Two Carboxamido Carbonyls Having Benzene Ring Between The Carbonyls And No Carboxamido Nitrogen Between The Carbonyls Patents (Class 564/156)
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Patent number: 7371887Abstract: Amphiphilic oligo(p-phenylene vinylene) compounds and methods of use en route to self-assembled composites and device fabrication.Type: GrantFiled: December 6, 2004Date of Patent: May 13, 2008Assignee: Northwestern UniversityInventors: Samuel I. Stupp, James F. Hulvat, Marina Sofos, Keisuke Tajima
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Patent number: 7342013Abstract: Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: GrantFiled: May 26, 2006Date of Patent: March 11, 2008Assignee: Millennium Pharmaceuticals, Inc.Inventors: Bing-Yan Zhu, Penglie Zhang, Lingyan Wang, Wenrong Huang, Erick A. Goldman, Wenhao Li, Jingmei Zuckett, Yonghong Song, Robert M. Scarborough
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Patent number: 7314874Abstract: Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: GrantFiled: September 15, 2004Date of Patent: January 1, 2008Assignee: Millennium Pharmaceuticals, Inc.Inventors: Bing-Yan Zhu, Penglie Zhang, Wenrong Huang, Robert M. Scarborough, deceased
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Patent number: 7314957Abstract: Compounds are described, having the following general formula (A) R(CONH—CHR10H)m (A) and their use as monomers in polymerization and polycondensation reactions.Type: GrantFiled: April 8, 2003Date of Patent: January 1, 2008Assignee: Eurotecnica Contractors & Engineers S.p.A.Inventor: Franco Codignola
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Patent number: 7285680Abstract: A compound of the general formula (I) (wherein the symbols are as defined in the description), or a prodrug or a salt thereof.Type: GrantFiled: May 28, 2003Date of Patent: October 23, 2007Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Hiromu Habashita, Masahiko Terakado, Shinji Nakade, Takuya Seko
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Patent number: 7271289Abstract: Compounds of formula (I): or pharmaceutically acceptable derivatives thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors.Type: GrantFiled: April 7, 2004Date of Patent: September 18, 2007Assignee: SmithKline Beecham CorporationInventor: Nicola Mary Aston
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Patent number: 7256192Abstract: The present invention relates to an aromatic diamide derivative represented by the general formula (I): [A1 is optionally substituted (C1-C8)alkylene group, (C3-C8)alkenylene group or the like, B is —O— or —N(R4)— (wherein R4 is H, (C1-C6)alkyl, halo(C1-C6)alkyl or the like), R1 is H, (C1-C6)alkyl, optionally substituted phenyl, optionally substituted heterocyclic group, or the like, R2 and R3 are each H, (C3-C6)cycloalkyl or —A2—R8 (A2 is —C(?O)—, —C(?S)— or —C(?NR9)—, R8 and R9 are each H, (C1-C6)alkyl or the like), Q1 to Q5 are each carbon or nitrogen, X and Y are each halogen, cyano, nitro, (C3-C6)cycloalkyl, optionally substituted phenyl, optionally substituted heterocyclic group, or the like, n is 0 to 4, m is 1 to 5, and Z1 and Z2 are each O or S] or a salt thereof, an agricultural and horticultural chemical, and a usage of the chemical.Type: GrantFiled: December 22, 2000Date of Patent: August 14, 2007Assignee: Nihon Nohyaku Co., Ltd.Inventors: Masanori Tohnishi, Eiji Kohno, Hayami Nakao, Tateki Nishida, Takashi Furuya, Toshiaki Shimizu, Akira Seo, Kazuyuki Sakata, Shinsuke Fujioka
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Patent number: 7244755Abstract: Disclosed are compounds of formula I: and the pharmaceutically acceptable salts thereof wherein the variables RN, R1, R2, R3, RP and RC are defined herein. These compounds are useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.Type: GrantFiled: October 4, 2002Date of Patent: July 17, 2007Assignee: Pharmacia & Upjohn CompanyInventors: Jed F. Fisher, Jon S. Jacobs, Brian Sherer
