Chalcogen Or Nitrogen Attached Indirectly To The Tricyclo Ring System By Acyclic Nonionic Bonding Patents (Class 548/444)
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Publication number: 20030129513Abstract: 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: ApplicationFiled: September 24, 2001Publication date: July 10, 2003Applicant: Samsung Electronics Co., Ltd.Inventors: Nusrallah Jubran, Hwan Koo Lee, Kam W. Law
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Publication number: 20030119893Abstract: 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: ApplicationFiled: September 26, 2002Publication date: June 26, 2003Inventors: Andre Gerard Bubendorf, Rolf-Dieter Gabel, Michael Hennig, Siegfried Krimmer, Guenter Neugebauer, Walter Preis, Alexander Wirl
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Publication number: 20030113132Abstract: A novel charge transport compound, a novel process using that novel compound and an organophotoreceptor includes:Type: ApplicationFiled: August 9, 2002Publication date: June 19, 2003Applicant: Samsung Information Systems AmericaInventors: Kam W. Law, Nusrallah Jubran, Zbigniew Tokarski, Alan R. Katritzky, Ritu Jain, Rexiat Maimait
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Publication number: 20030113644Abstract: This invention relates to an organophotoreceptor that includes:Type: ApplicationFiled: October 31, 2002Publication date: June 19, 2003Applicant: SAMSUNG Electronics Co., Ltd.Inventors: Kam W. Law, Nusrallah Jubran, Zbigniew Tokarski
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Patent number: 6566529Abstract: 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: GrantFiled: May 19, 2000Date of Patent: May 20, 2003Assignee: The United States of America as represented by the Secretary of the NavyInventors: Oh-Kil Kim, Han Young Woo, Kie-Soo Kim, Kwang-Sup Lee
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Publication number: 20030073846Abstract: 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: ApplicationFiled: August 6, 2002Publication date: April 17, 2003Inventors: Kiyoshi Taniguchi, Hiroshi Kayakiri, Minoru Sakurai, Naokaki Fujii, Kenichi Washizuka, Hitoshi Hamashima, Yasuyo Tomishima, Kaori Hamada, Nobuhiro Yamamoto, Hirofumi Ishikawa, Naoko Unami, Toshiko Miura
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Patent number: 6528657Abstract: 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: GrantFiled: September 28, 2001Date of Patent: March 4, 2003Assignee: Taiho Industries Co., Ltd.Inventors: Tadao Nakaya, Takao Yamauchi, Akio Tajima, Hidemasa Mouri
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Patent number: 6521667Abstract: 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: GrantFiled: August 11, 1998Date of Patent: February 18, 2003Assignees: 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
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Patent number: 6515010Abstract: 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: GrantFiled: May 15, 2002Date of Patent: February 4, 2003Assignee: SmithKline Beecham CorporationInventors: Miriam Franchini, Gopadi M. Venkatesh
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Patent number: 6514968Abstract: 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: GrantFiled: August 31, 2000Date of Patent: February 4, 2003Assignee: Pharmacia & Upjohn CompanyInventor: Ruth Elizabeth TenBrink
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Publication number: 20030023099Abstract: 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: ApplicationFiled: September 28, 2001Publication date: January 30, 2003Inventors: Tadao Nakaya, Takao Yamauchi, Akio Tajima, Hidemasa Mouri
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Patent number: 6512123Abstract: 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: GrantFiled: April 22, 2002Date of Patent: January 28, 2003Assignee: Hoffmann-La Roche Inc.Inventors: Adelbert Grossmann, Wolfgang von der Saal, Tim Sattelkau, Ulrich Tibes
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Patent number: 6495701Abstract: 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: GrantFiled: September 26, 2001Date of Patent: December 17, 2002Assignee: Asahi Kasei Kabushiki KaishaInventors: Koki Matsubara, Hitoshi Kida
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Publication number: 20020188123Abstract: 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: ApplicationFiled: May 2, 2002Publication date: December 12, 2002Applicant: DEGUSSA AGInventors: Axel Monsees, Carsten A. Schneider, Thomas Riermeier, Uwe Dingerdissen
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Publication number: 20020143045Abstract: 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: ApplicationFiled: June 28, 2001Publication date: October 3, 2002Inventors: Jean Hildesheim, Sergey Finogueev, Judith Aronhime, Ben-Zion Dolitzky, Shoshana Ben-Valid, Ilan Kor
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Publication number: 20020115869Abstract: 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: ApplicationFiled: September 5, 2001Publication date: August 22, 2002Inventors: Ging-Ho Hsiue, Wen-Jang Kuo, Ru-Jong Jeng
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Publication number: 20020107405Abstract: The present invention features substituted carbazole compounds of formula (I): 1Type: ApplicationFiled: November 21, 2001Publication date: August 8, 2002Inventors: Jiann T?apos;Suen Lin, K. R. Justin Thomas, Yu-Tai Tao, Chung-Wen Ko
