Polycyclo Ring System Patents (Class 568/326)
  • Patent number: 6166251
    Abstract: Disclosed are labeling reagents containing fluorescent compounds represented by the general formula ##STR1## where R is a group capable of combining with proteins, Ar is a conjugated double bond system, and n is a whole number. These labeling reagents have high fluorescence emission intensities, give high synthesis yields, permit both solid-phase measurements and liquid-phase measurements in immunoassays, and require less measuring steps.
    Type: Grant
    Filed: December 31, 1998
    Date of Patent: December 26, 2000
    Assignees: Kazuko Matsumoto, Suzuki Motor Corporation
    Inventors: Kazuko Matsumoto, Jingli Yuan
  • Patent number: 6139770
    Abstract: An oxygen scavenging composition or system is provided comprising an oxygen scavenging material, a photoinitiator, and at least one catalyst effective in catalyzing an oxygen scavenging reaction, wherein the photoinitiator comprises a benzophenone derivative containing at least two benzophenone moieties. A film, a multi-phase composition, a multi-layer composition, a multi-layer film, an article comprising the oxygen scavenging composition, a method for preparing the oxygen scavenging composition, and a method for scavenging oxygen are also provided. Non-extractable benzophenone derivative photoinitiators and methods for preparing same are also provided.
    Type: Grant
    Filed: May 16, 1997
    Date of Patent: October 31, 2000
    Assignees: Chevron Chemical Company LLC, Cryovac, Inc.
    Inventors: Kiyoshi Katsumoto, Ta Yen Ching, Joseph L. Goodrich, Drew Ve Speer
  • Patent number: 6114493
    Abstract: This invention relates to methods for preparing novel, solid-phase transfer reagents, specifically phosgenated oxime resins and non-symmetrical ureas, that are useful as supports in combinatorial synthesis for the creation of libraries of compounds for lead identification.
    Type: Grant
    Filed: December 22, 1998
    Date of Patent: September 5, 2000
    Assignee: E. I. du Pont de Nemours and Company
    Inventor: Mark Andrew Scialdone
  • Patent number: 6111118
    Abstract: A procedure for oxidizing organic compounds having allylic hydrogen atom(s) involving the steps of reactively contacting the organic compound with a combination of a periodic acid or metal periodate and an alkyl hydroperoxide under conditions of normal as well as elevated pressure of a suitable gas like air. The reaction can conveniently be conducted at temperatures between about 0-65.degree. C. in a cosolvent system of water and organic solvent(s).
    Type: Grant
    Filed: January 11, 1999
    Date of Patent: August 29, 2000
    Assignee: Humanetics Corporation
    Inventors: Padma Marwah, Henry A. Lardy
  • Patent number: 6080739
    Abstract: The present invention relates to colchicine and thiocolchicine derivatives which can be obtained from these molecules by functionalization of the C-7 to ketone or functionalization of the amino group. Said compounds have a marked antiblastic activity both on the normal cancer cells and on the chemoresistant phenotype. The compounds of the invention can be administered both by injection and orally.
    Type: Grant
    Filed: November 24, 1998
    Date of Patent: June 27, 2000
    Assignee: Indena S.p.A.
    Inventor: Ezio Bombardelli
  • Patent number: 6048877
    Abstract: Tetralone derivatives of the formula ##STR1## where R.sup.1 is halo, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, (aryl)alkenyl, (aryl)alkynyl, alkoxy, O-alkenyl, O-aryl, O-alkyl(heterocyclo), COO-alkyl,alkanoyl, CO-amino, CO-substituted amino, alkyl-CO-amino, alkyl-CO-substituted amino, NHCO-alkyl, NHCO-aryl, NHCO-alkyl(heterocyclo), N(alkyl)CO-alkyl, N(alkyl)CO-aryl, N(alkyl)CO-heterocyclo, N(alkyl)CO-alkyl(heterocyclo);R.sup.2 is hydrogen, alkyl, halo, aryl, alkoxy, amino, substituted amino;R.sup.3 is oxo, hydroxy, alkoxy, O--COalkyl, --O--COaryl, --O--COheterocyclo, NOH, NO-alkyl, N-amino, N-substituted amino, N-NHCONHalkyl, N-NHSO.sub.2 alkyl, N-NHSO.sub.2 aryl, amino, substituted amino, NHCO-alkyl, NHCO-aryl, NHCO-heterocyclo, spiroheterocyclo;R.sup.4 is hydrogen, alkyl, alkyl(COalkyl), alkyl(COOalkyl); orR.sup.3 and R.sup.4 taken together with the atoms to which they are attached form a five- to seven-membered ring which can contain up to three heteroatoms selected from oxygen, nitrogen and sulfur;R.sup.