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Patent number: 7238834Abstract: The present invention relates to substantially pure piperidine derivative compounds of the formulae: wherein R1 is hydrogen or hydroxy; R2 is hydrogen; or R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; R3 is —COOH or —COOR4; R4 has 1 to 6 carbon atoms; A, B, and D are the substituents of their respective rings each of which may be different or the same and are hydrogen, halogens, alkyl, hydroxy, alkoxy, or other substituents. A process of preparing such piperidine derivative compounds in substantially pure form is also disclosed.Type: GrantFiled: October 14, 2005Date of Patent: July 3, 2007Assignee: AMR Technology, Inc.Inventor: Thomas E. D'Ambra
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Patent number: 7214715Abstract: The present invention is substituted amines of formula (X) and of the formula (X?) useful in treating Alzheimer's disease and other similar diseases.Type: GrantFiled: June 29, 2001Date of Patent: May 8, 2007Assignees: Pharmacia & Upjohn, Elan PharmaceuticalsInventors: James P. Beck, Lawrence Y. Fang, John N. Freskos, Andrea Gailunas, Roy Hom, Barbara Jagodzinska, Varghese John, Michel Maillard, Shon R. Pulley, Ruth E. TenBrink
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Patent number: 7208629Abstract: Compounds of formula (I): wherein when m is 0 to 4 R1 is selected from C1–6alkyl, C3–7cycloalkyl, C2–6alkenyl, —SO2NR4R5, —CONR4R5 and —COOR4; and when m is 2 to 4 R1 is additionally selected from C1–6alkoxy, hydroxy, NR4R5, —NR4SO2R5, —NR4SOR5, —NR4COR5, and —NR4CONR4R5; R2 is selected from hydrogen, C1–6alkyl and —(CH2)n-C3–7cycloalkyl; R3 is the group —CO—NH—(CH2)p-R6; U is selected from methyl and halogen; W is selected from methyl and chlorine; V and Y are each selected independently from hydrogen, methyl and halogen; m is selected from 0, 1, 2, 3 and 4 wherein each carbon atom of the resulting carbon chain may be optionally substituted with one or two groups selected independently from C1–6alkyl; n is selected from 0, 1, 2 and 3; p and r are independently selected from 0, 1 and 2; s is selected from 0, 1 and 2; or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitorsType: GrantFiled: October 16, 2002Date of Patent: April 24, 2007Assignee: Glaxo Group LimitedInventors: Richard Martyn Angell, Nicola Mary Aston, Paul Bamborough, George Stuart Cockerill, Suzanne Joy Merrick, Kathryn Jane Smith, Ann Louise Walker
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Patent number: 7109376Abstract: Methods for making UV screening compositions by combining benzoxazolyl benzene derivatives of formula (I): wherein R1 is hydrogen, C1-20-alkyl or C2-20-alkenyl; R2 and R3 are independently a group —C(R4,R5)C(R6)?C(R7,R8) (a) or a group —C(R4?,R5?)CH(R6?)CH(R7?,R8?) (b), wherein R4, R5, R6, R7, R8, R4?, R5?, R6?, R7? and R8? are independently, hydrogen, C1-10-alkyl or C2-10-alkenyl, or C2-10-alkyl or C3-10-alkenyl containing at least one oxygen atom interrupting the hydrocarbon chain; or wherein R4, R5, R6, R4?, R5? and R6? are hydrogen, C1-10-alkyl or C2-10-alkyl containing at least one oxygen atom interrupting the hydrocarbon chain, or alkyl substituted by silane or oligosiloxane moiety, and one of R7 and R8 or R7? and R8? is a silane or oligosiloxane moiety and the other one of R7 and R8 or R7? and R8? is hydrogen; and X is phenylene or naphthylene, or substituted phenylene or naphthylene with a cosmetic base.Type: GrantFiled: December 19, 2005Date of Patent: September 19, 2006Assignee: DSM IP Assets B.V.Inventor: Ulrich Huber
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Patent number: 7091247Abstract: A novel biphenyl compound having GPR 14 antagonistic activity. It is a compound represented by the formula (I): wherein R1 represents hydrogen, etc.; X represents 1 to 12 spacers; A represents amino, etc., R2 and R3 each represents a hydrocarbon group, etc.; and rings B and C each represents an optionally further substituted benzene ring, or a salt thereof.Type: GrantFiled: June 28, 2001Date of Patent: August 15, 2006Assignee: Takeda Pharmaceutical Company LimitedInventors: Naoki Tarui, Takashi Santo, Hiroyuki Watanabe, Kazuyoshi Aso, Tetsuo Miwa, Shiro Takekawa
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Patent number: 7091374Abstract: Fluorinated compounds and emulsions including the compounds. The compositions are useful as oxygen carriers and surfactants. In one embodiment, the fluorinated compound is pH sensitive. In one embodiment, the fluorinated compound is a vitamin E derivative. In one embodiment, the fluorinated compound is a vitamin K derivative.Type: GrantFiled: April 23, 2004Date of Patent: August 15, 2006Assignee: Sonus Pharmaceuticals, Inc.Inventors: Yuehua Zhang, Manjari Lal, Andrew Leo, Nagesh Palepu
