formula I provided that R1 and R2 not simultaneously stand for phenyl, the use thereof in, for example, electroluminescent devices and as void detection compounds.
    Type: Grant
    Filed: August 22, 2000
    Date of Patent: July 10, 2001
    Assignee: Ciba Specialty Chemicals Corp.
    Inventors: Kazuhiko Kunimoto, Junji Otani, Kunihiko Kodama, Hiroshi Yamamoto, Patrick Verhoustraeten, Sonia Megert, Adalbert Braig
  • Patent number: 6252104
    Abstract: A naphthol derivative represented by the general formula (I), [wherein Y and Y′ indicate —(CONH)n—X or —COR; X is a phenyl group, a naphthyl group, an anthraquinonyl group, a benzimidazolonyl group or a carbazolyl group; R is a hydroxyl group, an alkoxy group having 1 to 6 carbon atoms, a halogen atom, a benzyloxy group, a phenyloxy group or a phenacyloxy group; R2 is a hydrogen atom, an alkaline metal, an alkyl group having 1 to 6 carbon atoms, an acyl group having 1 to 6 carbon atoms or a phenylalkyl group; Z is a group selected from the group consisting of a hydrogen atom, a halogen atom, a nitro group, a nitroso group and an amino group (Z may be substituted on any ring of the naphthalene ring); and n is an integer of 1 or 2; provided that R2 and Z do not simultaneously indicate a hydrogen atom when both R simultaneously indicate a hydroxyl group], and a process for producing the same.
    Type: Grant
    Filed: December 12, 1996
    Date of Patent: June 26, 2001
    Assignee: Kabushiki Kaisha Ueno Seiyaku Oyo Kenkyujo
    Inventors: Ryuzo Ueno, Shigeru Ito, Kenji Minami, Masaya Kitayama
  • Patent number: 6245775
    Abstract: Cycloakano-indole and -azaindole derivatives are prepared by reaction of appropriately substituted carbonylic acids with amines. The cycloalkano-indole and -azaindole derivatives are suitable as active compounds for medicaments, preferably antiatherosclerotic medicaments.
    Type: Grant
    Filed: July 3, 1997
    Date of Patent: June 12, 2001
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ulrich Müller, Richard Connell, Siegfried Goldmann, Rudi Grützmann, Martin Beuck, Hilmar Bischoff, Dirk Denzer, Anke Domdey-Bette, Stefan Wohlfeil
  • Patent number: 6235755
    Abstract: The present invention provides non-peptidic amino derivatives, their therapeutic use as well as pharmaceutical compositions that possess activity as Follicle Stimulating Hormone (FSH) agonists and are useful in the for treatment of infertility. In particular, the invention provides cyclic and acyclic alpha- and beta-aminocarboxamides, more particularly tetrahydroisoquinolinecarboxamides, piperidinecarboxamides, pyrrolidinecarboxamides, and 2-amino-3-carboxamidopyridine derivatives.
    Type: Grant
    Filed: August 5, 1999
    Date of Patent: May 22, 2001
    Assignee: Applied Research Systems ARS Holding N.A.
    Inventors: Nabil El Tayer, Adulla Reddy, David Buckler, Sharad Magar
  • Patent number: 6194439
    Abstract: Certain tricyclic polyhydroxylic compounds, and their pharmaceutically-acceptable salts, are inhibitors of tyrosine kinase enzymes, and so are useful for the control of tyrosine kinase dependent diseases (e.g., cancer, atherosclerosis).
    Type: Grant
    Filed: November 23, 1993
    Date of Patent: February 27, 2001
    Assignee: Pfizer Inc.
    Inventor: Robert L. Dow
  • Patent number: 6140352
    Abstract: Disclosed herein are selective beta 3 adrenergic agonists represented by the following structural formula: ##STR1## The variables in the structural formula shown above are defined in the specification. Also disclosed are methods of using these compounds for agonizing the beta 3 adrenergic receptor in patients in need of such treatment, for example, patients in need of treatment for obesity or Type II diabetes.
    Type: Grant
    Filed: May 4, 1998
    Date of Patent: October 31, 2000
    Assignee: Eli Lilly and Company
    Inventors: Thomas A. Crowell, Deborah A. Evrard, Charles D. Jones, Brian S. Muehl, Christopher J. Rito, Anthony J. Shuker, Andrew J. Thorpe, Kenneth J. Thrasher
  • Patent number: 6080338
    Abstract: Described are novel water soluble photochromic naphthopyran and benzopyran compounds having an alkylaminoalkylamino group on the pyran portion or on the pyran portion and the naphtho- or benzo-portion thereof. These compounds may be represented by one of the following graphic formula: ##STR1## wherein B and/or B' is an alkylaminoalkylamino-substituted aryl group and R.sub.1 may also be an alkylaminoalkylamino group. Articles such as ophthalmic lenses or other plastic transparencies and coating compositions such as paints and inks that incorporate the novel water soluble compounds are also described.