    Type: Grant
    Filed: January 20, 1998
    Date of Patent: April 11, 2000
    Assignee: Bristol-Myers Squibb Company
    Inventors: Saleem Ahmad, Philip D. Stein, Francis N. Ferrara, Karnail S. Atwal
  • Patent number: 6037361
    Abstract: Fluorinated butyric acid compounds and derivatives are described as well as acid methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A (72 kD gelatinase) and stromelysin-1, and also collagenase, matrilysin, and MMP-13, and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, treatment of burns, decubital ulcers, wound healing, cancer, inflammation, pain, arthritis, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.
    Type: Grant
    Filed: March 9, 1998
    Date of Patent: March 14, 2000
    Assignee: Warner-Lambert Company
    Inventors: Bruce David Roth, Patrick Michael O'Brien, Drago Robert Sliskovic
  • Patent number: 6017470
    Abstract: This invention provides a compound having the structure: ##STR1## wherein rings A and B represent independent electron accepting ring systems and wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are the same or different and are H, substituted or unsubstituted, saturated or unsaturated alkyl, alkenyl, cycloalkyl, aryl, or arylalkyl, --SR, --NRR', --OR, --OC(O)R, SC(O)R, --SCR, wherein R and R' are independently substituted or unsubstituted, saturated or unsaturated alkyl, alkenyl, cycloalkyl, aryl, or arylalkyl.This invention also provides thin films comprising a compound having the above structure or suitable derivatives thereof.This invention further provides liquid crystal display devices and non-linear optical devises comprising a compound having the above structure or a suitable derivative thereof.
    Type: Grant
    Filed: April 12, 1996
    Date of Patent: January 25, 2000
    Assignee: The Trustees of Columbia University in the City of New York
    Inventors: Thomas J. Katz, Colin P. Nuckolls
  • Patent number: 5993700
    Abstract: This invention provides an aggregate of a compound capable of forming helical structures such that the aggregate is capable of achieving a specific rotation of at least 100,000.degree. for plane polarized light having a wavelength of 589 nm.
    Type: Grant
    Filed: July 18, 1997
    Date of Patent: November 30, 1999
    Assignee: The Trustees of Columbia University in the City of New York
    Inventors: Thomas J. Katz, Colin P. Nuckolls
  • Patent number: 5968482
    Abstract: The invention relates to the use of .alpha.-hydroxyketoalkyl derivatives as light protection filters for cosmetic or pharmaceutical products, the .alpha.-hydroxyketoalkyl group being linked, if appropriate via a spacer, to a chromophoric group which has an absorption maximum in a wavelength range of between 280 and 400 nm and has a conjugated .pi.-electron system of at least 8 .pi.-electrons, and to new .alpha.-hydroxyalkyl derivatives, processes for their preparation and pharmaceutical and cosmetic formulations comprising these derivatives as light protection substances.
    Type: Grant
    Filed: September 20, 1996
    Date of Patent: October 19, 1999
    Assignee: Merck Patent Gesellschaft MIT Beschrankter Haftung
    Inventors: Roland Martin, Ingeborg Stein, Ulrich Heywang, Michael Schwarz, Thekla Kurz
  • Patent number: 5942641
    Abstract: The present invention provides a novel fluorenone derivatives represented by the formula: ##STR1## wherein R.sup.a -R.sup.g are defined in the specification, and a method for repairing and protecting central or peripheral nerve degeneration comprising use of a fluorenone derivative represented by the formula: ##STR2## wherein R.sup.1, R.sup.2 p and q are as defined in the specification as an active component.
    Type: Grant
    Filed: February 7, 1995
    Date of Patent: August 24, 1999
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Tatsuyoshi Tanaka, Yohji Sakurai, Nobutaka Fujisawa, Osamu Hongoh, Takao Nishi
  • Patent number: 5869709
    Abstract: A procedure for oxidizing organic compounds having allylic hydrogen atom(s) involving the steps of reactively contacting the organic compound with a combination of an alkali metal periodate and an alkyl hydroperoxide. The reaction can conveniently be conducted under ambient temperature and pressure conditions, and is conveniently conducted in a cosolvent system of water and organic solvent(s).