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Patent number: 6960588Abstract: Compounds of formula (I) in which M, B1, B2, B3, B4, B5, B6, A1, A2, A3, A4, A5, A6, K1 and K2 have the meanings as indicated in the description, are novel effective tryptase inhibitors.Type: GrantFiled: September 12, 2000Date of Patent: November 1, 2005Assignee: Altana Pharma AGInventor: Thomas Martin
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Patent number: 6936597Abstract: Polymeric prodrugs of the formula: wherein B is selected from the group consisting of OH, leaving groups, residues of amine-containing moieties and a residues of hydroxyl-containing moieties; Y1 is selected from the group consisting of O, S, and NR5; M is NR3, O or S; Ar is a moiety which when included in Formula I forms a multi-substituted aromatic or heteroaromatic hydrocarbon or a multi-substituted heterocyclic group; (m) is zero or a positive integer; R1-3 and R5 are independently selected from the group consisting of hydrogen, C1-6 alkyls, C3-12 branched alkyls, C3-8 cycloalkyls, C1-6 substituted alkyls, C3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C1-6 heteroalkyls, substituted C1-6 heteroalkyls, C1-6 alkoxy, phenoxy and C1-6 heteroalkoxy; and R4 is a polymeric residue; as well as methods of making and using the same are disclosed.Type: GrantFiled: March 21, 2002Date of Patent: August 30, 2005Assignee: Enzon, Inc.Inventors: Richard B. Greenwald, Yun H. Choe
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Patent number: 6936735Abstract: Compounds of Formula I: wherein R, R1 and R2 are each independently hydrogen or linear or branched C1 to C10 alkyl, or linear or branched C1 to C10 alkoxy; R3 is selected from the group consisting of COCH3, CO2R7, CONH2, CON(R8)2, CN, COX(CH2)n-N—(R4)(R5)(R6), and the quaternized salt form of the formula COX(CH2)n-N—(R4)(R5)(R6)+Y?; X is O or NH; n is an integer of 1 to 5; Y is an anion; R4, R5 and R6 are independently linear or branched C1 to C30 alkyl; and R7 and R8 are independently hydrogen or linear or branched C1-C30 alkyl. Sunscreen formulations containing compounds of Formula I, and methods for protecting hair, skin and substrates such as polymers, textiles, fabrics, leathers and paints using the compounds herein.Type: GrantFiled: August 27, 2002Date of Patent: August 30, 2005Assignee: EMD Chemicals, Inc.Inventor: Ratan K. Chaudhuri
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Patent number: 6864289Abstract: Aromatic diamide derivative represented by the general formula (I) or a salt thereof and agricultural/herticultural composition containing the same as the active ingredient, wherein A1 represents alkylene, alkenylene or alkynylene; B represents, CO— or —C(?N—OR4)— (wherein R4 represents H, etc.); R1 to R3 represent each H, etc.; Q1 to Q5 represent each N or carbon; Y represents halogeno, etc.; m is from 0 to 5; and Z1 and Z2 represent each O or S.Type: GrantFiled: September 22, 2000Date of Patent: March 8, 2005Assignee: Nihon Nohyaku Co., Ltd.Inventors: Masanori Tohnishi, Hayami Nakao, Eiji Kohno, Tateki Nishida, Takashi Furuya, Toshiaki Shimizu, Akira Seo, Kazuyuki Sakata, Shinsuke Fujioka, Hideo Kanno
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Patent number: 6849742Abstract: The present invention provides a binaphthol compound represented by formula [1]: and a salt thereof. The binaphthol compound of the present invention is useful for manufacturing antiseptic compounds or chiral catalysts. According to the method of the present invention, binaphthol compounds can be prepared in high yield with low cost.Type: GrantFiled: April 18, 2002Date of Patent: February 1, 2005Assignee: Kabushiki Kaisha Ueno Seiyaku Oyo KenkyujoInventors: Ryuzo Ueno, Masaya Kitayama, Kenji Minami, Hiroyuki Wakamori
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Publication number: 20040235754Abstract: Compounds of the formula 1Type: ApplicationFiled: July 2, 2004Publication date: November 25, 2004Inventor: Cynthia Anne Fink