    Type: Grant
    Filed: March 5, 1999
    Date of Patent: June 27, 2000
    Assignee: Transitions Optical, Inc.
    Inventor: Anil Kumar
  • Patent number: 6057347
    Abstract: Nonsteroidal antiinflammatory drugs which have been substituted with a nitrogen monoxide group; compositions comprising (i) a nonsteroidal antiinflammatory drug, which can optionally be substituted with a nitrogen monoxide group and (ii) a compound that directly donates, transfers or releases a nitrogen monoxide group (preferably as a charged species, particularly nitrosonium); and methods of treatment of inflammation, pain, gastrointestinal lesions and/or fever using the compositions are disclosed. The compounds and compositions protect against the gastrointestinal, renal and other toxicities that are otherwise induced by nonsteroidal antiinflammatory drugs.
    Type: Grant
    Filed: September 16, 1997
    Date of Patent: May 2, 2000
    Assignee: NitroMed, Inc.
    Inventors: David S. Garvey, L. Gordon Letts, H. Burt Renfroe, Sang William Tam
  • Patent number: 6037362
    Abstract: Compounds having a .beta.-3 adrenaline receptor agonist and are useful as drugs for the treatment and prevention of diabetes, obesity, hyperlipemia, etc., represented by a general formula (I) and salts thereof, and a process for producing these, and their intermediates, wherein R represents hydrogen or methyl; R.sup.1 represents hydrogen, halogen, hydroxy, benzyloxy, amino, or hydroxymethyl; R.sup.2 represents hydrogen, hydroxymethyl, NHR.sup.3, SO.sub.2 NR.sup.4 R.sup.4', or nitro; R.sup.6 represents hydrogen or lower alkyl; and X represents nitrogen, R.sup.9 represents hydrogen, one of R.sup.7 and R.sup.8 represent hydrogen, and the other thereof represents hydrogen, amino, acetylamino, or hydroxy.
    Type: Grant
    Filed: August 5, 1998
    Date of Patent: March 14, 2000
    Assignee: Asahi Kasei Kogyo Kabushiki Kaisha
    Inventors: Shiro Miyoshi, Kohei Ogawa
  • Patent number: 6013808
    Abstract: A process of purifying a (6-chloro-2-carbazolyl)methyl-malonic acid di(C.sub.1 -C.sub.6 alkyl) ester of Formula (I): ##STR1## wherein R.sub.a and R.sub.b must be the same and are selected from the group consisting of C.sub.1 -C.sub.6 alkyl; comprises phase separating one or more impurities from said carbazole ester at least once wherein the solvent used to carry out said phase separation is acetic acid. In a preferred embodiment said acetic acid is glacial acetic acid which is maintained at a temperature of from about 30.degree. to about 110.degree.0 C. and said carbazole ester is obtained in a purity of at least 99.90% by weight, so that the amount of impurities present therein is 0.10% or less by weight. In a more preferred embodiment of said process, said temperature is from about 50.degree. to about 70.degree. C., and said phase separation is carried out only once.
    Type: Grant
    Filed: April 15, 1999
    Date of Patent: January 11, 2000
    Assignee: Pfizer Inc.
    Inventors: Philip D. Hammen, Peter R. Rose, John L. Tucker, Keith M. Devries, Diane M. Rescek
  • Patent number: 6005085
    Abstract: The present invention provides novel condensed azo compounds using bisamide compounds of 2-hydroxynaphthalene-3,6-dicarboxylic acid, amide, or ester as the couplers, which have excellent properties such as excellent water resistance, chemical resistance, solvent resistance, and heat resistance.
    Type: Grant
    Filed: November 18, 1998
    Date of Patent: December 21, 1999
    Assignee: Kabushiki Kaisha Ueno Seiyaku Oyo Kenkyujo
    Inventors: Ryuzo Ueno, Masaya Kitayama, Kenji Minami, Hiroyuki Wakamori, Katsunori Tanikawa
  • Patent number: 5879592
    Abstract: Described are novel water soluble photochromic naphthopyran and benzopyran compounds having an alkylaminoalkylamino group on the naphtho- or benzo-portions and/or pyran portions thereof. These compounds may be represented by one of the following graphic formulae: ##STR1## wherein R.sub.1 is an alkylaminoalkylamino group. Articles such as ophthalmic lenses or other plastic transparencies and coating compositions such as paints and inks that incorporate the novel water soluble compounds are also described.