    Type: Grant
    Filed: May 7, 1997
    Date of Patent: February 9, 1999
    Assignee: Humanetics Corporation
    Inventors: Padma Marwah, Henry A. Lardy
  • Patent number: 5859297
    Abstract: Disclosed are labeling reagents containing fluorescent compounds represented by the general formula ##STR1## where R is a group capable of combining with proteins, Ar is a conjugated double bond system, and n is a whole number. These labeling reagents have high fluorescence emission intensities, give high synthesis yields, permit both solid-phase measurements and liquid-phase measurements in immunoassays, and require less measuring steps.
    Type: Grant
    Filed: October 23, 1996
    Date of Patent: January 12, 1999
    Assignees: Kazuko Matsumoto, Suzuki Motor Corporation
    Inventors: Kazuko Matsumoto, Jingli Yuan
  • Patent number: 5852160
    Abstract: This invention relates to methods for preparing novel, solid-phase transfer reagents, specifically phosgenated oxime resins and non-symmetrical ureas, that are useful as supports in combinatorial synthesis for the creation of libraries of compounds for lead identification.
    Type: Grant
    Filed: August 19, 1997
    Date of Patent: December 22, 1998
    Assignee: E. I. du Pont de Nemours and Company
    Inventor: Mark Andrew Scialdone
  • Patent number: 5849956
    Abstract: The present invention relates to phytocassanes which are novel diterpene compounds exhibiting an antifungal activity against rice blast fungus, Pyricularia oryzae (Magnaporthe grisea) and rice sheath blight fungus, Rhizoctonia solani, and more specifically, it relates to phytocassanes A, B, C, D, and EL and a process for producing phytocassanes or momilactones, antifungal diterpene compounds, at a high yield.
    Type: Grant
    Filed: August 8, 1997
    Date of Patent: December 15, 1998
    Assignee: Plant Biological Defense System Laboratories
    Inventors: Jinichiro Koga, Toyozo Yamauchi, Masaru Shimura, Yoko Ogasawara, Nagakatsu Ogasawara, Jyunko Suzuki
  • Patent number: 5840661
    Abstract: The present invention relates to novel 2-aryl-3-hydroxy-cyclopent-2-en-1-one derivatives of the formula (I) ##STR1## in which X represents halogen, nitro, cyano, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl or halogenoalkoxy,Y represents hydrogen, halogen, nitro, cyano, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl or halogenoalkoxy,Z represents halogen, nitro, cyano, alkyl, alkoxy or halogenoalkoxy andA, B, D.sup.1, D.sup.2, G and n have the meaning given in the description,several processes for their preparation and their use as compositions for controlling pests and as herbicides.
    Type: Grant
    Filed: December 31, 1996
    Date of Patent: November 24, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Reiner Fischer, Jacques Dumas, Thomas Bretschneider, Christoph Erdelen, Ulrike Wachendorff-Neumann, Hans-Joachim Santel, Markus Dollinger, Andreas Turberg, Norbert Mencke
  • Patent number: 5834521
    Abstract: Tetracyclic compounds having the following structure are described: ##STR1## wherein R.sub.1 -R.sub.10 are as defined. The tetracyclic compounds are capable of potent effects on steroid sensitive tissues and have demonstrated increased uterine weight, antiovulatory effects and potent steroid receptor binding. The compounds have therapeutic utility in reproductive applications such as fertility control, labor induction, ovulation induction and spermatogenesis. Methods for preparing the tetracyclic compounds from substituted indanones are also described.
    Type: Grant
    Filed: August 5, 1996
    Date of Patent: November 10, 1998
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: John H. Dodd, Lisa A. Dixon, James L. Bullington, Charles F. Schwender
  • Patent number: 5770763
    Abstract: Novel difunctionalized cyclobutabenzene monomers of the general formula: ##STR1## wherein Z can be hydrogens or a cyclobutane ring; and X and Y are carboxyl, amino, alcohol, isocyanate, acid halide, or bis-acyl halide groups. Exemplary difunctional bitricyclodecatriene monomers are ?2,2'-bidicyclo?2.4.0!octa-1,3,5-triene!-5,5'-dicarboxylic acid (BXTA) and ?2,2'-bitricyclo?6.2.0.0!deca-1,3,(6),7-triene!-7,7'-dicarboxylic acid (QXTA). The difunctionalized bitricyclodecatriene monomers can form part of a polymer backbone chain in which the multiple butane ring functionalities can be easily opened to produce strong, three-dimensional covalent bond crosslinking between polymer chains. The crosslinking can be induced simply by heating the polymer to a temperature in excess of 250.degree. C.