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Publication number: 20040162317Abstract: Mono-acylated o-phenylendiamines derivatives of formula A 1Type: ApplicationFiled: February 3, 2004Publication date: August 19, 2004Inventors: Georg Fertig, Frank Herting, Manfred Kubbies, Anja Limberg, Ulrike Reiff, Michael Weidner
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Publication number: 20040152598Abstract: The present invention provides a substituted anilide derivative of formula (I): 1Type: ApplicationFiled: November 17, 2003Publication date: August 5, 2004Inventors: Makoto Goto, Minoru Yamaguchi, Hiroto Harayama, Hayami Nakao, Takashi Furuya, Masanori Tohnishi, Masayuki Morimoto, Shinsuke Fujioka
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Publication number: 20040138503Abstract: The present invention relates to the surface modification of various carbonaceous materials, compounds and compositions. More specifically, the invention provides methods for introducing amide functionality on to the surface of carbonaceous materials, compounds and compositions, and similarly provides several surface modified carbonaceous materials resulting therefrom.Type: ApplicationFiled: January 13, 2003Publication date: July 15, 2004Inventors: Bollepalli Srinivas, Jorge Ayala, Anderson O. Dotson
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Publication number: 20040116299Abstract: The present invention relates to a phthalamide derivative represented by general formula (I): 1Type: ApplicationFiled: October 23, 2003Publication date: June 17, 2004Inventors: Hiroto Harayama, Masanori Tohnishi, Masayuki Morimoto, Shinsuke Fujioka, Rudiger Fischer, Jorg Konze
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Publication number: 20040097595Abstract: The present invention relates to a phthalamide derivative represented by general formula (I): 1Type: ApplicationFiled: October 23, 2003Publication date: May 20, 2004Inventors: Hayami Nakao, Hiroto Harayama, Minoru Yamaguchi, Masanori Tohnishi, Masayuki Morimoto, Shinsuke Fujioka
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Patent number: 6737420Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formula (XII): useful in treating Alzheimer's disease and other similar diseases.Type: GrantFiled: March 23, 2001Date of Patent: May 18, 2004Assignee: Elan Pharmaceuticals, Inc.Inventors: Roy Hom, Shumeye S. Mamo, Jay Tung, Andrea Gailunas, Varghese John, Lawrence Y. Fang
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Publication number: 20040082811Abstract: The invention relates to a process for the preparation of a compound of formula (I), wherein R represents a 2,3-dihydroxy-1-propyl or a 1,3-dihydroxy-2-propyl radical, via direct amidation of a dialkyl ester of 5-amino-1,3-benzenedicarboxylic acid of formula (V), wherein R1 represents a straight or branched (C1-C4)-alkyl group, with at least the stoichiometric amount of an amine of formula H2NR.Type: ApplicationFiled: December 22, 2003Publication date: April 29, 2004Inventors: Pier Lucio Anelli, Marino Brocchetta, Giovanna Lux, Enrico Cappelletti
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Publication number: 20040082812Abstract: A process for the preparation of (S)-N,N′-bis[2-hydroxy-1-(hydroxymethyl)ethyl]-5-[(2-hydroxy-1-oxo-propyl)amino]-2,4,6-triiodo-1,3-benzendicarboxamide (iopamidol) starling from 5-amino-N,N′-bis[2-hydroxy-1-(hydroxymethyl)ethyl]-2,4,6-triiodo-1,3-benzenedicarboxamide (II) which process comprises a) reacting the compound of formula (II) with a suitable protecting agent, to give a compound of formula (III) wherein R is a group of formula A or B wherein R1 is a hydrogen atom, a C1÷C4 straight or branched alkoxy group, R2 is hydrogen, a C1÷C4 straight or branched alkoxy group and R3 ?is a C1÷C4 straight or branched alkyl group, a trifuoromethyl or a trichloromethyl group; b) acylating the amino group in position 5 of the intermediate compound of formula (III), by reaction with a (S)-2-(acetyloxy)propanoyl chloride to give a compound of formula (IV) wherein R is as defined above; and c) removing all the acyl groups present in the compound of formType: ApplicationFiled: December 22, 2003Publication date: April 29, 2004Inventors: Pier Lucio Anelli, Marino Brocchetta, Giovanna Lux, Enrico Cappelletti