    Type: Grant
    Filed: December 10, 1997
    Date of Patent: March 9, 1999
    Assignee: PPG Industries, Inc.
    Inventor: Anil Kumar
  • Patent number: 5877199
    Abstract: A compound of formula (I): ##STR1## wherein Y.sup.1, Y.sup.2, Y.sup.3 and Y.sup.4 are each hydrogen, halogen, nitro, cyano, hydroxyl, thiol, amino, alkyl, haloalkyl, alkylthio, a protected or unprotected carboxyl, a protected or unprotected sulfonamide, or tetrazol; one of R.sup.1 and R.sup.2 is hydrogen, alkyl, aryl, aralkyl, oxazolyl, or a protected or unprotected carboxyl and the other of R.sup.1 and R.sup.2 is hydrogen, alkyl, aryl or aralkyl; and R.sup.3 is hydrogen or an amino protecting group, and pharmaceutically acceptable salts or esters thereof. The compounds are effective for treating dementia, Alzheimer's disease and delirium and are effective as sedatives.
    Type: Grant
    Filed: January 27, 1997
    Date of Patent: March 2, 1999
    Assignee: Sankyo Company, Limited
    Inventors: Nigel Birdsall, Sebastian Lazareno, Syunji Naruto, Masahiko Sugimoto, Kazuo Koyama, Shinji Marumoto
  • Patent number: 5824699
    Abstract: This invention provides compounds of formula I having the structure ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are, each, independently, hydrogen, alkyl, alkenyl, alkynyl, alkoxy, aralkoxy, trifluroalkoxy, alkanoyloxy, hydroxy, halo, trifluoromethyl, cyano, amino, mono- or di-alkylamino, alkanamido, or alkanesulfonamido;R.sub.5 is hydrogen, alkyl, alkenyl, alkoxyalkyl or alkylcycloalkyl;R.sub.6 is hydrogen, alkyl or alkenyl;X is oxygen or carbon;A is oxygen or NZ;Z is hydroxyl, alkoxy, aryloxy, carboxyalkyloxy of 2-7 carbon atoms, arylamino, or alkylsulfonyamino of 1-6 carbon atoms;or a pharmaceutically acceptable salt thereof, which are useful in the treatment of arthritic disorders, colorectal cancer, and Alzheimer's disease.
    Type: Grant
    Filed: March 16, 1998
    Date of Patent: October 20, 1998
    Assignee: American Home Products Corporation
    Inventors: Anthony F. Kreft, Craig E. Caufield, Amedeo A. Failli, Thomas J. Caggiano, Alexander A. Greenfield, Dennis M. Kubrak
  • Patent number: 5760057
    Abstract: The invention concerns acid derivatives of formula IR.sup.1 --CON(R.sup.2)--N(R.sup.3)CO--X.sup.1 --Q--X.sup.2 --G(I)and pharmaceutically acceptable metabolically labile esters or amides thereof, and pharmaceutically acceptable salts thereof, in which R.sup.1, R.sup.2, R.sup.3, X.sup.1, Q, X.sup.2 and G have the meanings given in the specification. The invention also concerns processes for the preparation of the acid derivatives of formula I, pharmaceutical compositions containing them their use as inhibitors of the binding of fibrinogen to glycoprotein IIb/IIIa.
    Type: Grant
    Filed: December 16, 1996
    Date of Patent: June 2, 1998
    Assignee: Zeneca Limited
    Inventors: Andrew George Brewster, Peter William Rodney Caulkett, Alan Wellington Faull, Robert James Pearce, Richard Eden Shute
  • Patent number: 5677328
    Abstract: Novel substituted carbazole compounds of Formula I are active as melatonergic agents: ##STR1## wherein: R.sub.1 is C(O)R.sub.3 or SO.sub.2 R.sub.4 ;R.sub.2 is H or C.sub.1-6 alkoxy;R.sub.3 is C.sub.1-6 alkyl, (CH.sub.2).sub.n SR.sub.4, (CH.sub.2).sub.n OR.sub.4, (CH.sub.2).sub.n SO.sub.2 R.sub.4, or NHR.sub.4 ;R.sub.4 is C.sub.1-4 alkyl; andm is 1 or 2; andn is 1 to 4.