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Patent number: 6413991Abstract: 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: GrantFiled: June 30, 2000Date of Patent: July 2, 2002Assignee: Eli Lilly and CompanyInventors: Thomas A. Crowell, Deborah A. Evrard, Charles D. Jones, Brian S. Muehl, Christopher J. Rito, Anthony J. Shuker, Andrew J. Thorpe, Kenneth J. Thrasher
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Patent number: 6399631Abstract: Carbazoles of the formula which are effective in treating conditions associated with neuropeptide Y-5 neurotransmission.Type: GrantFiled: July 21, 2000Date of Patent: June 4, 2002Assignee: Pfizer Inc.Inventors: Richard L. Elliott, David A. Griffith, Marlys Hammond
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Publication number: 20020065422Abstract: The present invention relates to methods for using a maleimide of formula (I) 1Type: ApplicationFiled: May 21, 2001Publication date: May 30, 2002Inventors: Kazuhiko Kunimoto, Junji Otani, Kunihiko Kodama, Hiroshi Yamamoto, Patrick Verhoustraeten, Sonia Megert, Adalbert Braig
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Patent number: 6340548Abstract: 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: GrantFiled: March 16, 2000Date of Patent: January 22, 2002Assignee: Imation Corp.Inventors: Nusrallah Jubran, Zbigniew Tokarski, Terrance P. Smith
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Patent number: 6258954Abstract: 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: GrantFiled: August 22, 2000Date of Patent: July 10, 2001Assignee: Ciba Specialty Chemicals Corp.Inventors: Kazuhiko Kunimoto, Junji Otani, Kunihiko Kodama, Hiroshi Yamamoto, Patrick Verhoustraeten, Sonia Megert, Adalbert Braig
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Patent number: 6252104Abstract: 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: GrantFiled: December 12, 1996Date of Patent: June 26, 2001Assignee: Kabushiki Kaisha Ueno Seiyaku Oyo KenkyujoInventors: Ryuzo Ueno, Shigeru Ito, Kenji Minami, Masaya Kitayama
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Patent number: 6245775Abstract: 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: GrantFiled: July 3, 1997Date of Patent: June 12, 2001Assignee: Bayer AktiengesellschaftInventors: Ulrich Müller, Richard Connell, Siegfried Goldmann, Rudi Grützmann, Martin Beuck, Hilmar Bischoff, Dirk Denzer, Anke Domdey-Bette, Stefan Wohlfeil
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Patent number: 6235755Abstract: 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: GrantFiled: August 5, 1999Date of Patent: May 22, 2001Assignee: Applied Research Systems ARS Holding N.A.Inventors: Nabil El Tayer, Adulla Reddy, David Buckler, Sharad Magar
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Patent number: 6194439Abstract: 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: GrantFiled: November 23, 1993Date of Patent: February 27, 2001Assignee: Pfizer Inc.Inventor: Robert L. Dow
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Patent number: 6140352Abstract: 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: GrantFiled: May 4, 1998Date of Patent: October 31, 2000Assignee: Eli Lilly and CompanyInventors: Thomas A. Crowell, Deborah A. Evrard, Charles D. Jones, Brian S. Muehl, Christopher J. Rito, Anthony J. Shuker, Andrew J. Thorpe, Kenneth J. Thrasher
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Patent number: 6080338Abstract: 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: GrantFiled: March 5, 1999Date of Patent: June 27, 2000Assignee: Transitions Optical, Inc.Inventor: Anil Kumar
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Patent number: 6057347Abstract: 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: GrantFiled: September 16, 1997Date of Patent: May 2, 2000Assignee: NitroMed, Inc.Inventors: David S. Garvey, L. Gordon Letts, H. Burt Renfroe, Sang William Tam
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Patent number: 6037362Abstract: 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: GrantFiled: August 5, 1998Date of Patent: March 14, 2000Assignee: Asahi Kasei Kogyo Kabushiki KaishaInventors: Shiro Miyoshi, Kohei Ogawa
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Patent number: 6013808Abstract: 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: GrantFiled: April 15, 1999Date of Patent: January 11, 2000Assignee: Pfizer Inc.Inventors: Philip D. Hammen, Peter R. Rose, John L. Tucker, Keith M. Devries, Diane M. Rescek
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Patent number: 6005085Abstract: 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: GrantFiled: November 18, 1998Date of Patent: December 21, 1999Assignee: Kabushiki Kaisha Ueno Seiyaku Oyo KenkyujoInventors: Ryuzo Ueno, Masaya Kitayama, Kenji Minami, Hiroyuki Wakamori, Katsunori Tanikawa
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Patent number: 5879592Abstract: 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: GrantFiled: December 10, 1997Date of Patent: March 9, 1999Assignee: PPG Industries, Inc.Inventor: Anil Kumar