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Publication number: 20040053976Abstract: The present invention is directed to polymeric-prodrug transport forms of the formula: 1Type: ApplicationFiled: August 8, 2003Publication date: March 18, 2004Inventors: Anthony J. Martinez, Annapurna Pendri, Richard B. Greenwald, Yun H. Choe
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Publication number: 20040053786Abstract: Compounds of Formula I and Formula II, and their N-oxides and agriculturally suitable salts, are disclosed that are useful for controlling invertebrate pests, Formula (I), Formula (II) wherein A, B, J, R1, R2, R3, R4, and n are as defined in the disclosure. Also disclosed are compositions comprising the compounds of Formula I or Formula II and methods for controlling invertebrate pests that involve contacting the invertebrate pests or their environment with an effective amount of a compound of Formula (I) or Formula (II).Type: ApplicationFiled: April 4, 2003Publication date: March 18, 2004Inventors: Thomas Paul Selby, King-Mo Sun
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Patent number: 6706763Abstract: O-anisamide compounds and their addition salts effective for the prevention and/or therapy of metabolic diseases such as hyperlipidemia and diabetes, in which peroxisome proliferator-activated receptor (PPAR) being intranuclear receptor, in particular, human PPAR participates, as agonistic drugs thereon, and processes for preparing them, wherein the o-anisamide compounds are represented by a general formula (1) [wherein R denotes a carboxyl group, carboxymethyl group or CH2CHXCOY (here X denotes a mercapto group or S(O)nMe (n=0, 1 or 2) and Y denotes an amino group or hydroxyl group)], their medicinally acceptable salts, and their hydrates.Type: GrantFiled: March 18, 2002Date of Patent: March 16, 2004Assignee: Kyorin Pharmaceutical Co., Ltd.Inventors: Hiroya Satoh, Masakatsu Komuro, Koji Murakami, Katsuya Awano
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Patent number: 6703379Abstract: The present invention provides an AP-1 activation inhibitor, NF-kappa B activation inhibitor, inflammatory cytokine production inhibitor, matrix metalloprotease production inhibitor, inflammatory cell adhesion molecule expression inhibitor, anti-inflammatory agent, antirheumatic agent, immunosuppressant, cancer metastasis inhibitor, remedy for arteriosclerosis and antiviral agent which contain the benzene derivative of the following general formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient.Type: GrantFiled: March 12, 2001Date of Patent: March 9, 2004Assignee: Ajinomoto Co., Inc.Inventors: Yukio Iino, Kohichi Fujita, Takashi Tsuji, Ariko Kodaira, Kenji Takehana, Tsuyoshi Kobayashi, Takashi Yamamoto
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Patent number: 6656971Abstract: The present invention relates to novel, non-peptidic small organic compounds having an affinity for cyclophilin (CyP)-type immunophilin proteins, and to pharmaceutical compositions comprising one or more of the said compounds. The invention further relates to the uses of these compounds and compositions for binding CyP-type proteins, inhibiting their peptidyl-prolyl isomerase activity, and for research, development, and therapeutic applications in a variety of medical disorders.Type: GrantFiled: January 25, 2002Date of Patent: December 2, 2003Assignee: Guilford Pharmaceuticals Inc.Inventors: Yong-Qian Wu, Sergei Belyakov, Gregory S. Hamilton, David Limburg, Joseph P. Steiner, Mark Vaal, Ling Wei, Douglas Wilkinson
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Publication number: 20030212113Abstract: The present invention provides novel compounds possessing one or more of the following activities: antibacterial, antifungal and antitumor activity.Type: ApplicationFiled: December 24, 2002Publication date: November 13, 2003Inventors: Natalia B. Dyatkina, Dong-Fang Shi, Christopher Don Roberts, Mark Douglas Velligan, Sebastian Johannes Reinhard Liehr, Janos Botyanszki, Wentao Zhang, Alexander Khorlin, Peter Harold Nelson, Joseph Martin Muchowski