    Type: Grant
    Filed: October 30, 1996
    Date of Patent: October 14, 1997
    Assignee: Bristol-Myers Squibb Company
    Inventors: Katherine S. Takaki, Marc A. Bruce, Graham S. Poindexter, Brett T. Watson, Joseph P. Yevich
  • Patent number: 5646295
    Abstract: The invention concerns diazapentalene derivatives of formula I ##STR1## in which X and Y represent leaving groups which are less nucleophilic than thiol compounds, as thiol-specific fluorochromes for the detection of compounds containing thiol groups, in particular in cells.
    Type: Grant
    Filed: January 31, 1996
    Date of Patent: July 8, 1997
    Assignee: Boehringer Mannheim GmbH
    Inventors: Rudolf Gompper, Manfred Kubbies, Axel Schmidt, Bernhard Virnekas
  • Patent number: 5621000
    Abstract: Nitric esters with pharmacological activity having general formula (I), their pharmaceutical utilisation and process for their preparation.
    Type: Grant
    Filed: May 26, 1995
    Date of Patent: April 15, 1997
    Assignee: Nicox S.A.
    Inventors: Barbara Arena, Piero Del Soldato
  • Patent number: 5607955
    Abstract: A tricyclic compound represented by the following formula (I): ##STR1## exhibits antagonism to angiotensin II receptors.
    Type: Grant
    Filed: May 1, 1995
    Date of Patent: March 4, 1997
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Etsuo Ohshima, Fumihiko Kanai, Hideyuki Sato, Hiroyuki Obase, Toshiaki Kumazawa, Shiho Takahara, Tetsuji Ohno, Tomoko Ishikawa, Koji Yamada
  • Patent number: 5541333
    Abstract: Novel tethered hapten intermediates and related conjugates based on carbazole and/or dibenzofuran, as well as methods for making and using such conjugates. Haptens based on the above core structures may be substituted at any position on the aromatic rings with a wide variety of substituents. Using tethered intermediates, immunogens, tracers, solid supports and labeled oligonucleotides are all described; as are methods for using the intermediates to prepare the conjugates, methods of using the conjugates to make and purify antibodies, as assay tracers, and in nucleic acid hybridization assays. Kits containing haptenated oligonucleotides and anti-hapten conjugates are also described.
    Type: Grant
    Filed: April 13, 1995
    Date of Patent: July 30, 1996
    Assignee: Abbott Laboratories
    Inventor: James R. Fino
  • Patent number: 5519134
    Abstract: Novel pyrrolidine monomers bearing various functional groups are used to prepare oligomeric structures. The pyrrolidine monomers can be joined via standard phosphate linkages including phosphodiester and phosphorothioate linkages. Useful functional groups include nucleobases as well as polar groups, hydrophobic groups, ionic groups, aromatic groups and/or groups that participate in hydrogen-bonding.
    Type: Grant
    Filed: January 11, 1994
    Date of Patent: May 21, 1996
    Assignee: Isis Pharmaceuticals, Inc.
    Inventors: Oscar L. Acevedo, Normand Hebert
  • Patent number: 5496834
    Abstract: The present invention provides novel compound of the formulas (Ia) or (I): ##STR1## wherein Q is one or two amino acid residues which may be substituted; R.sup.3 is a carboxyl group which may be esterified or an acyl group; A is an alkylene group; B is hydrogen or an alkyl group which may be substituted or an acyl group; or a salt thereof; ##STR2## wherein R.sup.1 and R.sup.2 may be the same or different and each is hydrogen or a hydrocarbon residue which may be substituted; R.sup.3, A and B have the same definitions as those shown above; m and n each is 0 or 1; provided that where both m and n are both equal to 0, R.sup.3 is a carboxyl group which may be esterified or an acyl group having not less than 7 carbon atoms; or a salt thereof.The compound (Ia) or (I) shows cathepsin L inhibitory and bone resorption inhibitory activities and are useful as a prophylactic/therapeutic agent for osteoporosis.
    Type: Grant
    Filed: September 2, 1994
    Date of Patent: March 5, 1996
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Takashi Sohda, Yukio Fujisawa, Satoru Oi, Junji Mizoguchi
  • Patent number: 5457122
    Abstract: The phenylalkan(en)oic acids of the formula: ##STR1## as defined herein, possess an antagonistic activity on leukotriene B.sub.4.