    Type: Grant
    Filed: August 30, 1996
    Date of Patent: June 23, 1998
    Assignee: The Board of Regents of the Univ. of Michigan
    Inventors: David C. Martin, Jeffrey S. Moore, Larry J. Markoski, Kenneth A. Walker, Gary E. Spilman
  • Patent number: 5760092
    Abstract: Disclosed are allocolchinones, which are anti-mitotic agents. Allocolchinones bind to tubulin reversibly and are more effective at inhibiting microtubule formation than colchicine. 7-Acetamido-allocolchinone inhibits the growth of a number of tumor cell lines at concentrations about 100 times lower than colchicine. Also disclosed is a method of treating an individual with cancer by administering a composition which comprises a therapeutically effective amount of an allocolchinone which inhibits microtubule assembly. Administering a therapeutically effective amount of a composition which comprises an allocolchinone which inhibits microtubule assembly can also be used for treating inflammatory diseases, multiple sclerosis, primary biliary cirrhosis, Alzheimer's Disease and Behcet's Disease.
    Type: Grant
    Filed: March 11, 1996
    Date of Patent: June 2, 1998
    Assignee: Brandeis University
    Inventors: Serge M. Timasheff, Marina J. Gorbunoff, Bernardo Perez-Ramirez
  • Patent number: 5741814
    Abstract: Cyclooctadiene derivative of the following formula (1): ##STR1## wherein A.sup.1, A.sup.2, A.sup.3 and A.sup.4 each independently represent COOR.sup.5 (where R.sup.5 represents a hydrogen atom, a C.sub.1 -C.sub.10 alkyl group, a phenyl group, a C.sub.7 -C.sub.12 aralkyl group or CONR.sup.6 R.sup.7 (where R.sup.6 and R.sup.7 each independently represent a hydrogen atom, a C.sub.1 -C.sub.10 alkyl group or a phenyl group), or A.sup.1 and A.sup.2, and/or A.sup.3 and A.sup.4 may be combined together to represent group(s) of: ##STR2## in which X represents an oxygen atom or NR.sup.8 {where R.sup.8 represents a hydrogen atom, a C.sub.1 -C.sub.10 alkyl group or a phenyl group),R.sup.0, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 each independently represent a hydrogen atom, a halogen atom, a hydroxyl group and an C.sub.1 -C.sub.10 alkyl group,the symbol ------ represents a single or double bond, and when it is a double bond, then R.sup.1 and R.sup.
    Type: Grant
    Filed: September 3, 1996
    Date of Patent: April 21, 1998
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Yasuyuki Nakajima, Hisayuki Watanabe, Michiaki Adachi, Michito Tagawa, Mitsugu Futagawa, Takashi Furusato, Hiroshi Ohya, Masanori Nishioka
  • Patent number: 5726325
    Abstract: The present invention relates to tricyclic compounds represented by general formula (I) which are useful as therapeutic agents for urinary incontinence: ##STR1## wherein R.sup.1 represents hydrogen and the like; --X.sup.1 --X.sup.2 --X.sup.3 -- represents --CR.sup.2 .dbd.CR.sup.3 --CR.sup.4 .dbd.CR.sup.5 -- (wherein R.sup.2, R.sup.3, R.sup.4, and R.sup.5 represent hydrogen and the like) and the like; and Y represents --CH.sub.2 O-- and the like.
    Type: Grant
    Filed: June 6, 1997
    Date of Patent: March 10, 1998
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Makoto Yoshida, Shin-ichi Sasaki, Shigeru Aono, Shigeki Fujiwara, Haruki Takai, Tsuyoshi Yamagata, Ken Nagashima, Akira Karasawa
  • Patent number: 5705704
    Abstract: Novel tricyclic compounds of formula I as defined in the specification, a process for their preparation and their use for the preparation of optically active or racemic colchicine and thiocolchicine derivatives.
    Type: Grant
    Filed: March 1, 1996
    Date of Patent: January 6, 1998
    Assignee: Roussel Uclaf
    Inventors: Francis Brion, Bernadette Chappert, Christian Diolez, Christian Marie, Alain Mazurie, Michel Middendorp, Didier Pronine, Edmond Toromanoff
  • Patent number: 5705169
    Abstract: The invention relates to ketotricyclo?5.2.1.0!decane derivatives of the formula I ##STR1## wherein Phe is a phenylene group which is unsubstituted or substituted by 1 to 4 hydroxyl, alkyl or alkoxy groups having 1 to 10 C atoms,and their preparation and use as UV filters, in particular in cosmetic or pharmaceutical preparations.