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Patent number: 6646151Abstract: The invention relates to a process for the preparation of compounds of the formula or, if appropriate, a tautomer thereof, in each case in the free form or in salt form, in which A, X, Y, Z, R2, R3, R4, R5, R7, R9 and n are as defined in claim 1 and the C═N double bond marked with E has the E configuration, which comprises a1) reacting either a compound of the formula (II) mentioned above with a compound of the formula (III) mentioned above, in which X1 is a leaving group, or a2) a compound of the formula (IV) mentioned above, if appropriate in the presence of a base, with a compound of the formula (V) mentioned above, or b1) reacting a compound of the formula (VI) mentioned above with a compound of the formula R7—A—X2 (VII), in which X2 is a leaving group, and either further reacting the compound thus obtainable, of the formula (IV), for example according to method a2), or b2) reacting it with hydroxylamine or a salt thereof, if appropriate in the presence of a basic orType: GrantFiled: September 26, 2000Date of Patent: November 11, 2003Assignee: Bayer AktiengesellschaftInventors: Saleem Farooq, Stephan Trah, Hugo Ziegler, René Zurflüh
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Publication number: 20030203966Abstract: The invention concerns novel compounds of general formula (1), their tautomeric forms, and their additive salts with pharmaceutically acceptable bases. The invention also concerns methods for preparing these compounds and their applications as medicines. These compounds inhibit the aldose reductase enzyme and can be used in the treatment or prevention of peripheral and autonomous neurological diabetic complications, renal and ocular disorders such as cataract and retinopathy.Type: ApplicationFiled: November 12, 2002Publication date: October 30, 2003Inventors: Francois Collonges, Herve Dumas, Claude Lardy, Philippe Durbin
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Patent number: 6586600Abstract: Novel sulfur-containing ligands for binding of heavy metals are disclosed. The ligands incorporate a central ring structure and pendant alkyl-thiol chains. The ligands are of the general structure: where n is an integer from 1-4, and X is selected from the group consisting of hydrogen, lithium, sodium, potassium, rubidium, cesium, and francium. The ligands of the present invention are suitable for binding any metal in or capable of being placed in a positive oxidation state, such as cadmium, lead, nickel, zinc, mercury, copper, and the like. Additionally, methods for removal of heavy metals from various substances are disclosed, comprising separating selected heavy metals from selected substances by contacting the substances with an effective amount of the novel sulfur-containing chelate ligands for a sufficient time to form stable, irreversible ligand-metal precipitates, and removing such precipitates.Type: GrantFiled: December 6, 2000Date of Patent: July 1, 2003Assignee: University of Kentucky Research FoundationInventors: David A. Atwood, Brock S. Howerton, Matthew Matlock
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Patent number: 6569896Abstract: This invention provides a novel class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds which are tissue-selective androgen receptor modulators (SARM), which are useful for oral testosterone replacement therapy, male contraception, maintaining sexual desire in women, treating prostate cancer and imaging prostate cancer. These agents have an unexpected in-vivo activity for an androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. These agents may be active alone or in combination with progestins or estrogens. The invention further provides a novel class of non-steroidal agonist compounds. The invention further provides compositions containing the selective androgen modulator compounds or the non-steroidal agonist compounds and methods of binding an androgen receptor, modulating spermatogenesis, treating and imaging prostate cancer, and providing hormonal therapy for androgen-dependent conditions.Type: GrantFiled: August 23, 2001Date of Patent: May 27, 2003Assignee: The University of Tennessee Research CorporationInventors: James T. Dalton, Duane D. Miller, Donghua Yin, Yali He
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Publication number: 20030055287Abstract: The present invention provides a phthalic acid diamide derivative represented by the general formula (I) 1Type: ApplicationFiled: January 4, 2002Publication date: March 20, 2003Inventors: Masanori Tohnishi, Hayami Nakao, Eiji Kohno, Tateki Nishida, Takashi Furuya, Toshiaki Shimizu, Akira Seo, Kazuyuki Sakata, Shinsuke Fujioka, Hideo Kanno