    Type: Grant
    Filed: July 13, 1993
    Date of Patent: October 10, 1995
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Mitoshi Konno, Takahiko Nakae, Nobuyuki Hamanaka
  • Patent number: 5446065
    Abstract: Compounds of the formula I ##STR1## in which R.sub.1 signifies an aryl, aralkyl or an aralkenyl group, the aryl radical of which can, in each case, be substituted one or more times by halogen, cyano, alkyl, trifluoromethyl, alkoxy, alkylthio, trifluoromethoxy, hydroxyl or carboxyl, m a whole number from 1 to 3, n a whole number from 1 to 5, R.sub.2 hydrogen, an alkyl, aralkyl or acyl group, Q a bond or an oxygen atom, R.sub.3 hydrogen or a lower alkyl radical which is possibly terminally substituted by carboxyl or by a hydroxyl group and R.sub.4 hydrogen, a lower alkyl group with 1-4 C-atoms, which is possibly terminally substituted by carboxyl or hydroxyl, a possibly substituted phenyl, heteroaryl, cycloalkyl or acyl group or a group ##STR2## in which R.sub.
    Type: Grant
    Filed: June 21, 1993
    Date of Patent: August 29, 1995
    Assignee: Boehringer Mannheim GmbH
    Inventors: Ernst-Christian Witte, Hansjorg Beckh, Karlheinz Stegmeier, Liesel Doerge
  • Patent number: 5428034
    Abstract: Compounds of formula (I): ##STR1## thereof have valuable anthelmintic, acaricidal and insecticidal activities.
    Type: Grant
    Filed: June 9, 1993
    Date of Patent: June 27, 1995
    Assignees: Sankyo Co., Ltd., Ciba-Geigy Corporation
    Inventors: Yasuhiro Morisawa, Akio Saito, Toshimitsu Toyama, Susumu Kaneko
  • Patent number: 5391772
    Abstract: Described is a process for converting an alcohol to an azide with S.sub.N 2 inversion using a phosphoryl azide, e.g. diphenylphosphoryl azide (DPPA). Good yields of azide in high enantiomeric excess can be achieved specifically for benzylic alcohols and alpha-hydroxy alkyl esters. The process is carried at preferably room temperature in an inert dry aprotic solvent, e.g. toluene, and in the presence of a proton acceptor, e.g. 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU) to afford high yields of high enantiomeric purities.
    Type: Grant
    Filed: July 8, 1993
    Date of Patent: February 21, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Andrew S. Thompson, Edward J. J. Grabowski
  • Patent number: 5330981
    Abstract: This application describes 3-arylalkyl esters of 4,5-dihydro-9,10-dioxo-2-anthracenecarboxylic acid and a process for making them. Also described is a method of using the compounds in the treatment of arthritis.
    Type: Grant
    Filed: December 30, 1992
    Date of Patent: July 19, 1994
    Assignee: Istituto Gentili S.p.A.
    Inventors: Sergio Rosini, Maurizio Mian
  • Patent number: 5220027
    Abstract: This invention provides azamethine compounds represented by the formula (I): ##STR1## wherein X represents ##STR2## R.sub.1 to R.sub.4 represent independently a hydrogen atom, an alkyl group, an alkoxyl group, a halogen atom, a nitro group, a cyano group, a hydroxyl group, an amino group, ##STR3## R.sub.5 and R.sub.6 represent independently a hydrogen atom or an alkyl group which may be substituted by a hydroxyl group; R.sub.7 represents a hydrogen atom, an alkyl group, an alkyoxyl group, a hydroxyl group, a halogen atom, a nitro group, a cyano group, ##STR4## wherein -A represents ##STR5## and R and R' represent independently a hydrogen atom or an alkyl group; and R.sub.10 to R.sub.12 represent independently a hydrogen atom or an alkyl group, a process for producing such compounds, and a medium for recording optical information using these compounds.
    Type: Grant
    Filed: April 12, 1991
    Date of Patent: June 15, 1993
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Takeshi Hioki, Kiyoteru Kojima, Jun Tomioka
  • Patent number: 5208333
    Abstract: (2R)-1-(Aryloxy)-3-(butyryloxy)-2-propanols of the general formula (I), ##STR1## where Ar is a monocyclic or polycyclic aromatic or heteroaromatic radical, and a process for their preparation by the reaction of (2R)-glycidyl butyrate with an aromatic hydroxy compound Ar--OH in the presence of a quaternary ammonium halide.
    Type: Grant
    Filed: December 9, 1988
    Date of Patent: May 4, 1993
    Assignee: BASF Aktiengesellschaft
    Inventors: Axel Paul, Wolfgang Ladner, Hardo Siegel