    Type: Grant
    Filed: July 24, 1995
    Date of Patent: January 6, 1998
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Inge Stein, Michael Schwarz, Ulrich Heywang
  • Patent number: 5698595
    Abstract: Application of a compound having at least one sulfonic acid functional group which is at least partially non-neutralized, in a cosmetic or dermatological composition, to the skin is useful for treating intrinsic ageing of the skin.
    Type: Grant
    Filed: December 19, 1996
    Date of Patent: December 16, 1997
    Assignee: L'Oreal
    Inventors: Jean Paul Boelle, Jean-Pierre Laugier, Serge Forestier
  • Patent number: 5519027
    Abstract: New D-homo-(16-ene)-11.beta.-aryl-4-estrenes of general formula I ##STR1## as well as their pharmaceutically compatible addition salts with acids are described in whichX stands for an oxygen atom, the hydroxyimino grouping >N.about.OH or two hydrogen atoms,R.sup.1 stands for a hydrogen atom or a methyl group,R.sup.2 stands for an hydroxy group, a C.sub.1 -C.sub.10 alkoxy or C.sub.1 -C.sub.10 acyloxy group,R.sup.11 stands for a fluorine, chlorine or bromine atom, and then R.sup.12 and R.sup.13 together mean an additional bond orR.sup.11 stands for a straight-chain or branched-chain C.sub.1 -C.sub.4 -alkyl radical or a hydrogen atom, and then R.sup.12 and R.sup.13 each mean a hydrogen atom or together mean an additional bond,and R.sup.3 and R.sup.4 have the usual meanings indicated in the description for competitive progesterone antagonists.
    Type: Grant
    Filed: February 25, 1994
    Date of Patent: May 21, 1996
    Assignee: Schering Aktiengesellschaft
    Inventors: Wolfgang Schwede, Eckhard Ottow, Arwed Cleve, Walter Elger, Krzysztof Chwalisz, Martin Schneider
  • Patent number: 5514675
    Abstract: This invention provides methods of treating a physiological disorder associated with an excess of bradykinins in a mammal which comprises administering to a mammal in need of said treatment a compound selected from a series of substituted dihydronaphthalenes and naphthalenes.
    Type: Grant
    Filed: October 20, 1994
    Date of Patent: May 7, 1996
    Assignee: Eli Lilly and Company
    Inventors: Robert F. Bruns, Jr., Donald R. Gehlert, J. Jeffry Howbert, William H. W. Lunn
  • Patent number: 5500156
    Abstract: Compositions for use in non-linear optical devices. The compositions have first molecular electronic hyperpolarizability (.beta.) either positive or negative in sign and therefore display second order non-linear optical properties when incorporated into non-linear optical devices.
    Type: Grant
    Filed: April 11, 1994
    Date of Patent: March 19, 1996
    Assignee: California Institute of Technology
    Inventors: Seth R. Marder, Chin-Ti Chen, Lap-Tak Cheng
  • Patent number: 5492917
    Abstract: Novel compounds of the general structural formula I: ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, pulmonary hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, inflammatory diseases including Raynaud's disease and asthma.
    Type: Grant
    Filed: September 29, 1993
    Date of Patent: February 20, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Ralph A. Rivero, Peter D. Williams, Daniel F. Veber
  • Patent number: 5488180
    Abstract: This invention relates to complex hydrophobe compounds and to alkoxylation products, i.e., condensation reaction products of alkylene oxides and complex hydrophobe compounds having at least one active hydrogen. This invention also relates to alkoxylation products that have beneficial, narrow molecular weight ranges.
    Type: Grant
    Filed: May 29, 1992
    Date of Patent: January 30, 1996
    Assignee: Union Carbide Chemicals & Plastics Technology Corporation
    Inventors: Richard D. Jenkins, David R. Bassett, Danny E. Smith, John N. Argyropoulos, James E. Loftus, Gregory D. Shay
  • Patent number: 5480913
    Abstract: Disclosed are novel classes of anti-androgens including dihydrophenanthrene derivatives, their method of synthesis and their use in treating disorders associated with excessive androgenic activities.
    Type: Grant
    Filed: May 3, 1993
    Date of Patent: January 2, 1996
    Assignee: Arch Development Corporation
    Inventors: Shutsung Liao, John Pataki, Ronald G. Harvey
  • Patent number: 5478862
    Abstract: The invention is drawn to 17-oxo-15,16-seco-19-nor steroids which are useful as intermediates in the production of various 15,16-seco-19-nor progestins. These progestins display elevated progestational activity with a minimum of ancillary hormonal activity and are thus useful in the suppression of ovulation in the human female.