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Publication number: 20020193409Abstract: Polymeric prodrugs of the formula: 1Type: ApplicationFiled: March 21, 2002Publication date: December 19, 2002Inventors: Richard B. Greenwald, Yun H. Choe
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Patent number: 6495693Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: March 30, 1999Date of Patent: December 17, 2002Assignees: Athena Neurosciences, Inc., Eli Lilly & CompanyInventors: James E. Audia, Beverly K. Folmer, Varghese John, Lee H. Latimer, Jeffrey S. Nissen, Warren J. Porter, Eugene D. Thorsett, Jing Wu
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Patent number: 6489364Abstract: Compounds of formula (I), wherein A′ and A″ are independently the same or different group of formula (II) wherein: R′ is H, CH3, C(CH3)2, —ORa, —N(Ra)2, —N(Ra)ORa or —DP; R′″ is H or CH3; Ra is H, C1-C3 alkyl; D is a bond, alkylene, —C(═O)—, —S(O)— or S(O)2—; P is an optionally substituted, mono or bicyclic carbo- or hetereocycle; R″ is H, any of the sidechains found in the natural amino acids, carboxacetamide, or a group (CH2)nDP; M is a bond or —C(═O)N(R′″)—; Q is absent, a bond, —CH(OH)— or CH2—; or R″ together with Q, M and R′ define an optionally substituted 5 or 6 membered carbo- or heterocyclic ring which is optionally fused with a further 5 or 6 membered carbo- or heterocyclic ring; with the proviso that R′ is —ORa, —, N(Ra)2, —N(Ra)ORa or -DP, if M is a bond and Q is absent; X is H, OH, OCH3, Y is H, OH, OCH3, but X and Y areType: GrantFiled: June 21, 2001Date of Patent: December 3, 2002Assignee: Medivir ABInventors: Bjorn Classon, Ingemar Sven-Anders Kvarnstrom, Bengt Bertil Samuelsson
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Patent number: 6482827Abstract: A compound, which is an amine derivative of formula (I) wherein W is —CNHOH or —COOH: R1 and R2 are each hydrogen or an organic residue, R3 is an organic group, Q is a secondary or tertiary acyclic or cyclic amido group, and the pharmaceutically acceptable salts, solvates and hydrates thereof, are inhibitors of matrix metalloproteinases (MMPs) and of the release of tumor necrosis factor-alpha (TNF) from cells. They are therefore useful in the prevention, control and treatment of diseases in which MMPs or TNF are involved, especially tumoral and inflammatory diseases. Processes for their preparation and pharmaceutical compositions containing them are also described.Type: GrantFiled: March 10, 1999Date of Patent: November 19, 2002Assignee: Pharmacia & Upjohn S.p.A.Inventors: Marco Alpegiani, Pierluigi Bissolino, Francesca Abrate, Ettore Perrone, Riccardo Corigli, Daniela Jabes
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Publication number: 20020120137Abstract: The present invention provides compounds, pharmaceutical compositions and methods that are useful in modulating the farnesoid X receptor (FXR). As FXR is involved in negatively controlling the expression level of cholesterol 7&agr;-hydroxylase (cyp7a), the rate-limiting enzyme involved in the oxidative metabolism of cholesterol into bile acids, the compounds described herein find utility in treating diseases associated with abnormally high or low cholesterol levels. In certain aspects, the FXR modulators (e.g., antagonists) described herein block the negative feed-back downregulation of cyp7a expression produced by certain cholic acids, the endogenous ligands for FXR. Moreover, as FXR forms heterodimers with the retinoid X receptor (RXR) in some cell types, modulation of the level of FXR activity in cells has a wide range of effects on a variety of biological processes which are mediated by RXR or other RXR-interacting proteins such as PPAR&ggr; and PPAR&agr;.Type: ApplicationFiled: August 31, 2001Publication date: August 29, 2002Applicant: Tularik Inc.Inventors: Jonathan Houze, Sharon McKendry, Joshua P. Gergely, Yi Xia, Bei Shan, Frank Kayser