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Patent number: 5877199Abstract: 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: GrantFiled: January 27, 1997Date of Patent: March 2, 1999Assignee: Sankyo Company, LimitedInventors: Nigel Birdsall, Sebastian Lazareno, Syunji Naruto, Masahiko Sugimoto, Kazuo Koyama, Shinji Marumoto
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Patent number: 5824699Abstract: 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: GrantFiled: March 16, 1998Date of Patent: October 20, 1998Assignee: American Home Products CorporationInventors: Anthony F. Kreft, Craig E. Caufield, Amedeo A. Failli, Thomas J. Caggiano, Alexander A. Greenfield, Dennis M. Kubrak
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Patent number: 5760057Abstract: 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: GrantFiled: December 16, 1996Date of Patent: June 2, 1998Assignee: Zeneca LimitedInventors: Andrew George Brewster, Peter William Rodney Caulkett, Alan Wellington Faull, Robert James Pearce, Richard Eden Shute
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Patent number: 5677328Abstract: 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: GrantFiled: October 30, 1996Date of Patent: October 14, 1997Assignee: Bristol-Myers Squibb CompanyInventors: Katherine S. Takaki, Marc A. Bruce, Graham S. Poindexter, Brett T. Watson, Joseph P. Yevich
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Patent number: 5646295Abstract: 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: GrantFiled: January 31, 1996Date of Patent: July 8, 1997Assignee: Boehringer Mannheim GmbHInventors: Rudolf Gompper, Manfred Kubbies, Axel Schmidt, Bernhard Virnekas
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Patent number: 5621000Abstract: Nitric esters with pharmacological activity having general formula (I), their pharmaceutical utilisation and process for their preparation.Type: GrantFiled: May 26, 1995Date of Patent: April 15, 1997Assignee: Nicox S.A.Inventors: Barbara Arena, Piero Del Soldato
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Patent number: 5607955Abstract: A tricyclic compound represented by the following formula (I): ##STR1## exhibits antagonism to angiotensin II receptors.Type: GrantFiled: May 1, 1995Date of Patent: March 4, 1997Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Ohshima, Fumihiko Kanai, Hideyuki Sato, Hiroyuki Obase, Toshiaki Kumazawa, Shiho Takahara, Tetsuji Ohno, Tomoko Ishikawa, Koji Yamada
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Patent number: 5541333Abstract: 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: GrantFiled: April 13, 1995Date of Patent: July 30, 1996Assignee: Abbott LaboratoriesInventor: James R. Fino
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Patent number: 5519134Abstract: 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: GrantFiled: January 11, 1994Date of Patent: May 21, 1996Assignee: Isis Pharmaceuticals, Inc.Inventors: Oscar L. Acevedo, Normand Hebert
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Patent number: 5496834Abstract: 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: GrantFiled: September 2, 1994Date of Patent: March 5, 1996Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Yukio Fujisawa, Satoru Oi, Junji Mizoguchi
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Patent number: 5457122Abstract: The phenylalkan(en)oic acids of the formula: ##STR1## as defined herein, possess an antagonistic activity on leukotriene B.sub.4.Type: GrantFiled: July 13, 1993Date of Patent: October 10, 1995Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Mitoshi Konno, Takahiko Nakae, Nobuyuki Hamanaka
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Patent number: 5446065Abstract: 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: GrantFiled: June 21, 1993Date of Patent: August 29, 1995Assignee: Boehringer Mannheim GmbHInventors: Ernst-Christian Witte, Hansjorg Beckh, Karlheinz Stegmeier, Liesel Doerge
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Patent number: 5428034Abstract: Compounds of formula (I): ##STR1## thereof have valuable anthelmintic, acaricidal and insecticidal activities.Type: GrantFiled: June 9, 1993Date of Patent: June 27, 1995Assignees: Sankyo Co., Ltd., Ciba-Geigy CorporationInventors: Yasuhiro Morisawa, Akio Saito, Toshimitsu Toyama, Susumu Kaneko
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Patent number: 5391772Abstract: 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: GrantFiled: July 8, 1993Date of Patent: February 21, 1995Assignee: Merck & Co., Inc.Inventors: Andrew S. Thompson, Edward J. J. Grabowski
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Patent number: 5330981Abstract: 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: GrantFiled: December 30, 1992Date of Patent: July 19, 1994Assignee: Istituto Gentili S.p.A.Inventors: Sergio Rosini, Maurizio Mian
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Patent number: 5220027Abstract: 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: GrantFiled: April 12, 1991Date of Patent: June 15, 1993Assignee: Sumitomo Chemical Company, LimitedInventors: Takeshi Hioki, Kiyoteru Kojima, Jun Tomioka
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Patent number: 5208333Abstract: (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: GrantFiled: December 9, 1988Date of Patent: May 4, 1993Assignee: BASF AktiengesellschaftInventors: Axel Paul, Wolfgang Ladner, Hardo Siegel