    Type: Grant
    Filed: May 13, 1994
    Date of Patent: December 26, 1995
    Assignee: SRI International
    Inventors: Richard H. Peters, Masato Tanabe
  • Patent number: 5476860
    Abstract: Diaromatic compounds, characterized in that they correspond to the following general formula: ##STR1## in which: R.sub.1 is --CH.sub.3, --CH.sub.2 OH, --COR.sub.8 or --CH.sub.2 OCOR.sub.9, R.sub.8 is H, OH, --OR.sub.10, --N(rr') or alkyl, R.sub.10 is alkyl, alkenyl, aryl or aralkyl, r and r' being H, alkyl, aryl, aralkyl, etc., r and r' together form a heterocycle, R.sub.9 is alkyl, alkenyl or a sugar residue, R.sub.2 and R.sub.3 are --OR.sub.11 or --OCOR.sub.11, R.sub.11 is H, alkyl, fluoroalkyl, aryl or aralkyl, R.sub.3 in addition being H, R.sub.4 is H, OH, alkyl, alkoxy, F, Cl or --CF.sub.3, R.sub.5 and R.sub.7 are H, OH, alkoxy, .alpha.-substituted alkyl or .alpha.,.alpha.'-disubstituted alkyl, etc., R.sub.6 is H, OH, alkyl, alkoxy, cycloalkyl, etc., R.sub.5 and R.sub.7 cannot simultaneously be OH or alkoxy and R.sub.4, R.sub.5, R.sub.6 and R.sub.7 cannot simultaneously be H, R.sub.5 and R.sub.6 or R.sub.6 and R.sub.
    Type: Grant
    Filed: December 8, 1993
    Date of Patent: December 19, 1995
    Assignee: Centre International de Recherches Dermatologiques (CIRD Galderma)
    Inventor: Jean-Michel Bernardon
  • Patent number: 5457108
    Abstract: The invention relates to substituted 5-oxo-di-benzo[a,d]cyclohepta-1,4-dienes of the formula (I) ##STR1## processes for their preparation and their use as retroviral agents.
    Type: Grant
    Filed: September 17, 1993
    Date of Patent: October 10, 1995
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hanno Wild, Jutta Hansen, Jorg Lautz, Arnold Paessens
  • Patent number: 5457239
    Abstract: A process for the preparation of a formylated aromatic compound comprising contacting an aromatic compound with (i) a halogenated compound in the presence of a Lewis acid, and (ii) a base, is described. The subject process provides an efficient and effective means of preparing formylated compounds which may be useful in a wide variety of applications.
    Type: Grant
    Filed: May 25, 1994
    Date of Patent: October 10, 1995
    Assignee: Union Camp Corporation
    Inventors: Walter C. Frank, Richard L. Veazey, John J. Mahurter, Mark J. Jenkins, Neil R. Fairfax
  • Patent number: 5405948
    Abstract: A compound of formula (I): selected from 1,5-diyne-3-cyclodecene and undecene compounds. ##STR1## in which: R represents a hydrogen atom, a straight-chain or branched (C.sub.1 -C.sub.6) acyl radical or a glycoside radical,R' represents a hydrogen atom ##STR2## n is 1 or 2, and R.sub.1 and R.sub.2 simultaneously represent two hydrogen atoms or, together with the two carbon atoms and the double bond to which they are attached, form a phenyl ring.
    Type: Grant
    Filed: September 30, 1992
    Date of Patent: April 11, 1995
    Assignee: Adir et Compagnie
    Inventors: Jean-Marie Beau, Christophe Crevisy, Ghanem Atassi, Alain Pierre
  • Patent number: 5380718
    Abstract: Arthropodicidal tetrahydropyridazines of Formulae I and II, ##STR1## wherein Q,X,X.sup.1 Y, and G are as defined in the text, compositions containing them and their use in the control of arthropods.
    Type: Grant
    Filed: November 12, 1992
    Date of Patent: January 10, 1995
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Charles R. Harrison, George P. Lahm, Thomas M. Stevenson
  • Patent number: 5329050
    Abstract: 1-Indanones of the formula IV or IVa ##STR1## in which R.sup.1 and R.sup.7 are preferably hydrogen or alkyl, or adjacent radicals R.sup.1 to R.sup.4 form a ring, are obtained in a one-step reaction by reacting a compound I ##STR2## with a compound of the formula II or a compound III ##STR3## in liquid hydrogen fluoride.