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Publication number: 20020095053Abstract: A process for preparing 5-amino-N,N′-bis(R)isophthalamides, where A is 2,3-dihydroxypropyl or 1,3-dihydroxyisopropyl, useful as intermediates in preparing iodinated diagnostic agents, which comprises reacting a di-lower-alkyl 5-nitroisophthalate with a compound of the formula RNH2 in the presence of a basic catalyst and without isolating the intermediate 5-nitro-N,N′-bis(R)isophthalamide, catalytically hydrogenating the latter.Type: ApplicationFiled: May 14, 2001Publication date: July 18, 2002Inventors: Edward David Parady, Karl Olaf Gelotte
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Patent number: 6399776Abstract: This invention relates to novel processes for preparing the pharmaceutically active compound 5-(3-[(2S)-exo-bicyclo[2.2.1]hept-2-yloxy]-4-methoxyphenyl)-3,4,5,6-tetrahydropyrimidin-2(1H)-one and its corresponding 2R enantiomer and for preparing certain intermediates used in the synthesis of these compounds. It also relates to novel intermediates used in the synthesis of such pharmaceutically active compounds and to other novel compounds that are related to such intermediates.Type: GrantFiled: June 11, 2001Date of Patent: June 4, 2002Assignee: Pfizer INCInventors: Thomas G. LaCour, Charles William Murtiashaw, III
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Patent number: 6362369Abstract: The present invention provides a phthalic acid diamide derivative represented by the general formula (I) (wherein R1, R2 and R3 are each H, C3-C6 cycloalkyl group, group of the formula —A1—Ql or the like; X may be the same or different and are each halogen atom, nitro group, phenyl group, group of the formula —A2—R7 or the like; n is 1 to 4; Y may be same or different and are each halogen atom, cyano group, phenyl group, group of the formula —A2—R7 or the like; m is 1 to 5; Z1 and Z2 are each 0 or S), fluorine-containing aniline compound represented by the general formula (ST-I) as starting material for said phthalic acid diamide derivative (wherein Ra is halogen atom, C1-C6 alkyl group or the like and Rb, Rc and Rd is H or C2-C6 perfluoroalkyl group), and an agricultural and horticultural insecticide containing said phthaldiamide derivative, as well as to provide a method for use of said insecticide.Type: GrantFiled: February 16, 1999Date of Patent: March 26, 2002Assignee: Nihon Nohyaku Co., Ltd.Inventors: Masanori Tohnishi, Hayami Nakao, Eiji Kohno, Tateki Nishida, Takashi Furuya, Toshiaki Shimizu, Akira Seo, Kazuyuki Sakata, Shinsuke Fujioka, Hideo Kanno
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Publication number: 20020028970Abstract: A new composition of matter for a diamidodiol and a method for preparing the diamidodiol. The exemplary diamidodiol has the formula C15H30N2O4 and is prepared by reacting a first quantity of 2-amino-2-methyl-1-propanol with a second quantity of a di-substituted malonyl dichloride (i.e., diethylmalonyl dichloride), preferably in ethyl acetate as solvent. A tetraamido macrocycle is prepared from the diamidodiol in two steps by oxidizing the diamidodiol to form a diacid followed by coupling using a known procedure of the diacid with an aryl diamine (e.g., 1 ,2-diaminobenzene)to yield the tetraamido macrocycle.Type: ApplicationFiled: August 30, 2001Publication date: March 7, 2002Applicant: THE CLOROX COMPANYInventors: James E. Deline, Michael M. Ott
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Publication number: 20010041814Abstract: The present invention provides a phthalic acid diamide derivative represented by the general formula (I) 1Type: ApplicationFiled: February 16, 1999Publication date: November 15, 2001Inventors: MASANORI TOHNISHI, HAYAMI NAKAO, EIJI KOHNO, TATEKI NISHIDA, TAKASHI FURUYA, TOSHIAKI SHIMIZU, AKIRA SEO, KAZUYUKI SAKATA, SHINSUKE FUJIOKA, HIDEO KANNO
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Patent number: RE38856Abstract: The invention provides a process by which ultra low salt content triiodinated aromatic compounds may be isolated from a highly acidic hot triiodination raction reaction medium in a straightforward fashion. The process involves increasing the pH to above 5 a value in the range of 3 to 7 with sodium hydroxide, addition of sodium bisulphite and/or sodium dithionite, addition of seed crystals, cooling slowly, and washing the collected precipitate with water.Type: GrantFiled: October 24, 2002Date of Patent: October 25, 2005Assignee: Amersham Health ASInventors: William Thielking, Einar Odd Ingvoldstad, Trygve Gulbrandsen