    Type: Grant
    Filed: April 27, 1993
    Date of Patent: July 12, 1994
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Laurent Weisse, Jurgen Rohrmann, Frank Kuber, Heinz Strutz
  • Patent number: 5232915
    Abstract: 9.alpha.-Hydroxy-19,11.beta.-bridged steroids of general formula I ##STR1## are described. The more detailed meaning of A, B, R.sup.1, R.sup.2, G, Z, R.sup.4 --Y and R.sup.4' --Y' follows from the description. The steroids of general formula I have antigestagen and/or antiglucocorticoidal action and can be used for the production of pharmaceutical agents.
    Type: Grant
    Filed: January 14, 1992
    Date of Patent: August 3, 1993
    Assignee: Schering Aktiengesellschaft
    Inventors: Eckhard Ottow, Gunter Neef, Rudolf Wiechert, Walter Elger, Sybille Beier, Karl-Heinrich Fritzemeier
  • Patent number: 5213709
    Abstract: A mesomorphic compound represented by the following formula (I): ##STR1## wherein R.sub.1 and R.sub.2 respectively denote an alkyl group having 1-16 carbon atoms optionally substituted; X.sub.1 and X.sub.3 respectively denote a single bond, --O--, ##STR2## X.sub.2 denotes a single bond, ##STR3## A.sub.1 denotes a single bond ##STR4## A.sub.3 denotes ##STR5## A.sub.2 denotes 9, 10-dihydro-2,7-phenanthrenediyl, 2,7-fluorenediyl or 2,7-fluorenonediyl; n is 0 or 1; and X.sub.4 and X.sub.5 respectively denote hydrogen, F, Cl, Br, --CH.sub.3, --CN or --CF.sub.3, with proviso that X.sub.1 is a single bond when A.sub.1 is a single bond.
    Type: Grant
    Filed: April 30, 1991
    Date of Patent: May 25, 1993
    Assignee: Canon Kabushiki Kaisha
    Inventors: Takao Takiguchi, Takashi Iwaki, Takeshi Togano, Yoko Yamada, Shinichi Nakamura
  • Patent number: 5208263
    Abstract: Disclosed are novel classes of anti-androgen including dihydrophenanthrene derivatives, their method of synthesis and their use in treating disorders associated with excessive androgenic activities.
    Type: Grant
    Filed: September 27, 1989
    Date of Patent: May 4, 1993
    Assignee: Arch Development Corporation
    Inventors: Shutsung Liao, John Pataki, Ronald G. Harvey
  • Patent number: 5192817
    Abstract: Novel phenanthrene derivatives represented by the general formula (1), ##STR1## wherein the group of the formula ##STR2## is a group of the formula ##STR3## (wherein R.sup.1 is a hydrogen atom or a lower alkyl group), a group of the formula ##STR4## (wherein R.sup.2 is a hydrogen atom or a lower alkanoyl group) or a group of the formula ##STR5## (wherein R.sup.2 is the same as defined above), and salts thereof, and other compounds derived therefrom and salts thereof; processes for preparing the same; and interleukin-1 (IL-1) inhibitors containing the abovementioned novel phenanthrene derivatives as to the active ingredient(s).
    Type: Grant
    Filed: November 5, 1991
    Date of Patent: March 9, 1993
    Assignees: Otsuka Pharmaceutical Co., Ltd., Otsuka Pharmaceutical Factory, Inc.
    Inventors: Yoshihisa Takaishi, Kiyoto Goto, Takuji Uesako, Toshiko Kuwahara, Masaaki Takai, Yukihisa Ono, Yoshihiro Taniguchi, Sachiko Manabe, Takahiro Asakuni
  • Patent number: 5185447
    Abstract: Ketones having formulas (1)-(3) are provided by improved methods which involve the treatment of compounds having formulas (9)-(11) with aqueous base. ##STR1## wherein R.sub.x is NO.sub.2.
    Type: Grant
    Filed: January 29, 1992
    Date of Patent: February 9, 1993
    Assignee: Du Pont Merck Pharmaceutical Company
    Inventor: Edward C. Crapps
  • Patent number: 5183942
    Abstract: Macrocyclic enediynediols and enediynediones having a ten carbon ring and open chain enediyne dihydroperoxides having eight carbons between the hydroperoxide groups that cleave DNA are disclosed, as are methods of making and using the same.
    Type: Grant
    Filed: November 5, 1991
    Date of Patent: February 2, 1993
    Assignee: The Scripps Research Institute
    Inventors: Kyriacos C. Nicolaou, Erik Sorensen, Chan-Kou Hwang, Robert Discordia, Robert G. Bergman, Robert E. Minto
  • Patent number: 5162588
    Abstract: Compound of formula ##STR1## wherein a) indexes m and n are identical and stand each for an integer number equal to zero, symbols R.sup.1 and R.sup.2 are identical and represent each a hydrogen atom, or are different and represent each a hydrogen atom or a methyl radical, symbols R.sup.5 and R.sup.8 stand each for a methyl radical, symbols R.sup.6 and R.sup.7 can be identical or different and designate each a hydrogen atom or a methyl radical and, either symbol R.sup.4 represents a methyl radical and symbol R.sup.3 stands for a hydrogen atom or a methyl radical, or symbols R.sup.3 and R.sup.4 represent each a methylene radical belonging to a ring such as indicated by the dotted line, with the proviso that the following combinations are excluded:1. R.sup.1 =R.sup.2 =R.sup.3 =R.sup.6 =R.sup.7 =H, or2. R.sup.1 =R.sup.2 =R.sup.3 =H and R.sup.6 or R.sup.7 =CH.sub.3, or3. R.sup.2 =CH.sub.3 and R.sup.3 =R.sup.6 =R.sup.7 =H, or4. R.sup.2 =CH.sub.3 and R.sup.3 =H and R.sup.6 or R.sup.7 =CH.sub.3, or5. R.sup.1 =R.sup.
    Type: Grant
    Filed: June 26, 1990
    Date of Patent: November 10, 1992
    Assignee: Firmenich S.A.
    Inventors: Charles Fehr, Jose Galindo
  • Patent number: 5144081
    Abstract: The invention relates to dialkoxybenzylidene-camphor derivatives of the formula I ##STR1## in which R.sup.1 and R.sup.2, in each case independently of one another, are a straight-chain or branched alkyl radical having 1 to 10 c atoms, andX is H or SO.sub.3 H,and to a process for their preparation and their use in cosmetic and pharmaceutical preparations.
    Type: Grant
    Filed: September 4, 1991
    Date of Patent: September 1, 1992
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Ulrich Heywang, Roland Martin, Ingeborg Stein
  • Patent number: 5140044
    Abstract: A UCN-1028D derivative represented by the formula: ##STR1## has protein kinase C inhibitory activity and is expected to be used as an active ingredient in anti-tumor agents, etc.
    Type: Grant
    Filed: March 27, 1990
    Date of Patent: August 18, 1992
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Teruo Kishi, Hiromitsu Saito, Hiroshi Sano, Isami Takahashi, Tatsuya Tamaoki
  • Patent number: 5136099
    Abstract: 5-Hydroxy-benzo-(1',2')-cyclodeca-2,7-diyne-1-one and derivatives thereof and related fused ring diyneone macrocyclic compounds are disclosed. The compounds possess DNA-cleaving, antibiotic and tumor growth-inhibiting properties. Methods of making and using the same are also disclosed.
    Type: Grant
    Filed: August 1, 1990
    Date of Patent: August 4, 1992
    Assignee: Scripps Clinic and Research Foundation
    Inventors: Golfo Skokotas, Kyriacos C. Nicolaou
  • Patent number: 5117062
    Abstract: A novel synthesis of aromatic tertiary amines involves reacting an aromatic anil and an aromatic ether in a molar ratio of 1:1; adjusting the ratio to 2:1 produces novel enamines and by employing a two step process for enamine production, various unsymmetrically substituted enamines can be obtained which are readily hydrolyzed to corresponding deoxybenzoins which in turn are readily oxidized to benzils, the aromatic tertiary amines may be used to produce charge transport layers in xerography, while the benzils may be used to produce a variety of desired polymers.
    Type: Grant
    Filed: January 22, 1991
    Date of Patent: May 26, 1992
    Inventors: Allan S. Hay, Martino Paventi
  • Patent number: 5100921
    Abstract: New angucyclinones with a therapeutic action can be prepared with the aid of a strain of the genus Streptomyces.
    Type: Grant
    Filed: April 25, 1989
    Date of Patent: March 31, 1992
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Susanne Grabley, Joachim Wink, Carlo Giani, Gerhard Seibert, Wolfgang Raether, Susanne Dobreff, Axel Zeeck
  • Patent number: 5095099
    Abstract: This invention concerns novel fluorescent compositions having the potential for absorption of visible and UV radiation and for re-emitting the radiation at longer wavelengths. The compositions comprise rare earth chelates containing a phenalenone nucleus.
    Type: Grant
    Filed: December 10, 1990
    Date of Patent: March 10, 1992
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Bruce A. Parkinson, Andrew Streitwieser, Jr., Douglas W. Wiley